Capmatinib-dihydrochloride-hydrate-INC280-dihydrochloride-hydrate-DataSheet-生命科学试剂-MedChemExpress.pdf

Hotline: 400-820-3792 Inhibitors • Screening Libraries • Proteins www.MedChemE Capmatinib dihydrochloride hydrate Cat. No.: HY-13404C CAS No.: 1865733-40-9 Synonyms: INC280 dihydrochloride hydrate; INCB-28060 dihydrochloride hydrate 分⼦式: C₂₃H₂₁Cl₂FN₆O₂ 分⼦量: 503.36 作⽤靶点: c-Met/HGFR; Apoptosis 作⽤通路: Protein Tyrosine Kinase/RTK; Apoptosis 储存⽅式: Please store the product under the recommended conditions in the Certificate of Analysis. BIOLOGICAL ACTIVITY ⽣物活性 Capmatinib (INC280; INCB28060) dihydrochloride hydrate 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 hydrate 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 hydrate 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 hydrate 主要由 CYP3A4 和醛氧化酶代谢。 体外研究 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 [1]. Capmatinib (INCB28060) (0-10000 nM; 72 h) inhibits the proliferation of SN