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Identification
NameDasatinib
Accession NumberDB01254
TypeSmall Molecule
GroupsApproved, Investigational
Description

Dasatinib is an oral dual BCR/ABL and Src family tyrosine kinase inhibitor approved for use in patients with chronic myelogenous leukemia (CML). The main targets of Dasatinib, are BCRABL, SRC, Ephrins and GFR.

Structure
Thumb
Synonyms
Anh. dasatinib
Anhydrous dasatinib
BMS dasatinib
BMS-354825
Dasatinib
Dasatinib (anh.)
Dasatinibum
N-(2-CHLORO-6-methylphenyl)-2-({6-[4-(2-hydroxyethyl)piperazin-1-yl]-2-methylpyrimidin-4-yl}amino)-1,3-thiazole-5-carboxamide
External Identifiers
  • BMS-354825
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Spryceltablet50 mgoralBristol Myers Squibb Canada2007-04-13Not applicableCanada
Spryceltablet70 mg/1oralE.R. Squibb & Sons, L.L.C.2006-06-272016-04-23Us
Spryceltablet20 mgoralBristol Myers Squibb Canada2007-04-13Not applicableCanada
Spryceltablet70 mg/1oralPhysicians Total Care, Inc.2007-02-122016-04-05Us
Spryceltablet140 mg/1oralE.R. Squibb & Sons, L.L.C.2010-10-282016-04-23Us
Spryceltablet140 mgoralBristol Myers Squibb Canada2011-03-29Not applicableCanada
Spryceltablet80 mg/1oralE.R. Squibb & Sons, L.L.C.2010-10-282016-04-23Us
Spryceltablet80 mgoralBristol Myers Squibb Canada2011-09-02Not applicableCanada
Spryceltablet100 mg/1oralE.R. Squibb & Sons, L.L.C.2008-05-302016-04-23Us
Spryceltablet100 mgoralBristol Myers Squibb Canada2009-05-04Not applicableCanada
Spryceltablet50 mg/1oralE.R. Squibb & Sons, L.L.C.2006-06-272016-04-23Us
Spryceltablet70 mgoralBristol Myers Squibb Canada2007-04-13Not applicableCanada
Spryceltablet20 mg/1oralE.R. Squibb & Sons, L.L.C.2006-06-272016-04-23Us
Generic Prescription ProductsNot Available
Over the Counter ProductsNot Available
International BrandsNot Available
Brand mixturesNot Available
SaltsNot Available
Categories
UNIIX78UG0A0RN
CAS number302962-49-8
WeightAverage: 488.006
Monoisotopic: 487.155721508
Chemical FormulaC22H26ClN7O2S
InChI KeyInChIKey=ZBNZXTGUTAYRHI-UHFFFAOYSA-N
InChI
InChI=1S/C22H26ClN7O2S/c1-14-4-3-5-16(23)20(14)28-21(32)17-13-24-22(33-17)27-18-12-19(26-15(2)25-18)30-8-6-29(7-9-30)10-11-31/h3-5,12-13,31H,6-11H2,1-2H3,(H,28,32)(H,24,25,26,27)
IUPAC Name
N-(2-chloro-6-methylphenyl)-2-({6-[4-(2-hydroxyethyl)piperazin-1-yl]-2-methylpyrimidin-4-yl}amino)-1,3-thiazole-5-carboxamide
SMILES
CC1=NC(NC2=NC=C(S2)C(=O)NC2=C(C)C=CC=C2Cl)=CC(=N1)N1CCN(CCO)CC1
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as n-arylpiperazines. These are organic compounds containing a piperazine ring where the nitrogen ring atom carries an aryl group.
KingdomOrganic compounds
Super ClassOrganoheterocyclic compounds
ClassDiazinanes
Sub ClassPiperazines
Direct ParentN-arylpiperazines
Alternative Parents
Substituents
  • N-arylpiperazine
  • N-arylamide
  • Aminotoluene
  • Dialkylarylamine
  • Thiazolecarboxylic acid or derivatives
  • Thiazolecarboxamide
  • N-alkylpiperazine
  • Toluene
  • Halobenzene
  • Chlorobenzene
  • Aminopyrimidine
  • 2,5-disubstituted 1,3-thiazole
  • Imidolactam
  • Benzenoid
  • Pyrimidine
  • Monocyclic benzene moiety
  • Aryl halide
  • Aryl chloride
  • Heteroaromatic compound
  • Thiazole
  • Azole
  • Tertiary aliphatic amine
  • Tertiary amine
  • Secondary carboxylic acid amide
  • Carboxamide group
  • 1,2-aminoalcohol
  • Azacycle
  • Secondary amine
  • Carboxylic acid derivative
  • Alkanolamine
  • Hydrocarbon derivative
  • Primary alcohol
  • Organooxygen compound
  • Organonitrogen compound
  • Organochloride
  • Organohalogen compound
  • Carbonyl group
  • Amine
  • Alcohol
  • Aromatic heteromonocyclic compound
Molecular FrameworkAromatic heteromonocyclic compounds
External Descriptors
Pharmacology
IndicationFor the treatment of adults with chronic, accelerated, or myeloid or lymphoid blast phase chronic myeloid leukemia with resistance or intolerance to prior therapy. Also indicated for the treatment of adults with Philadelphia chromosome-positive acute lymphoblastic leukemia with resistance or intolerance to prior therapy.
PharmacodynamicsDasatinib is an oral dual BCR/ABL and Src family tyrosine kinase inhibitor
Mechanism of actionDasatinib, at nanomolar concentrations, inhibits the following kinases: BCR-ABL, SRC family (SRC, LCK, YES, FYN), c-KIT, EPHA2, and PDGFRβ. Based on modeling studies, dasatinib is predicted to bind to multiple conformations of the ABL kinase. In vitro, dasatinib was active in leukemic cell lines representing variants of imatinib mesylate sensitive and resistant disease. Dasatinib inhibited the growth of chronic myeloid leukemia (CML) and acute lymphoblastic leukemia (ALL) cell lines overexpressing BCR-ABL. Under the conditions of the assays, dasatinib was able to overcome imatinib resistance resulting from BCR-ABL kinase domain mutations, activation of alternate signaling pathways involving the SRC family kinases (LYN, HCK), and multi-drug resistance gene overexpression.
Related Articles
AbsorptionNot Available
Volume of distribution
  • 2505 L
Protein binding96%
Metabolism

Dasatinib is extensively metabolized in humans, primarily by the cytochrome P450 enzyme 3A4

Route of eliminationDasatinib is extensively metabolized in humans, primarily by the cytochrome P450 enzyme 3A4. Elimination is primarily via the feces.
Half lifeThe overall mean terminal half-life of dasatinib is 3-5 hours.
ClearanceNot Available
ToxicityAcute overdose in animals was associated with cardiotoxicity.
