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Capmatinib dihydrochloride

CAS No. : 1197376-85-4

MCE 站：Capmatinib dihydrochloride

产品活性：Capmatinib (INC280; INCB28060) dihydrochloride 是一种有效的、口服活性的、选择性的、ATP 竞争性的 c-Met 激酶抑制剂 (IC₅₀=0.13 nM)。Capmatinib dihydrochloride 可抑制 c-MET 的磷酸化，以及 c-MET 通路下游效应蛋白如 ERK1/2、AKT、FAK、GAB1 和 STAT3/5。Capmatinib dihydrochloride 有效抑制 c-Met 依赖性肿瘤细胞的增殖和迁移，并有效诱导细胞凋亡。在肿瘤小鼠模型中表现出抗肿瘤活性。Capmatinib dihydrochloride 主要由 CYP3A4 和醛氧化酶代谢。

研究领域：Protein Tyrosine Kinase/RTK  |  Apoptosis

作用靶点：c-Met/HGFR  |  Apoptosis

In Vitro: Capmatinib (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.
Capmatinib (INCB28060) (0-10000 nM; 72 h) inhibits the proliferation of SNU-5, S114, H441 ａnd U-87MG.
Capmatinib (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.
Capmatinib (INCB28060) (0.24-63 nM; over night) prevents HGF-stimulated H441 cell migration.
Capmatinib (INCB28060) (0.5-50 nM; 20 min) suppresses phosphorylation of both EGFR ａnd HER-3 rapidly.
Capmatinib (INCB28060) (0-333 nM; 24 h) induces apoptosis in SNU-5 cells.

In Vivo: Capmatinib (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.
Capmatinib (INCB28060) (0.03-10 mg/kg; PO, single dosage) causes inhibition of c-MET phosphorylation in S114 tumor mice model.

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