Capmatinib hydrochloride

Details:

CAS number :1865733-40-9

English name :Capmatinibhydrochloride

English alias :INC-2802HCl.H2O; INCB280602HCl.H2O; NVP-INC2802HCl.H2O; Capmatinib2HCl.H2O; Capmatinibhydrochloride; CapmatinibhydrochlorideHydrate; CapmatinibHClhydrate(INCB-28060; Capmatinibdihydrochloridehydrate; CapmatinibHydrChemicalbookochlorideHydrate (INCB28060); 2 - fluoro - N - methyl - 4-7 - (quinolin - 6 - ylmethyl) imidazo [1, 2 - b] [1, 4-trichlorobenzene] triazin - 2 - yl) benzamidedihydrochloridemonohydrate

The compound CAPMATINIB2HCL.H2O

CBNumber:CB04848242

Molecular formula :C23H20ClFN6O2

Molecular weight :466.9

In Vitro: INCB28060 inhibits c-MET phosphorylation with an IC₅₀ value of approximately 1 nM and a concentration of approximately 4 nM inhibits c-MET more than 90%, which is reversible and the effect is significantly reduced in several hours after the compound is removed and completely disappeared by 48 hours.
INCB28060 (0-10000 nM; 72 h) inhibits the proliferation of SNU-5, S114, H441 and U-87MG.
INCB28060 (0.06-62.25 nM; 2h) effectively inhibits phosphorylation of c-MET as well as c-MET pathway downstream effectors such as ERK1/2, AKT, FAK, GAB1, and STAT3/5.
INCB28060 (0.24-63 nM; Over night) prevents HGF-stimulated H441 cell migration.
INCB28060 (0.5-50 nM; 20 min) suppresses phosphorylation of both EGFR and HER-3 rapidly.

In Vivo: INCB28060 (1-30 mg/kg; PO, twice daily, for 2 weeks) exhibits dose-dependent inhibition of tumor growth, and shows well tolerance at all doses during the treatment periods, with no evidence of overt toxicity or weight loss in U-87MG tumor mice model.
INCB28060 (0.03-10 mg/kg; PO, single dosage) causes inhibition of c-MET phosphorylation in S114 tumor mice model.