Theliatinib (HMPL-309) 是一种有效、ATP 竞争性、高度选择性的 EGFR 抑制剂，对 EGFR 及其下游蛋白 AKT 和 ERK 的磷酸化水平具有很强的抑制作用，具有抗肿瘤活性。Theliatinib (HMPL-309) 对野生型 EGFR 的 Ki 和 IC50 值分别为 0.05 nM 和 3 nM，对 EGFR T790M/L858R 突变体的 IC50 值为 22 nM。
货号:ajcx14288
CAS:1353644-70-8
分子式:C25H26N6O2
分子量：442.51
溶解度:DMSO: 5 mg/mL (11.30 mM)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

Theliatinib (HMPL-309) is a potent, ATP-competitive and highly selective EGFR inhibitor, significantly inhibits phosphorylation of EGFR (p-EGFR) and its downstream targets, AKT and ERK (p-AKT and p-ERK), with anti-tumor activity. Theliatinib (HMPL-309) shows a Ki of 0.05 nM for wild type EGFR, and IC50s of 3 and 22 nM for EGFR and EGFR T790M/L858R mutant, respectively[1].

[1]. Ren Y, et al. Anti-tumor efficacy of theliatinib in esophageal cancer patient-derived xenografts models with epidermal growth factor receptor (EGFR) overexpression and gene amplification. Oncotarget. 2017 Apr 19;8(31):50832-50844.