This drug entry is a stub and has not been fully annotated. It is scheduled to be annotated soon.

Identification

Name
RAF-265
Accession Number
DB05984
Type
Small Molecule
Groups
Investigational
Description
Not Available
Structure
Thumb
Synonyms
Not Available
External IDs
CHIR-265 / NVP-RAF265 / RAF265
Categories
Not Available
UNII
8O434L3768
CAS number
927880-90-8
Weight
Average: 518.423
Monoisotopic: 518.128978137
Chemical Formula
C24H16F6N6O
InChI Key
YABJJWZLRMPFSI-UHFFFAOYSA-N
InChI
InChI=1S/C24H16F6N6O/c1-36-19-7-6-15(10-17(19)34-22(36)33-14-4-2-13(3-5-14)23(25,26)27)37-16-8-9-31-18(11-16)21-32-12-20(35-21)24(28,29)30/h2-12H,1H3,(H,32,35)(H,33,34)
IUPAC Name
1-methyl-5-({2-[5-(trifluoromethyl)-1H-imidazol-2-yl]pyridin-4-yl}oxy)-N-[4-(trifluoromethyl)phenyl]-1H-1,3-benzodiazol-2-amine
SMILES
CN1C(NC2=CC=C(C=C2)C(F)(F)F)=NC2=CC(OC3=CC=NC(=C3)C3=NC=C(N3)C(F)(F)F)=CC=C12

Pharmacology

Indication

Investigated for use/treatment in melanoma.

Pharmacodynamics
Not Available
Mechanism of action

CHIR-265 binds and inhibits Raf kinases, which may result in a reduction of tumor cell growth and proliferation, and tumor cell death. In addition, this agent inhibits vascular endothelial growth factor receptor type 2 (VEGFR-2), thereby disrupting tumor angiogenesis. Raf kinases are critical enzymes in the Ras/Raf/MEK/ERK signaling pathway and are frequently upregulated in neoplasms.

TargetActionsOrganism
UVascular endothelial growth factor receptor 2Not AvailableHumans
USerine/threonine-protein kinase B-rafNot AvailableHumans
Absorption
Not Available
Volume of distribution
Not Available
Protein binding
Not Available
Metabolism
Not Available
Route of elimination
Not Available
Half life
Not Available
Clearance
Not Available
Toxicity
Not Available
Affected organisms
Not Available
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
Not Available
Food Interactions
Not Available

References

General References
Not Available
External Links
ChemSpider
9831256
BindingDB
31088
ChEBI
91451
ChEMBL
CHEMBL558752
ZINC
ZINC000018710085
PDBe Ligand
55J
PDB Entries
5ct7

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
1CompletedTreatmentAdvanced Solid Tumors1
2CompletedTreatmentMetastatic Melanoma1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage forms
Not Available
Prices
Not Available
Patents
Not Available

Properties

State
Solid
Experimental Properties
Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.00285 mg/mLALOGPS
logP5.8ALOGPS
logP5.86ChemAxon
logS-5.3ALOGPS
pKa (Strongest Acidic)9.28ChemAxon
pKa (Strongest Basic)7.21ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count4ChemAxon
Hydrogen Donor Count2ChemAxon
Polar Surface Area80.65 Å2ChemAxon
Rotatable Bond Count7ChemAxon
Refractivity131.42 m3·mol-1ChemAxon
Polarizability46.52 Å3ChemAxon
Number of Rings5ChemAxon
Bioavailability0ChemAxon
Rule of FiveNoChemAxon
Ghose FilterNoChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleYesChemAxon
Predicted ADMET features
Not Available

Spectra

Mass Spec (NIST)
Not Available
Spectra
Not Available

Taxonomy

Classification
Not classified

Targets

Kind
Protein
Organism
Humans
Pharmacological action
Unknown
General Function
Vascular endothelial growth factor-activated receptor activity
Specific Function
Tyrosine-protein kinase that acts as a cell-surface receptor for VEGFA, VEGFC and VEGFD. Plays an essential role in the regulation of angiogenesis, vascular development, vascular permeability, and ...
Gene Name
KDR
Uniprot ID
P35968
Uniprot Name
Vascular endothelial growth factor receptor 2
Molecular Weight
151525.555 Da
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
General Function
Protein serine/threonine kinase activity
Specific Function
Protein kinase involved in the transduction of mitogenic signals from the cell membrane to the nucleus. May play a role in the postsynaptic responses of hippocampal neuron. Phosphorylates MAP2K1, a...
Gene Name
BRAF
Uniprot ID
P15056
Uniprot Name
Serine/threonine-protein kinase B-raf
Molecular Weight
84436.135 Da

Drug created on November 18, 2007 11:29 / Updated on June 12, 2020 10:52

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