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9852
Blood Brain Barrier-0.507
Caco-2 permeable-0.5638
P-glycoprotein substrateSubstrate0.6562
P-glycoprotein inhibitor IInhibitor0.5371
P-glycoprotein inhibitor IIInhibitor0.5425
Renal organic cation transporterNon-inhibitor0.7288
CYP450 2C9 substrateNon-substrate0.7061
CYP450 2D6 substrateNon-substrate0.8152
CYP450 3A4 substrateSubstrate0.5704
CYP450 1A2 substrateNon-inhibitor0.5612
CYP450 2C9 inhibitorInhibitor0.8008
CYP450 2D6 inhibitorNon-inhibitor0.8358
CYP450 2C19 inhibitorInhibitor0.574
CYP450 3A4 inhibitorInhibitor0.7295
CYP450 inhibitory promiscuityHigh CYP Inhibitory Promiscuity0.8343
Ames testNon AMES toxic0.7185
CarcinogenicityNon-carcinogens0.7308
BiodegradationNot ready biodegradable0.9863
Rat acute toxicity2.4772 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.8538
hERG inhibition (predictor II)Inhibitor0.718
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
ManufacturersNot Available
Packagers
Dosage forms
FormRouteStrength
Tabletoral100 mg/1
Tabletoral100 mg
Tabletoral140 mg/1
Tabletoral140 mg
Tabletoral20 mg
Tabletoral20 mg/1
Tabletoral50 mg
Tabletoral50 mg/1
Tabletoral70 mg/1
Tabletoral70 mg
Tabletoral80 mg
Tabletoral80 mg/1
Prices
Unit descriptionCostUnit
Sprycel 100 mg tablet278.24USD tablet
Sprycel 50 mg tablet139.12USD tablet
Sprycel 70 mg tablet139.12USD tablet
Sprycel 20 mg tablet69.56USD tablet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
CA2366932 No2009-08-252020-04-12Canada
US6596746 No2000-06-282020-06-28Us
US7125875 No2000-04-132020-04-13Us
US7153856 No2000-04-282020-04-28Us
US7491725 No2006-03-282026-03-28Us
US8680103 No2005-02-042025-02-04Us
Properties
StateSolid
Experimental Properties
PropertyValueSource
melting point280-286 °CNot Available
logP1.8Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.0128 mg/mLALOGPS
logP2.77ALOGPS
logP3.82ChemAxon
logS-4.6ALOGPS
pKa (Strongest Acidic)8.49ChemAxon
pKa (Strongest Basic)7.22ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count8ChemAxon
Hydrogen Donor Count3ChemAxon
Polar Surface Area106.51 Å2ChemAxon
Rotatable Bond Count7ChemAxon
Refractivity133.08 m3·mol-1ChemAxon
Polarizability51.58 Å3ChemAxon
Number of Rings4ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
SpectraNot Available
References
Synthesis ReferenceUS6596746
General References
  1. Das J, Chen P, Norris D, Padmanabha R, Lin J, Moquin RV, Shen Z, Cook LS, Doweyko AM, Pitt S, Pang S, Shen DR, Fang Q, de Fex HF, McIntyre KW, Shuster DJ, Gillooly KM, Behnia K, Schieven GL, Wityak J, Barrish JC: 2-aminothiazole as a novel kinase inhibitor template. Structure-activity relationship studies toward the discovery of N-(2-chloro-6-methylphenyl)-2-[[6-[4-(2-hydroxyethyl)-1- piperazinyl)]-2-methyl-4-pyrimidinyl]amino)]-1,3-thiazole-5-carboxamide (dasatinib, BMS-354825) as a potent pan-Src kinase inhibitor. J Med Chem. 2006 Nov 16;49(23):6819-32. [PubMed:17154512 ]
  2. Talpaz M, Shah NP, Kantarjian H, Donato N, Nicoll J, Paquette R, Cortes J, O'Brien S, Nicaise C, Bleickardt E, Blackwood-Chirchir MA, Iyer V, Chen TT, Huang F, Decillis AP, Sawyers CL: Dasatinib in imatinib-resistant Philadelphia chromosome-positive leukemias. N Engl J Med. 2006 Jun 15;354(24):2531-41. [PubMed:16775234 ]
External Links
ATC CodesL01XE06
AHFS CodesNot Available
PDB EntriesNot Available
FDA labelDownload (237 KB)
MSDSNot Available
Interactions
Drug Interactions
Drug
AbciximabDasatinib may increase the anticoagulant activities of Abciximab.
AcenocoumarolDasatinib may increase the anticoagulant activities of Acenocoumarol.
AcetaminophenAcetaminophen may increase the hepatotoxic activities of Dasatinib.
Acetylsalicylic acidDasatinib may increase the anticoagulant activities of Acetylsalicylic acid.
ado-trastuzumab emtansineThe serum concentration of ado-trastuzumab emtansine can be increased when it is combined with Dasatinib.
AlfentanilThe serum concentration of Alfentanil can be increased when it is combined with Dasatinib.
AlfuzosinThe serum concentration of Alfuzosin can be increased when it is combined with Dasatinib.
AlitretinoinThe serum concentration of Alitretinoin can be increased when it is combined with Dasatinib.
AlprazolamThe serum concentration of Alprazolam can be increased when it is combined with Dasatinib.
Aluminum hydroxideAluminum hydroxide can cause a decrease in the absorption of Dasatinib resulting in a reduced serum concentration and potentially a decrease in efficacy.
AminophyllineThe serum concentration of Aminophylline can be increased when it is combined with Dasatinib.
AmlodipineThe serum concentration of Amlodipine can be increased when it is combined with Dasatinib.
ApixabanDasatinib may increase the anticoagulant activities of Apixaban.
AprepitantThe serum concentration of Aprepitant can be increased when it is combined with Dasatinib.
ArgatrobanDasatinib may increase the anticoagulant activities of Argatroban.
AripiprazoleThe serum concentration of Aripiprazole can be increased when it is combined with Dasatinib.
ArmodafinilThe serum concentration of Armodafinil can be increased when it is combined with Dasatinib.
AtazanavirThe serum concentration of Dasatinib can be increased when it is combined with Atazanavir.
AtorvastatinThe serum concentration of Atorvastatin can be increased when it is combined with Dasatinib.
AvanafilThe serum concentration of Avanafil can be increased when it is combined with Dasatinib.
AxitinibThe serum concentration of Axitinib can be increased when it is combined with Dasatinib.
BenzphetamineThe serum concentration of Benzphetamine can be increased when it is combined with Dasatinib.
BexaroteneThe serum concentration of Dasatinib can be decreased when it is combined with Bexarotene.
BisoprololThe serum concentration of Bisoprolol can be increased when it is combined with Dasatinib.
BivalirudinDasatinib may increase the anticoagulant activities of Bivalirudin.
BoceprevirThe serum concentration of Dasatinib can be increased when it is combined with Boceprevir.
BosentanThe serum concentration of Dasatinib can be decreased when it is combined with Bosentan.
BosutinibThe serum concentration of Bosutinib can be increased when it is combined with Dasatinib.
BrexpiprazoleThe serum concentration of Brexpiprazole can be increased when it is combined with Dasatinib.
BromocriptineThe serum concentration of Bromocriptine can be increased when it is combined with Dasatinib.
BudesonideThe serum concentration of Budesonide can be increased when it is combined with Dasatinib.
BuprenorphineThe serum concentration of Buprenorphine can be increased when it is combined with Dasatinib.
BuspironeThe serum concentration of Buspirone can be increased when it is combined with Dasatinib.
CabazitaxelThe serum concentration of Cabazitaxel can be increased when it is combined with Dasatinib.
CabozantinibThe serum concentration of Cabozantinib can be increased when it is combined with Dasatinib.
CalcitriolThe serum concentration of Calcitriol can be increased when it is combined with Dasatinib.
Calcium carbonateCalcium carbonate can cause a decrease in the absorption of Dasatinib resulting in a reduced serum concentration and potentially a decrease in efficacy.
CangrelorDasatinib may increase the anticoagulant activities of Cangrelor.
CarbamazepineThe serum concentration of Dasatinib can be decreased when it is combined with Carbamazepine.
