Capmatinib (dihydrochloride hydrate)

Capmatinib (INC280; INCB28060) dihydrochloride hydrate is a potent, orally active, selective, and ATP competitive c-Met kinase inhibitor (IC50=0.13 nM) . Capmatinib dihydrochloride hydrate 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 hydrate potently inhibits c-MET-dependent tumor cell proliferation and migration and effectively induces apoptosis. Antitumor activity. Capmatinib dihydrochloride hydrate is largely metabolized by CYP3A4 and aldehyde oxidase[1][2][3].

Product Specifications

CAS Number

[1865733-40-9]

Product Name Alternative

INC280 (dihydrochloride hydrate) ; INCB-28060 (dihydrochloride hydrate)

UNSPSC

12352005

Target

Apoptosis; c-Met/HGFR

Type

Reference compound

Related Pathways

Apoptosis; Protein Tyrosine Kinase/RTK

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/capmatinib-dihydrochloride-hydrate.html

Purity

99.78

Solubility

DMSO : 20.83 mg/mL (ultrasonic; warming; heat to 60°C) |H2O : 3.33 mg/mL (ultrasonic)

Smiles

O=C(NC)C1=CC=C(C2=NN3C(N=C2)=NC=C3CC4=CC=C5N=CC=CC5=C4)C=C1F.O.Cl.Cl

Molecular Formula

C23H21Cl2FN6O2

Molecular Weight

503.36

References & Citations

[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.