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Product Description
– Capmatinib (INC280; INCB28060) dihydrochloride is a potent, orally active, selective, and ATP competitive c-Met kinase inhibitor (IC50=0.13 nM). Capmatinib dihydrochloride can inhibit phosphorylation of c-MET as well as c-MET pathway downstream effectors such as ERK1/2, AKT, FAK, GAB1, and STAT3/5. Capmatinib dihydrochloride potently inhibits c-MET-dependent tumor cell proliferation and migration and effectively induces apoptosis. Antitumor activity. Capmatinib dihydrochloride is largely metabolized by CYP3A4 and aldehyde oxidase[1][2][3].
Web ID
– HY-13404A
Shipping
– Room temperature
Applications
– Cancer-Kinase/protease
Molecular Formula
– C23H19Cl2FN6O
References
– [1]Liu X, et al. A novel kinase inhibitor, INCB28060, blocks c-MET-dependent signaling, neoplastic activities, and cross-talk with EGFR and HER-3. Clin Cancer Res. 2011 Nov 15;17(22):7127-38.|[2]Baltschukat S, et al. Capmatinib (INC280) Is Active Against Models of Non-Small Cell Lung Cancer and Other Cancer Types with Defined Mechanisms of MET Activation. Clin Cancer Res. 2019 May 15;25(10):3164-3175.|[3]Dhillon S. Capmatinib: First Approval. Drugs. 2020 Jul;80(11):1125-1131.
CAS Number
– 1197376-85-4
Molecular Weight
– 485.34
SMILES
– O=C(NC)C1=CC=C(C2=NN3C(N=C2)=NC=C3CC4=CC=C5N=CC=CC5=C4)C=C1F.Cl.Cl
Clinical Information
– Launched
Research Area
– Cancer
Solubility
– 10 mM in DMSO
Target
– Apoptosis;c-Met/HGFR
Pathway
– Apoptosis;Protein Tyrosine Kinase/RTK
Product type
– Reference compound
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