CeritinibThe serum concentration of Dasatinib can be increased when it is combined with Ceritinib.
ChlordiazepoxideThe serum concentration of Chlordiazepoxide can be increased when it is combined with Dasatinib.
ChloroquineThe serum concentration of Chloroquine can be increased when it is combined with Dasatinib.
CilostazolDasatinib may increase the anticoagulant activities of Cilostazol.
CimetidineCimetidine can cause a decrease in the absorption of Dasatinib resulting in a reduced serum concentration and potentially a decrease in efficacy.
CinacalcetThe serum concentration of Cinacalcet can be increased when it is combined with Dasatinib.
CitalopramDasatinib may increase the QTc-prolonging activities of Citalopram.
Citric AcidDasatinib may increase the anticoagulant activities of Citric Acid.
ClarithromycinThe serum concentration of Dasatinib can be increased when it is combined with Clarithromycin.
ClonazepamThe serum concentration of Clonazepam can be increased when it is combined with Dasatinib.
ClopidogrelDasatinib may increase the anticoagulant activities of Clopidogrel.
ClorazepateThe serum concentration of Clorazepate can be increased when it is combined with Dasatinib.
ClozapineThe risk or severity of adverse effects can be increased when Dasatinib is combined with Clozapine.
CobicistatThe serum concentration of Dasatinib can be increased when it is combined with Cobicistat.
CobimetinibThe serum concentration of Cobimetinib can be increased when it is combined with Dasatinib.
CocaineThe serum concentration of Cocaine can be increased when it is combined with Dasatinib.
ColchicineThe serum concentration of Colchicine can be increased when it is combined with Dasatinib.
ConivaptanThe serum concentration of Dasatinib can be increased when it is combined with Conivaptan.
CrizotinibThe serum concentration of Crizotinib can be increased when it is combined with Dasatinib.
CyclosporineThe serum concentration of Cyclosporine can be increased when it is combined with Dasatinib.
Cyproterone acetateThe serum concentration of Cyproterone acetate can be increased when it is combined with Dasatinib.
Dabigatran etexilateDasatinib may increase the anticoagulant activities of Dabigatran etexilate.
DabrafenibThe serum concentration of Dasatinib can be decreased when it is combined with Dabrafenib.
DaclatasvirThe serum concentration of Daclatasvir can be increased when it is combined with Dasatinib.
DalteparinDasatinib may increase the anticoagulant activities of Dalteparin.
DanaparoidDasatinib may increase the anticoagulant activities of Danaparoid.
DantroleneThe serum concentration of Dantrolene can be increased when it is combined with Dasatinib.
DapsoneThe serum concentration of Dapsone can be increased when it is combined with Dasatinib.
DarifenacinThe serum concentration of Darifenacin can be increased when it is combined with Dasatinib.
DarunavirThe serum concentration of Dasatinib can be increased when it is combined with Darunavir.
DeferasiroxThe serum concentration of Dasatinib can be decreased when it is combined with Deferasirox.
DenosumabThe risk or severity of adverse effects can be increased when Denosumab is combined with Dasatinib.
DesirudinDasatinib may increase the anticoagulant activities of Desirudin.
DesvenlafaxineDasatinib may increase the anticoagulant activities of Desvenlafaxine.
DexamethasoneThe serum concentration of Dasatinib can be decreased when it is combined with Dexamethasone.
DiazepamThe serum concentration of Diazepam can be increased when it is combined with Dasatinib.
DiclofenacDasatinib may increase the anticoagulant activities of Diclofenac.
DicoumarolDasatinib may increase the anticoagulant activities of Dicoumarol.
DiflunisalDasatinib may increase the anticoagulant activities of Diflunisal.
DihydroergotamineThe serum concentration of Dihydroergotamine can be increased when it is combined with Dasatinib.
DiltiazemThe serum concentration of Diltiazem can be increased when it is combined with Dasatinib.
DipyridamoleDasatinib may increase the anticoagulant activities of Dipyridamole.
DocetaxelThe serum concentration of Docetaxel can be increased when it is combined with Dasatinib.
DofetilideDasatinib may increase the QTc-prolonging activities of Dofetilide.
DoxazosinThe serum concentration of Doxazosin can be increased when it is combined with Dasatinib.
DoxorubicinThe serum concentration of Doxorubicin can be increased when it is combined with Dasatinib.
DuloxetineDasatinib may increase the anticoagulant activities of Duloxetine.
Edetic AcidDasatinib may increase the anticoagulant activities of Edetic Acid.
EdoxabanDasatinib may increase the anticoagulant activities of Edoxaban.
EletriptanThe serum concentration of Eletriptan can be increased when it is combined with Dasatinib.
EnoxaparinDasatinib may increase the anticoagulant activities of Enoxaparin.
EnzalutamideThe serum concentration of Dasatinib can be decreased when it is combined with Enzalutamide.
EplerenoneThe serum concentration of Eplerenone can be increased when it is combined with Dasatinib.
EptifibatideDasatinib may increase the anticoagulant activities of Eptifibatide.
Ergoloid mesylateThe serum concentration of Ergoloid mesylate can be increased when it is combined with Dasatinib.
ErgonovineThe serum concentration of Ergonovine can be increased when it is combined with Dasatinib.
ErgotamineThe serum concentration of Ergotamine can be increased when it is combined with Dasatinib.
ErlotinibThe serum concentration of Erlotinib can be increased when it is combined with Dasatinib.
ErythromycinThe serum concentration of Erythromycin can be increased when it is combined with Dasatinib.
EsomeprazoleThe serum concentration of Dasatinib can be decreased when it is combined with Esomeprazole.
EszopicloneThe serum concentration of Eszopiclone can be increased when it is combined with Dasatinib.
EthosuximideThe serum concentration of Ethosuximide can be increased when it is combined with Dasatinib.
Ethyl biscoumacetateDasatinib may increase the anticoagulant activities of Ethyl biscoumacetate.
EtodolacDasatinib may increase the anticoagulant activities of Etodolac.
EtoposideThe serum concentration of Etoposide can be increased when it is combined with Dasatinib.
EverolimusThe serum concentration of Everolimus can be increased when it is combined with Dasatinib.
FamotidineFamotidine can cause a decrease in the absorption of Dasatinib resulting in a reduced serum concentration and potentially a decrease in efficacy.
FelbamateThe serum concentration of Felbamate can be increased when it is combined with Dasatinib.
FelodipineThe serum concentration of Felodipine can be increased when it is combined with Dasatinib.
FenoprofenDasatinib may increase the anticoagulant activities of Fenoprofen.
FentanylThe serum concentration of Fentanyl can be increased when it is combined with Dasatinib.
FesoterodineThe serum concentration of Fesoterodine can be increased when it is combined with Dasatinib.
FlibanserinThe serum concentration of Flibanserin can be increased when it is combined with Dasatinib.
FloctafenineDasatinib may increase the anticoagulant activities of Floctafenine.
FluconazoleThe metabolism of Dasatinib can be decreased when combined with Fluconazole.
FlunisolideThe serum concentration of Flunisolide can be increased when it is combined with Dasatinib.
FlurazepamThe serum concentration of Flurazepam can be increased when it is combined with Dasatinib.
FlurbiprofenDasatinib may increase the anticoagulant activities of Flurbiprofen.
FlutamideThe serum concentration of Flutamide can be increased when it is combined with Dasatinib.
FluvoxamineDasatinib may increase the anticoagulant activities of Fluvoxamine.
Fondaparinux sodiumDasatinib may increase the anticoagulant activities of Fondaparinux sodium.
