KW-2450
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This drug entry is a stub and has not been fully annotated. It is scheduled to be annotated soon.
Identification
- Generic Name
- KW-2450 free base
Commonly known or available as KW-2450 - DrugBank Accession Number
- DB16637
- Background
Not Available
- Type
- Small Molecule
- Groups
- Experimental
- Structure
- Weight
- Average: 515.63
Monoisotopic: 515.199110988 - Chemical Formula
- C28H29N5O3S
- Synonyms
- Not Available
- External IDs
- KW-2450 free base
Pharmacology
- Indication
Not Available
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- Pharmacodynamics
Not Available
- Mechanism of action
Target Actions Organism UInsulin receptor inhibitorHumans UInsulin-like growth factor 1 receptor inhibitorHumans - 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
- Adverse Effects
- Improve decision support & research outcomesWith structured adverse effects data, including: blackbox warnings, adverse reactions, warning & precautions, & incidence rates. View sample adverse effects data in our new Data Library!Improve decision support & research outcomes with our structured adverse effects data.
- Toxicity
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
Products
- Drug product information from 10+ global regionsOur datasets provide approved product information including:dosage, form, labeller, route of administration, and marketing period.Access drug product information from over 10 global regions.
- Product Ingredients
Ingredient UNII CAS InChI Key KW-2450 2TRH1EX32K 1360433-93-7 SIJKXSMUXNJNQM-HRNDJLQDSA-N
Categories
- Drug Categories
- Classification
- Not classified
- Affected organisms
- Not Available
Chemical Identifiers
- UNII
- RS6V91I0HT
- CAS number
- 904899-25-8
- InChI Key
- HHCSNTXVZDWIGT-CMDGGOBGSA-N
- InChI
- InChI=1S/C28H29N5O3S/c1-19-10-15-37-27(19)28(36)29-25-16-20(17-32-11-13-33(14-12-32)26(35)18-34)6-7-21(25)8-9-24-22-4-2-3-5-23(22)30-31-24/h2-10,15-16,34H,11-14,17-18H2,1H3,(H,29,36)(H,30,31)/b9-8+
- IUPAC Name
- N-(5-{[4-(2-hydroxyacetyl)piperazin-1-yl]methyl}-2-[(1E)-2-(1H-indazol-3-yl)ethenyl]phenyl)-3-methylthiophene-2-carboxamide
- SMILES
- CC1=C(SC=C1)C(=O)NC1=CC(CN2CCN(CC2)C(=O)CO)=CC=C1\C=C\C1=NNC2=CC=CC=C12
References
- General References
- Not Available
- External Links
- ChemSpider
- 64853777
Clinical Trials
- Clinical Trials
Phase Status Purpose Conditions Count 1 Completed Treatment Solid Tumors 1 1 Terminated Treatment Breast Cancer 1
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage Forms
- Not Available
- Prices
- Not Available
- Patents
- Not Available
Properties
- State
- Not Available
- Experimental Properties
- Not Available
- Predicted Properties
Property Value Source logP 3.59 Chemaxon pKa (Strongest Acidic) 13.42 Chemaxon pKa (Strongest Basic) 6.25 Chemaxon Physiological Charge 0 Chemaxon Hydrogen Acceptor Count 5 Chemaxon Hydrogen Donor Count 3 Chemaxon Polar Surface Area 101.56 Å2 Chemaxon Rotatable Bond Count 7 Chemaxon Refractivity 149.11 m3·mol-1 Chemaxon Polarizability 57.17 Å3 Chemaxon Number of Rings 5 Chemaxon Bioavailability 1 Chemaxon Rule of Five No Chemaxon Ghose Filter No Chemaxon Veber's Rule No Chemaxon MDDR-like Rule Yes Chemaxon - Predicted ADMET Features
- Not Available
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
- Chromatographic Properties
Collision Cross Sections (CCS)
Not Available
Targets
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1. DetailsInsulin receptor
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- Receptor signaling protein tyrosine kinase activity
- Specific Function
- Receptor tyrosine kinase which mediates the pleiotropic actions of insulin. Binding of insulin leads to phosphorylation of several intracellular substrates, including, insulin receptor substrates (...
- Gene Name
- INSR
- Uniprot ID
- P06213
- Uniprot Name
- Insulin receptor
- Molecular Weight
- 156331.465 Da
References
- Umehara H, Maekawa Y, Koizumi F, Shimizu M, Ota T, Fouad TM, Willey J, Kaito H, Shiraishi N, Nakashima D, Akinaga S, Ueno NT: Preclinical and phase I clinical studies of KW-2450, a dual IGF-1R/IR tyrosine kinase inhibitor, in combination with lapatinib and letrozole. Ther Adv Med Oncol. 2018 Jul 30;10:1758835918786858. doi: 10.1177/1758835918786858. eCollection 2018. [Article]
2. DetailsInsulin-like growth factor 1 receptor
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- Protein tyrosine kinase activity
- Specific Function
- Receptor tyrosine kinase which mediates actions of insulin-like growth factor 1 (IGF1). Binds IGF1 with high affinity and IGF2 and insulin (INS) with a lower affinity. The activated IGF1R is involv...
- Gene Name
- IGF1R
- Uniprot ID
- P08069
- Uniprot Name
- Insulin-like growth factor 1 receptor
- Molecular Weight
- 154791.73 Da
References
- Umehara H, Maekawa Y, Koizumi F, Shimizu M, Ota T, Fouad TM, Willey J, Kaito H, Shiraishi N, Nakashima D, Akinaga S, Ueno NT: Preclinical and phase I clinical studies of KW-2450, a dual IGF-1R/IR tyrosine kinase inhibitor, in combination with lapatinib and letrozole. Ther Adv Med Oncol. 2018 Jul 30;10:1758835918786858. doi: 10.1177/1758835918786858. eCollection 2018. [Article]
Drug created at March 11, 2021 17:34 / Updated at March 13, 2021 17:03