| 名称 | Tepotinib |
| 描述 | Tepotinib (EMD-1214063) is a c-MET tyrosine kinase inhibitor (IC50=3 nM) that is selective, orally active, and ATP-competitive. Tepotinib has antitumor effect and is used in the treatment of non-small cell lung cancer. |
| 体外活性 | Tepotinib inhibits HGF-induced c-Met phosphorylation in A549 cells with IC50 of 6 nM. Treatment with Tepotinib induces a marked reduction of c-Met–constitutive phosphorylation in EBC-1 cells with IC50 of 9 nM. Tepotinib effectively blocka phosphorylation of the major downstream effectors of the c-Met enzyme, such as Grb2, Gab1, Sos, PLCγ, and phosphoinositide 3-kinase, in EBC-1, MKN-45, and Hs746T cells in the range of 1 to 10 nM. Tepotinib considerably inhibits the viability of MKN-45 cells with IC50 of less than 1 nM. Treatment with Tepotinib (as low as 0.1 nM) inhibits HGF-induced NCI-H441 cell migration, whereas concentrations of 100 nM to 1 μM almost completely prevents it. [1] |
| 体内活性 | Tepotinib treatment, at doses of 10 mg/kg or more, results in more than 90% inhibition of c-Met phosphorylation in Hs746T xenograft tumor for a period of at least 72 hours. Tepotinib induces more than 50% reduction of cyclin D1 expression, which persists after 96 hours upon treatment with doses of 100 mg/kg. A transient induction of p27 and cleaved caspase-3 are also observed upon treatment with Tepotinib. Tepotinib (15 mg/kg, daily) treatment induces complete regression of gastric carcinoma xenografts Hs746T, in which c-Met is amplified, overexpressed, and activated in a ligand-independent fashion. [1] |
| 存储条件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 溶解度 | H2O : < 1 mg/mL (insoluble or slightly soluble)
DMSO : 1 mg/mL
Ethanol : < 1 mg/mL (insoluble or slightly soluble)
10% DMSO+90% Saline : 0.27 mg/mL (0.55 mM), Please add co-solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately.
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| 关键字 | Tepotinib | EMD 1214063 | EMD1214063 | MSC-2156119 | MSC 2156119 |
| 相关产品 | Gilteritinib | Larotrectinib sulfate | L-Ascorbic acid 2-phosphate trisodium | Crizotinib | Amitriptyline hydrochloride | 7,8-Dihydroxyflavone | Diosmetin | GW 441756 | Cabozantinib S-malate |
| 相关库 | 高选择性抑制剂库 | 经典已知活性库 | 膜蛋白靶向化合物库 | 激酶抑制剂库 | 抗癌上市药物库 | FDA 上市激酶抑制剂库 | FDA 上市药物库 | 已知活性化合物库 | 抗癌药物库 | 抗癌活性化合物库 |
United States