FosaprepitantThe serum concentration of Dasatinib can be increased when it is combined with Fosaprepitant.
FosphenytoinThe serum concentration of Dasatinib can be decreased when it is combined with Fosphenytoin.
Fusidic AcidThe serum concentration of Dasatinib can be increased when it is combined with Fusidic Acid.
GefitinibThe serum concentration of Gefitinib can be increased when it is combined with Dasatinib.
GoserelinDasatinib may increase the QTc-prolonging activities of Goserelin.
GuanfacineThe serum concentration of Guanfacine can be increased when it is combined with Dasatinib.
HaloperidolThe serum concentration of Haloperidol can be increased when it is combined with Dasatinib.
HeparinDasatinib may increase the anticoagulant activities of Heparin.
HydrocodoneThe serum concentration of Hydrocodone can be increased when it is combined with Dasatinib.
Hydroxyprogesterone caproateThe serum concentration of Hydroxyprogesterone caproate can be increased when it is combined with Dasatinib.
IbrutinibThe serum concentration of Ibrutinib can be increased when it is combined with Dasatinib.
IbuprofenDasatinib may increase the anticoagulant activities of Ibuprofen.
IdelalisibThe serum concentration of Dasatinib can be increased when it is combined with Idelalisib.
IndinavirThe serum concentration of Dasatinib can be increased when it is combined with Indinavir.
IndomethacinDasatinib may increase the anticoagulant activities of Indomethacin.
IrinotecanThe serum concentration of Irinotecan can be increased when it is combined with Dasatinib.
IsavuconazoniumThe serum concentration of Isavuconazonium can be increased when it is combined with Dasatinib.
IsosorbideThe serum concentration of Isosorbide can be increased when it is combined with Dasatinib.
Isosorbide DinitrateThe serum concentration of Isosorbide Dinitrate can be increased when it is combined with Dasatinib.
Isosorbide MononitrateThe serum concentration of Isosorbide Mononitrate can be increased when it is combined with Dasatinib.
IsradipineThe serum concentration of Isradipine can be increased when it is combined with Dasatinib.
ItraconazoleThe serum concentration of Dasatinib can be increased when it is combined with Itraconazole.
IvabradineThe serum concentration of Ivabradine can be increased when it is combined with Dasatinib.
IvacaftorThe serum concentration of Dasatinib can be increased when it is combined with Ivacaftor.
IxabepiloneThe serum concentration of Ixabepilone can be increased when it is combined with Dasatinib.
KetamineThe serum concentration of Ketamine can be increased when it is combined with Dasatinib.
KetoconazoleThe serum concentration of Dasatinib can be increased when it is combined with Ketoconazole.
KetoprofenDasatinib may increase the anticoagulant activities of Ketoprofen.
KetorolacDasatinib may increase the anticoagulant activities of Ketorolac.
LansoprazoleThe serum concentration of Dasatinib can be decreased when it is combined with Lansoprazole.
LapatinibThe serum concentration of Lapatinib can be increased when it is combined with Dasatinib.
LeflunomideThe risk or severity of adverse effects can be increased when Dasatinib is combined with Leflunomide.
LeuprolideDasatinib may increase the QTc-prolonging activities of Leuprolide.
LevomilnacipranDasatinib may increase the anticoagulant activities of Levomilnacipran.
LidocaineThe serum concentration of Lidocaine can be increased when it is combined with Dasatinib.
LomitapideThe serum concentration of Lomitapide can be increased when it is combined with Dasatinib.
LovastatinThe serum concentration of Lovastatin can be increased when it is combined with Dasatinib.
LuliconazoleThe serum concentration of Dasatinib can be increased when it is combined with Luliconazole.
LurasidoneThe serum concentration of Lurasidone can be increased when it is combined with Dasatinib.
MACITENTANThe serum concentration of MACITENTAN can be increased when it is combined with Dasatinib.
Magnesium hydroxideMagnesium hydroxide can cause a decrease in the absorption of Dasatinib resulting in a reduced serum concentration and potentially a decrease in efficacy.
Magnesium oxideMagnesium oxide can cause a decrease in the absorption of Dasatinib resulting in a reduced serum concentration and potentially a decrease in efficacy.
MaravirocThe serum concentration of Maraviroc can be increased when it is combined with Dasatinib.
Mefenamic acidDasatinib may increase the anticoagulant activities of Mefenamic acid.
MefloquineThe serum concentration of Mefloquine can be increased when it is combined with Dasatinib.
MeloxicamDasatinib may increase the anticoagulant activities of Meloxicam.
MetamizoleThe risk or severity of adverse effects can be increased when Metamizole is combined with Dasatinib.
MethadoneThe serum concentration of Methadone can be increased when it is combined with Dasatinib.
MidazolamThe serum concentration of Midazolam can be increased when it is combined with Dasatinib.
MifepristoneThe serum concentration of Dasatinib can be increased when it is combined with Mifepristone.
MilnacipranDasatinib may increase the anticoagulant activities of Milnacipran.
MirtazapineThe serum concentration of Mirtazapine can be increased when it is combined with Dasatinib.
MitotaneThe serum concentration of Dasatinib can be decreased when it is combined with Mitotane.
ModafinilThe serum concentration of Modafinil can be increased when it is combined with Dasatinib.
NabumetoneDasatinib may increase the anticoagulant activities of Nabumetone.
NadroparinDasatinib may increase the anticoagulant activities of Nadroparin.
NaloxegolThe serum concentration of Naloxegol can be increased when it is combined with Dasatinib.
NaproxenDasatinib may increase the anticoagulant activities of Naproxen.
NatalizumabThe risk or severity of adverse effects can be increased when Dasatinib is combined with Natalizumab.
NateglinideThe serum concentration of Nateglinide can be increased when it is combined with Dasatinib.
NefazodoneThe serum concentration of Dasatinib can be increased when it is combined with Nefazodone.
NelfinavirThe serum concentration of Dasatinib can be increased when it is combined with Nelfinavir.
NetupitantThe serum concentration of Dasatinib can be increased when it is combined with Netupitant.
NicardipineThe serum concentration of Nicardipine can be increased when it is combined with Dasatinib.
NifedipineThe serum concentration of Nifedipine can be increased when it is combined with Dasatinib.
NimodipineThe serum concentration of Nimodipine can be increased when it is combined with Dasatinib.
NisoldipineThe serum concentration of Nisoldipine can be increased when it is combined with Dasatinib.
NizatidineNizatidine can cause a decrease in the absorption of Dasatinib resulting in a reduced serum concentration and potentially a decrease in efficacy.
OlaparibThe serum concentration of Olaparib can be increased when it is combined with Dasatinib.
OmeprazoleThe serum concentration of Dasatinib can be decreased when it is combined with Omeprazole.
OxaprozinDasatinib may increase the anticoagulant activities of Oxaprozin.
OxycodoneThe serum concentration of Oxycodone can be increased when it is combined with Dasatinib.
PaclitaxelThe serum concentration of Paclitaxel can be increased when it is combined with Dasatinib.
PalbociclibThe serum concentration of Dasatinib can be increased when it is combined with Palbociclib.
PanobinostatThe serum concentration of Panobinostat can be increased when it is combined with Dasatinib.
PantoprazoleThe serum concentration of Dasatinib can be decreased when it is combined with Pantoprazole.
ParoxetineDasatinib may increase the anticoagulant activities of Paroxetine.
PazopanibThe serum concentration of Pazopanib can be increased when it is combined with Dasatinib.
PhenindioneDasatinib may increase the anticoagulant activities of Phenindione.
