Capmatinib hydrochloride CAS NO.1865733-40-9

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CAS号:1865733-40-9

英文名:Capmatinibhydrochloride

英文别名: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][1,2,4]triazin-2-yl)benzamidedihydrochloridemonohydrate

中文名:盐酸卡玛替尼一水合物中文别名:盐酸卡玛替尼;盐酸卡玛替尼一水合物;盐酸卡马替尼一水合物;

化合物CAPMATINIB2HCL.H2O

CBNumber:CB04848242

分子式:C23H20ClFN6O2

分子量: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.