Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Tepotinib (EMD-1214063) 是一种具有潜在抗肿瘤活性的 MET 酪氨酸激酶抑制剂。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 397 | 现货 | ||
2 mg | ¥ 588 | 现货 | ||
5 mg | ¥ 982 | 现货 | ||
10 mg | ¥ 1,690 | 现货 | ||
25 mg | ¥ 3,190 | 现货 | ||
50 mg | ¥ 3,850 | 现货 | ||
100 mg | ¥ 5,520 | 现货 | ||
500 mg | ¥ 11,300 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 1,130 | 现货 |
产品描述 | Tepotinib (EMD-1214063) is an inhibitor of MET tyrosine kinase with potential antineoplastic activity. |
靶点活性 | c-Met:4 nM |
体外活性 | EMD 1214063 inhibits HGF-induced c-Met phosphorylation in A549 cells with IC50 of 6 nM. Treatment with EMD 1214063 induces a marked reduction of c-Met–constitutive phosphorylation in EBC-1 cells with IC50 of 9 nM. EMD 1214063 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. EMD 1214063 considerably inhibits the viability of MKN-45 cells with IC50 of less than 1 nM. Treatment with EMD 1214063 (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 | EMD 1214063 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. EMD 1214063 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 EMD 1214063. EMD 1214063 (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] |
别名 | 特泊替尼, EMD-1214063, MSC2156119 |
分子量 | 492.57 |
分子式 | C29H28N6O2 |
CAS No. | 1100598-32-0 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
H2O: < 1 mg/mL (insoluble or slightly soluble)
Ethanol: < 1 mg/mL (insoluble or slightly soluble)
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
Tepotinib 1100598-32-0 Tyrosine Kinase/Adaptors Trk receptor c-Met/HGFR TAM Receptor 特泊替尼 EMD-1214063 EMD 1214063 MSC2156119 EMD1214063 MSC-2156119 MSC 2156119 Inhibitor inhibitor inhibit