Powder: -20°C for 3 years | In solvent: -80°C for 1 year
TPX-0131 是一种有效、选择性、CNS 渗透性和口服活性的野生型ALK 抑制剂 (IC50为 1.4 nM) 并且有效对抗 ALK 耐药突变,例如G1202R(IC50为 0.3 nM)、L1196M(IC50为 0.3 nM)。TPX-0131 具有很强的抗肿瘤活性。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
2 mg | ¥ 2,520 | 5日内发货 | ||
25 mg | ¥ 10,700 | 10-14周 | ||
50 mg | ¥ 13,995 | 10-14周 | ||
100 mg | ¥ 20,996 | 10-14周 |
产品描述 | TPX-0131 is a potent, selective, CNS-penetrant and orally active inhibitor of wild-type ALK ( IC 50 of 1.4 nM) and is potent against ALK-resistant mutation, e.g. G1202R ( IC 50 of 0.3 nM), L1196M ( IC 50 of 0.3 nM). TPX-0131 has strong antitumor activities [1]. |
体外活性 | TPX-0131 potently inhibits the resistance mutations of wild-type ALK (IC 50 = 1.4 nM) and 26 ALK. TPX-0131 inhibits C1156Y, E1210K/S1206C, L1198F/C1156Y, L1196M/L1198F, E1210K, L1196M, T1151M, deleted G1202, S1206R, G1202R/L1198F, F1174L, F1245C, R1275Q, and G1202R ALK mutations with IC50 values of <1 nM. TPX0131 has IC 50 values of 1-2 nM for the following ALK mutations: L1198F, L1152R, F1174S, T1151-L1152 insT, V1180L, G1269A, F1174C. TPX-0131 is less active against ALK mutations including I1171N, L1152P, D1203N, D1203N/E1210K, and G1269S, with IC 50 values of 2-7 nM [1]. TPX-0131 is a potent inhibitor of ALK autophosphorylation in Ba/F3 cells expressing EML4-ALK G1202R solvent front, EML4-ALK G1202R/L1196M, or EML4-ALK G1202R/L1198F mutations, with IC50 values of approximately 3-10 nM [1]. |
体内活性 | TPX-0131 (2-10 mg/kg; p.o.; twice a day; for 2 weeks) treatment at 2 mg/kg, 5 mg/kg, and 10 mg/kg caused dose-dependent tumor growth inhibition (TGI) of 64%, 120%, and 200% (complete regression), respectively [1]. Animal Model: Female SCID/beige mice (5-8 weeks old) bearing Ba/F3 cells [1] Dosage: 2 mg/kg, 5 mg/kg, and 10 mg/kg Administration: p.o.; twice a day; for 2 weeks Result: Caused complete tumor regression in ALK mutation-dependent xenograft models. |
分子量 | 447.41 |
分子式 | C21H20F3N5O3 |
CAS No. | 2648641-36-3 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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。
TPX-0131 2648641-36-3 TPX0131 TPX 0131 Inhibitor inhibitor inhibit