PhenobarbitalThe serum concentration of Dasatinib can be decreased when it is combined with Phenobarbital.
PhenprocoumonDasatinib may increase the anticoagulant activities of Phenprocoumon.
PhenytoinThe serum concentration of Dasatinib can be decreased when it is combined with Phenytoin.
PimecrolimusThe risk or severity of adverse effects can be increased when Pimecrolimus is combined with Dasatinib.
PimozideThe serum concentration of Pimozide can be increased when it is combined with Dasatinib.
PipotiazineThe serum concentration of Pipotiazine can be increased when it is combined with Dasatinib.
PiroxicamDasatinib may increase the anticoagulant activities of Piroxicam.
PosaconazoleThe serum concentration of Dasatinib can be increased when it is combined with Posaconazole.
PrasugrelDasatinib may increase the anticoagulant activities of Prasugrel.
PraziquantelThe serum concentration of Praziquantel can be increased when it is combined with Dasatinib.
PrimidoneThe serum concentration of Dasatinib can be decreased when it is combined with Primidone.
PropacetamolDasatinib may increase the hepatotoxic activities of Propacetamol.
RabeprazoleThe serum concentration of Dasatinib can be decreased when it is combined with Rabeprazole.
RanitidineRanitidine can cause a decrease in the absorption of Dasatinib resulting in a reduced serum concentration and potentially a decrease in efficacy.
RanolazineThe serum concentration of Ranolazine can be increased when it is combined with Dasatinib.
RegorafenibThe serum concentration of Regorafenib can be increased when it is combined with Dasatinib.
RifabutinThe serum concentration of Dasatinib can be decreased when it is combined with Rifabutin.
RifampicinThe serum concentration of Dasatinib can be decreased when it is combined with Rifampicin.
RifapentineThe serum concentration of Dasatinib can be decreased when it is combined with Rifapentine.
RitonavirThe serum concentration of Dasatinib can be increased when it is combined with Ritonavir.
RivaroxabanDasatinib may increase the anticoagulant activities of Rivaroxaban.
RoflumilastRoflumilast may increase the immunosuppressive activities of Dasatinib.
RuxolitinibThe serum concentration of Ruxolitinib can be increased when it is combined with Dasatinib.
SalmeterolThe serum concentration of Salmeterol can be increased when it is combined with Dasatinib.
SaquinavirThe serum concentration of Dasatinib can be increased when it is combined with Saquinavir.
SaxagliptinThe serum concentration of Saxagliptin can be increased when it is combined with Dasatinib.
SertralineDasatinib may increase the anticoagulant activities of Sertraline.
SildenafilThe serum concentration of Sildenafil can be increased when it is combined with Dasatinib.
SilodosinThe serum concentration of Silodosin can be increased when it is combined with Dasatinib.
SiltuximabThe serum concentration of Dasatinib can be decreased when it is combined with Siltuximab.
SimeprevirThe serum concentration of Dasatinib can be increased when it is combined with Simeprevir.
SimvastatinThe serum concentration of Simvastatin can be increased when it is combined with Dasatinib.
Sipuleucel-TThe therapeutic efficacy of Sipuleucel-T can be decreased when used in combination with Dasatinib.
SirolimusThe serum concentration of Sirolimus can be increased when it is combined with Dasatinib.
Sodium bicarbonateSodium bicarbonate can cause a decrease in the absorption of Dasatinib resulting in a reduced serum concentration and potentially a decrease in efficacy.
SolifenacinThe serum concentration of Solifenacin can be increased when it is combined with Dasatinib.
SonidegibThe serum concentration of Sonidegib can be increased when it is combined with Dasatinib.
SpiramycinThe serum concentration of Spiramycin can be increased when it is combined with Dasatinib.
St. John's WortThe serum concentration of Dasatinib can be decreased when it is combined with St. John's Wort.
StiripentolThe serum concentration of Dasatinib can be increased when it is combined with Stiripentol.
SufentanilThe serum concentration of Sufentanil can be increased when it is combined with Dasatinib.
SulindacDasatinib may increase the anticoagulant activities of Sulindac.
SulodexideDasatinib may increase the anticoagulant activities of Sulodexide.
SunitinibThe serum concentration of Sunitinib can be increased when it is combined with Dasatinib.
SuvorexantThe serum concentration of Suvorexant can be increased when it is combined with Dasatinib.
TacrolimusThe serum concentration of Tacrolimus can be increased when it is combined with Dasatinib.
TadalafilThe serum concentration of Tadalafil can be increased when it is combined with Dasatinib.
TamoxifenThe serum concentration of Tamoxifen can be increased when it is combined with Dasatinib.
TamsulosinThe serum concentration of Tamsulosin can be increased when it is combined with Dasatinib.
TelaprevirThe serum concentration of Dasatinib can be increased when it is combined with Telaprevir.
TelithromycinThe serum concentration of Dasatinib can be increased when it is combined with Telithromycin.
TemsirolimusThe serum concentration of Temsirolimus can be increased when it is combined with Dasatinib.
TeniposideThe serum concentration of Teniposide can be increased when it is combined with Dasatinib.
TheophyllineThe serum concentration of Theophylline can be increased when it is combined with Dasatinib.
TiagabineThe serum concentration of Tiagabine can be increased when it is combined with Dasatinib.
Tiaprofenic acidDasatinib may increase the anticoagulant activities of Tiaprofenic acid.
TicagrelorDasatinib may increase the anticoagulant activities of Ticagrelor.
TiclopidineDasatinib may increase the anticoagulant activities of Ticlopidine.
TinzaparinDasatinib may increase the anticoagulant activities of Tinzaparin.
TirofibanDasatinib may increase the anticoagulant activities of Tirofiban.
TocilizumabThe serum concentration of Dasatinib can be decreased when it is combined with Tocilizumab.
TofacitinibDasatinib may increase the immunosuppressive activities of Tofacitinib.
TolmetinDasatinib may increase the anticoagulant activities of Tolmetin.
TolterodineThe serum concentration of Tolterodine can be increased when it is combined with Dasatinib.
TolvaptanThe serum concentration of Tolvaptan can be increased when it is combined with Dasatinib.
TrabectedinThe serum concentration of Trabectedin can be increased when it is combined with Dasatinib.
TrastuzumabTrastuzumab may increase the neutropenic activities of Dasatinib.
TrazodoneThe serum concentration of Trazodone can be increased when it is combined with Dasatinib.
TreprostinilDasatinib may increase the anticoagulant activities of Treprostinil.
TriazolamThe serum concentration of Triazolam can be increased when it is combined with Dasatinib.
TrimipramineThe serum concentration of Trimipramine can be increased when it is combined with Dasatinib.
VardenafilThe serum concentration of Vardenafil can be increased when it is combined with Dasatinib.
VenlafaxineDasatinib may increase the anticoagulant activities of Venlafaxine.
VerapamilThe serum concentration of Verapamil can be increased when it is combined with Dasatinib.
VilazodoneDasatinib may increase the anticoagulant activities of Vilazodone.
VinblastineThe serum concentration of Vinblastine can be increased when it is combined with Dasatinib.
VincristineThe serum concentration of Vincristine can be increased when it is combined with Dasatinib.
VinorelbineThe serum concentration of Vinorelbine can be increased when it is combined with Dasatinib.
VorapaxarDasatinib may increase the anticoagulant activities of Vorapaxar.
VoriconazoleVoriconazole may increase the QTc-prolonging activities of Dasatinib.
