Capmatinib 2HCl.H2O 是一种具有潜在抗肿瘤活性的原癌基因 c-Met (HGFR) 的口服生物可利用抑制剂。

Capmatinib 2HCl.H2O is an orally bioavailable inhibitor of the proto-oncogene c-Met (HGFR)with potential antineoplastic activity.

Capmatinib was found to be highly selective for MET over other kinases.?It was active against cancer models that are characterized by MET amplification, marked MET overexpression, MET exon 14 skipping mutations, or MET activation via expression of the ligand hepatocyte growth factor (HGF)[1].

In cancer models where MET is the dominant oncogenic driver, anticancer activity could be further enhanced by combination treatments, for example, by the addition of apoptosis-inducing BH3 mimetics.?The combinations of capmatinib and other kinase inhibitors resulted in enhanced anticancer activity against models where MET activation co-occurred with other oncogenic drivers, for example EGFR activating mutations[1].

1865733-40-9

C23H21Cl2FN6O2

503.36

INC-280 2HCl.H2O;NVP-INC280 2HCl.H2O;INCB28060 2HCl.H2O

DMSO:10 mM
Powder: -20°C for 3 years
In solvent: -80°C for 2 years