TPX-0131 T9414

Product Introduction
Bioactivity


英文名: TPX-0131

描述: 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。

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.

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

关键字: TPX0131 | TPX 0131 | TPX-0131

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途