VortioxetineDasatinib may increase the anticoagulant activities of Vortioxetine.
WarfarinDasatinib may increase the anticoagulant activities of Warfarin.
ZolpidemThe serum concentration of Zolpidem can be increased when it is combined with Dasatinib.
ZonisamideThe serum concentration of Zonisamide can be increased when it is combined with Dasatinib.
ZopicloneThe serum concentration of Zopiclone can be increased when it is combined with Dasatinib.
Food InteractionsNot Available

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
multitarget
General Function:
Syntaxin binding
Specific Function:
Non-receptor tyrosine-protein kinase that plays a role in many key processes linked to cell growth and survival such as cytoskeleton remodeling in response to extracellular stimuli, cell motility and adhesion, receptor endocytosis, autophagy, DNA damage response and apoptosis. Coordinates actin remodeling through tyrosine phosphorylation of proteins controlling cytoskeleton dynamics like WASF3 ...
Gene Name:
ABL1
Uniprot ID:
P00519
Molecular Weight:
122871.435 Da
References
  1. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed:17016423 ]
  2. Piccaluga PP, Paolini S, Martinelli G: Tyrosine kinase inhibitors for the treatment of Philadelphia chromosome-positive adult acute lymphoblastic leukemia. Cancer. 2007 Sep 15;110(6):1178-86. [PubMed:17701954 ]
  3. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
multitarget
General Function:
Sh3/sh2 adaptor activity
Specific Function:
Non-receptor protein tyrosine kinase which is activated following engagement of many different classes of cellular receptors including immune response receptors, integrins and other adhesion receptors, receptor protein tyrosine kinases, G protein-coupled receptors as well as cytokine receptors. Participates in signaling pathways that control a diverse spectrum of biological activities including...
Gene Name:
SRC
Uniprot ID:
P12931
Molecular Weight:
59834.295 Da
References
  1. Kamath AV, Wang J, Lee FY, Marathe PH: Preclinical pharmacokinetics and in vitro metabolism of dasatinib (BMS-354825): a potent oral multi-targeted kinase inhibitor against SRC and BCR-ABL. Cancer Chemother Pharmacol. 2008 Mar;61(3):365-76. Epub 2007 Apr 11. [PubMed:17429625 ]
  2. Serrels A, Macpherson IR, Evans TR, Lee FY, Clark EA, Sansom OJ, Ashton GH, Frame MC, Brunton VG: Identification of potential biomarkers for measuring inhibition of Src kinase activity in colon cancer cells following treatment with dasatinib. Mol Cancer Ther. 2006 Dec;5(12):3014-22. Epub 2006 Dec 5. [PubMed:17148760 ]
  3. Quintas-Cardama A, Kantarjian H, Cortes J: Targeting ABL and SRC kinases in chronic myeloid leukemia: experience with dasatinib. Future Oncol. 2006 Dec;2(6):655-65. [PubMed:17155893 ]
  4. Schittenhelm MM, Shiraga S, Schroeder A, Corbin AS, Griffith D, Lee FY, Bokemeyer C, Deininger MW, Druker BJ, Heinrich MC: Dasatinib (BMS-354825), a dual SRC/ABL kinase inhibitor, inhibits the kinase activity of wild-type, juxtamembrane, and activation loop mutant KIT isoforms associated with human malignancies. Cancer Res. 2006 Jan 1;66(1):473-81. [PubMed:16397263 ]
  5. Nam S, Kim D, Cheng JQ, Zhang S, Lee JH, Buettner R, Mirosevich J, Lee FY, Jove R: Action of the Src family kinase inhibitor, dasatinib (BMS-354825), on human prostate cancer cells. Cancer Res. 2005 Oct 15;65(20):9185-9. [PubMed:16230377 ]
  6. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
antagonist
General Function:
Transmembrane receptor protein tyrosine kinase activity
Specific Function:
Receptor tyrosine kinase which binds promiscuously membrane-bound ephrin-A family ligands residing on adjacent cells, leading to contact-dependent bidirectional signaling into neighboring cells. The signaling pathway downstream of the receptor is referred to as forward signaling while the signaling pathway downstream of the ephrin ligand is referred to as reverse signaling. Activated by the lig...
Gene Name:
EPHA2
Uniprot ID:
P29317
Molecular Weight:
108265.585 Da
References
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284 ]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed:17016423 ]
  3. Lindauer M, Hochhaus A: Dasatinib. Recent Results Cancer Res. 2010;184:83-102. doi: 10.1007/978-3-642-01222-8_7. [PubMed:20072833 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
multitarget
General Function:
Sh2 domain binding
Specific Function:
Non-receptor tyrosine-protein kinase that plays an essential role in the selection and maturation of developing T-cells in the thymus and in the function of mature T-cells. Plays a key role in T-cell antigen receptor (TCR)-linked signal transduction pathways. Constitutively associated with the cytoplasmic portions of the CD4 and CD8 surface receptors. Association of the TCR with a peptide antig...
Gene Name:
LCK
Uniprot ID:
P06239
Molecular Weight:
58000.15 Da
References
  1. Das J, Chen P, Norris D, Padmanabha R, Lin J, Moquin RV, Shen Z, Cook LS, Doweyko AM, Pitt S, Pang S, Shen DR, Fang Q, de Fex HF, McIntyre KW, Shuster DJ, Gillooly KM, Behnia K, Schieven GL, Wityak J, Barrish JC: 2-aminothiazole as a novel kinase inhibitor template. Structure-activity relationship studies toward the discovery of N-(2-chloro-6-methylphenyl)-2-[[6-[4-(2-hydroxyethyl)-1- piperazinyl)]-2-methyl-4-pyrimidinyl]amino)]-1,3-thiazole-5-carboxamide (dasatinib, BMS-354825) as a potent pan-Src kinase inhibitor. J Med Chem. 2006 Nov 16;49(23):6819-32. [PubMed:17154512 ]
  2. Lindauer M, Hochhaus A: Dasatinib. Recent Results Cancer Res. 2010;184:83-102. doi: 10.1007/978-3-642-01222-8_7. [PubMed:20072833 ]
  3. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
inhibitor
General Function:
Receptor binding
Specific Function:
Non-receptor protein tyrosine kinase that is involved in the regulation of cell growth and survival, apoptosis, cell-cell adhesion, cytoskeleton remodeling, and differentiation. Stimulation by receptor tyrosine kinases (RTKs) including EGRF, PDGFR, CSF1R and FGFR leads to recruitment of YES1 to the phosphorylated receptor, and activation and phosphorylation of downstream substrates. Upon EGFR a...
Gene Name:
YES1
Uniprot ID:
P07947
Molecular Weight:
60800.78 Da
References
  1. Trevino JG, Summy JM, Lesslie DP, Parikh NU, Hong DS, Lee FY, Donato NJ, Abbruzzese JL, Baker CH, Gallick GE: Inhibition of SRC expression and activity inhibits tumor progression and metastasis of human pancreatic adenocarcinoma cells in an orthotopic nude mouse model. Am J Pathol. 2006 Mar;168(3):962-72. [PubMed:16507911 ]
  2. Margutti S, Laufer SA: Are MAP kinases drug targets? Yes, but difficult ones. ChemMedChem. 2007 Aug;2(8):1116-40. [PubMed:17541990 ]
  3. Lindauer M, Hochhaus A: Dasatinib. Recent Results Cancer Res. 2010;184:83-102. doi: 10.1007/978-3-642-01222-8_7. [PubMed:20072833 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
antagonist
General Function:
Transmembrane receptor protein tyrosine kinase activity
Specific Function:
Tyrosine-protein kinase that acts as cell-surface receptor for the cytokine KITLG/SCF and plays an essential role in the regulation of cell survival and proliferation, hematopoiesis, stem cell maintenance, gametogenesis, mast cell development, migration and function, and in melanogenesis. In response to KITLG/SCF binding, KIT can activate several signaling pathways. Phosphorylates PIK3R1, PLCG1...
Gene Name:
KIT
Uniprot ID:
P10721
Molecular Weight:
109863.655 Da
References
  1. Schittenhelm MM, Shiraga S, Schroeder A, Corbin AS, Griffith D, Lee FY, Bokemeyer C, Deininger MW, Druker BJ, Heinrich MC: Dasatinib (BMS-354825), a dual SRC/ABL kinase inhibitor, inhibits the kinase activity of wild-type, juxtamembrane, and activation loop mutant KIT isoforms associated with human malignancies. Cancer Res. 2006 Jan 1;66(1):473-81. [PubMed:16397263 ]
  2. Shah NP, Lee FY, Luo R, Jiang Y, Donker M, Akin C: Dasatinib (BMS-354825) inhibits KITD816V, an imatinib-resistant activating mutation that triggers neoplastic growth in most patients with systemic mastocytosis. Blood. 2006 Jul 1;108(1):286-91. Epub 2006 Jan 24. [PubMed:16434489 ]
  3. Dizdar O, Dede DS, Bulut N, Altundag K: Dasatinib may also inhibit c-Kit in triple negative breast cancer cell lines. Breast Cancer Res Treat. 2008 Jan;107(2):303. Epub 2007 Mar 10. [PubMed:17351742 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
antagonist
General Function:
Vascular endothelial growth factor binding
Specific Function:
Tyrosine-protein kinase that acts as cell-surface receptor for homodimeric PDGFB and PDGFD and for heterodimers formed by PDGFA and PDGFB, and plays an essential role in the regulation of embryonic development, cell proliferation, survival, differentiation, chemotaxis and migration. Plays an essential role in blood vessel development by promoting proliferation, migration and recruitment of peri...
Gene Name:
PDGFRB
Uniprot ID:
P09619
Molecular Weight:
123966.895 Da
References
  1. Zhang Z, Meier KE: New assignments for multitasking signal transduction inhibitors. Mol Pharmacol. 2006 May;69(5):1510-2. Epub 2006 Feb 23. [PubMed:16497876 ]
  2. Chen Z, Lee FY, Bhalla KN, Wu J: Potent inhibition of platelet-derived growth factor-induced responses in vascular smooth muscle cells by BMS-354825 (dasatinib). Mol Pharmacol. 2006 May;69(5):1527-33. Epub 2006 Jan 25. [PubMed:16436588 ]
  3. Lindauer M, Hochhaus A: Dasatinib. Recent Results Cancer Res. 2010;184:83-102. doi: 10.1007/978-3-642-01222-8_7. [PubMed:20072833 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Transcription factor activity, sequence-specific dna binding
Specific Function:
Carries out a dual function: signal transduction and activation of transcription. Mediates cellular responses to the cytokine KITLG/SCF and other growth factors. Binds to the GAS element and activates PRL-induced transcription.
Gene Name:
STAT5B
Uniprot ID:
P51692
Molecular Weight:
89865.35 Da
References
  1. Fiskus W, Pranpat M, Balasis M, Bali P, Estrella V, Kumaraswamy S, Rao R, Rocha K, Herger B, Lee F, Richon V, Bhalla K: Cotreatment with vorinostat (suberoylanilide hydroxamic acid) enhances activity of dasatinib (BMS-354825) against imatinib mesylate-sensitive or imatinib mesylate-resistant chronic myelogenous leukemia cells. Clin Cancer Res. 2006 Oct 1;12(19):5869-78. [PubMed:17020995 ]
  2. Nam S, Williams A, Vultur A, List A, Bhalla K, Smith D, Lee FY, Jove R: Dasatinib (BMS-354825) inhibits Stat5 signaling associated with apoptosis in chronic myelogenous leukemia cells. Mol Cancer Ther. 2007 Apr;6(4):1400-5. [PubMed:17431118 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
multitarget
General Function:
Receptor binding
Specific Function:
Non-receptor tyrosine-protein kinase that plays an ABL1-overlapping role in key processes linked to cell growth and survival such as cytoskeleton remodeling in response to extracellular stimuli, cell motility and adhesion and receptor endocytosis. Coordinates actin remodeling through tyrosine phosphorylation of proteins controlling cytoskeleton dynamics like MYH10 (involved in movement); CTTN (...
Gene Name:
ABL2
Uniprot ID:
P42684
Molecular Weight:
128341.935 Da
References
  1. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed:17016423 ]
  2. Lindauer M, Hochhaus A: Dasatinib. Recent Results Cancer Res. 2010;184:83-102. doi: 10.1007/978-3-642-01222-8_7. [PubMed:20072833 ]
  3. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
multitarget
General Function:
Protein tyrosine kinase activity
Specific Function:
Non-receptor tyrosine-protein kinase that plays a role in many biological processes including regulation of cell growth and survival, cell adhesion, integrin-mediated signaling, cytoskeletal remodeling, cell motility, immune response and axon guidance. Inactive FYN is phosphorylated on its C-terminal tail within the catalytic domain. Following activation by PKA, the protein subsequently associa...
Gene Name:
FYN
Uniprot ID:
P06241
Molecular Weight:
60761.49 Da
References
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284 ]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed:17016423 ]
  3. Lindauer M, Hochhaus A: Dasatinib. Recent Results Cancer Res. 2010;184:83-102. doi: 10.1007/978-3-642-01222-8_7. [PubMed:20072833 ]
  4. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Vitamin d3 25-hydroxylase activity
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation reactions (e.g. caffeine 8-oxidation, omeprazole sulphoxidation, midazolam 1'-hydroxylation and midazolam 4-hydroxylation) of structurally unrelated compounds, including steroids, fatty acids, and xenobiot...
Gene Name:
CYP3A4
Uniprot ID:
P08684
Molecular Weight:
57342.67 Da
References
  1. van Erp NP, Gelderblom H, Guchelaar HJ: Clinical pharmacokinetics of tyrosine kinase inhibitors. Cancer Treat Rev. 2009 Dec;35(8):692-706. doi: 10.1016/j.ctrv.2009.08.004. Epub 2009 Sep 5. [PubMed:19733976 ]
  2. Wang L, Christopher LJ, Cui D, Li W, Iyer R, Humphreys WG, Zhang D: Identification of the human enzymes involved in the oxidative metabolism of dasatinib: an effective approach for determining metabolite formation kinetics. Drug Metab Dispos. 2008 Sep;36(9):1828-39. doi: 10.1124/dmd.107.020255. Epub 2008 Jun 12. [PubMed:18556438 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Vitamin d 24-hydroxylase activity
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics.
Gene Name:
CYP1A1
Uniprot ID:
P04798
Molecular Weight:
58164.815 Da
References
  1. van Erp NP, Gelderblom H, Guchelaar HJ: Clinical pharmacokinetics of tyrosine kinase inhibitors. Cancer Treat Rev. 2009 Dec;35(8):692-706. doi: 10.1016/j.ctrv.2009.08.004. Epub 2009 Sep 5. [PubMed:19733976 ]
  2. Wang L, Christopher LJ, Cui D, Li W, Iyer R, Humphreys WG, Zhang D: Identification of the human enzymes involved in the oxidative metabolism of dasatinib: an effective approach for determining metabolite formation kinetics. Drug Metab Dispos. 2008 Sep;36(9):1828-39. doi: 10.1124/dmd.107.020255. Epub 2008 Jun 12. [PubMed:18556438 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygen
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics. Most active in catalyzing 2-hydroxylation. Caffeine is metabolized primarily by cytochrome CYP1A2 in the liver through an initial N...
Gene Name:
CYP1A2
Uniprot ID:
P05177
Molecular Weight:
58293.76 Da
References
  1. van Erp NP, Gelderblom H, Guchelaar HJ: Clinical pharmacokinetics of tyrosine kinase inhibitors. Cancer Treat Rev. 2009 Dec;35(8):692-706. doi: 10.1016/j.ctrv.2009.08.004. Epub 2009 Sep 5. [PubMed:19733976 ]
  2. Wang L, Christopher LJ, Cui D, Li W, Iyer R, Humphreys WG, Zhang D: Identification of the human enzymes involved in the oxidative metabolism of dasatinib: an effective approach for determining metabolite formation kinetics. Drug Metab Dispos. 2008 Sep;36(9):1828-39. doi: 10.1124/dmd.107.020255. Epub 2008 Jun 12. [PubMed:18556438 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Oxygen binding
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, retinoid and xenobiotics. Preferentially oxidizes 17beta-estradiol to the carcinogenic 4-hydroxy derivative, and a variety of procarcinogenic compou...
Gene Name:
CYP1B1
Uniprot ID:
Q16678
Molecular Weight:
60845.33 Da
References
  1. van Erp NP, Gelderblom H, Guchelaar HJ: Clinical pharmacokinetics of tyrosine kinase inhibitors. Cancer Treat Rev. 2009 Dec;35(8):692-706. doi: 10.1016/j.ctrv.2009.08.004. Epub 2009 Sep 5. [PubMed:19733976 ]
  2. Wang L, Christopher LJ, Cui D, Li W, Iyer R, Humphreys WG, Zhang D: Identification of the human enzymes involved in the oxidative metabolism of dasatinib: an effective approach for determining metabolite formation kinetics. Drug Metab Dispos. 2008 Sep;36(9):1828-39. doi: 10.1124/dmd.107.020255. Epub 2008 Jun 12. [PubMed:18556438 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Oxygen binding
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics.
Gene Name:
CYP3A5
Uniprot ID:
P20815
Molecular Weight:
57108.065 Da
References
  1. van Erp NP, Gelderblom H, Guchelaar HJ: Clinical pharmacokinetics of tyrosine kinase inhibitors. Cancer Treat Rev. 2009 Dec;35(8):692-706. doi: 10.1016/j.ctrv.2009.08.004. Epub 2009 Sep 5. [PubMed:19733976 ]
  2. Wang L, Christopher LJ, Cui D, Li W, Iyer R, Humphreys WG, Zhang D: Identification of the human enzymes involved in the oxidative metabolism of dasatinib: an effective approach for determining metabolite formation kinetics. Drug Metab Dispos. 2008 Sep;36(9):1828-39. doi: 10.1124/dmd.107.020255. Epub 2008 Jun 12. [PubMed:18556438 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Trimethylamine monooxygenase activity
Specific Function:
Involved in the oxidative metabolism of a variety of xenobiotics such as drugs and pesticides. It N-oxygenates primary aliphatic alkylamines as well as secondary and tertiary amines. Plays an important role in the metabolism of trimethylamine (TMA), via the production of TMA N-oxide (TMAO). Is also able to perform S-oxidation when acting on sulfide compounds (PubMed:9224773).
Gene Name:
FMO3
Uniprot ID:
P31513
Molecular Weight:
60032.975 Da
References
  1. Wang L, Christopher LJ, Cui D, Li W, Iyer R, Humphreys WG, Zhang D: Identification of the human enzymes involved in the oxidative metabolism of dasatinib: an effective approach for determining metabolite formation kinetics. Drug Metab Dispos. 2008 Sep;36(9):1828-39. doi: 10.1124/dmd.107.020255. Epub 2008 Jun 12. [PubMed:18556438 ]

Transporters

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrateinhibitor
General Function:
Xenobiotic-transporting atpase activity
Specific Function:
Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells.
Gene Name:
ABCB1
Uniprot ID:
P08183
Molecular Weight:
141477.255 Da
References
  1. Dohse M, Scharenberg C, Shukla S, Robey RW, Volkmann T, Deeken JF, Brendel C, Ambudkar SV, Neubauer A, Bates SE: Comparison of ATP-binding cassette transporter interactions with the tyrosine kinase inhibitors imatinib, nilotinib, and dasatinib. Drug Metab Dispos. 2010 Aug;38(8):1371-80. doi: 10.1124/dmd.109.031302. Epub 2010 Apr 27. [PubMed:20423956 ]
  2. Hegedus C, Ozvegy-Laczka C, Apati A, Magocsi M, Nemet K, Orfi L, Keri G, Katona M, Takats Z, Varadi A, Szakacs G, Sarkadi B: Interaction of nilotinib, dasatinib and bosutinib with ABCB1 and ABCG2: implications for altered anti-cancer effects and pharmacological properties. Br J Pharmacol. 2009 Oct;158(4):1153-64. doi: 10.1111/j.1476-5381.2009.00383.x. Epub 2009 Sep 28. [PubMed:19785662 ]
  3. Giannoudis A, Davies A, Lucas CM, Harris RJ, Pirmohamed M, Clark RE: Effective dasatinib uptake may occur without human organic cation transporter 1 (hOCT1): implications for the treatment of imatinib-resistant chronic myeloid leukemia. Blood. 2008 Oct 15;112(8):3348-54. doi: 10.1182/blood-2007-10-116236. Epub 2008 Jul 31. [PubMed:18669873 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrateinhibitor
General Function:
Xenobiotic-transporting atpase activity
Specific Function:
High-capacity urate exporter functioning in both renal and extrarenal urate excretion. Plays a role in porphyrin homeostasis as it is able to mediates the export of protoporhyrin IX (PPIX) both from mitochondria to cytosol and from cytosol to extracellular space, and cellular export of hemin, and heme. Xenobiotic transporter that may play an important role in the exclusion of xenobiotics from t...
Gene Name:
ABCG2
Uniprot ID:
Q9UNQ0
Molecular Weight:
72313.47 Da
References
  1. Dohse M, Scharenberg C, Shukla S, Robey RW, Volkmann T, Deeken JF, Brendel C, Ambudkar SV, Neubauer A, Bates SE: Comparison of ATP-binding cassette transporter interactions with the tyrosine kinase inhibitors imatinib, nilotinib, and dasatinib. Drug Metab Dispos. 2010 Aug;38(8):1371-80. doi: 10.1124/dmd.109.031302. Epub 2010 Apr 27. [PubMed:20423956 ]
  2. Hegedus C, Ozvegy-Laczka C, Apati A, Magocsi M, Nemet K, Orfi L, Keri G, Katona M, Takats Z, Varadi A, Szakacs G, Sarkadi B: Interaction of nilotinib, dasatinib and bosutinib with ABCB1 and ABCG2: implications for altered anti-cancer effects and pharmacological properties. Br J Pharmacol. 2009 Oct;158(4):1153-64. doi: 10.1111/j.1476-5381.2009.00383.x. Epub 2009 Sep 28. [PubMed:19785662 ]
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Drug created on May 08, 2007 18:32 / Updated on May 02, 2016 02:27