【产品介绍】：

产品名称 CO-1686(AVL-301) 英文名称 CO-1686 (AVL-301) 规格或纯度 ≥99% 生化机理 Description:IC50 Value: 21.5±1.7 nM (EGFRL858R/T790M); 303.3 ± 26.7 nM (EGFRWT) [1]CO-1686 is a novel, irreversible and orally delivered kinase inhibitor that specifically targets the mutant forms of EGFR including T790M while exhibiting minimal activity towards the wild-type (WT) receptor.in vitro: CO-1686 is a potent inhibitor of EGFR L858R/T790M kinase (kinact/Ki = (2.41 ± 0.30) x 105 M-1s-1) and is approximately 22-fold selective over WT EGFR (kinactt/Ki = (1.12 ± 0.14) x 104 M-1s-1). CO-1686 potently inhibited proliferation in the mutant-EGFR NSCLC cellswith GI50 values ranging from 7 - 32 nM. In comparison, the GI50 value for A431 cells, an epidermoid cell line that is driven by amplified WT EGFR(19), was 547 nM. Two cell linesexpressing WT EGFR in the presence of an N- or KRAS mutation (NCI-H1299 and NCI-H358,respectively) were inhibited by CO-1686 at a concentration of 4275 and 1806 nM, respectively [1].CAS编号 1374640-70-6 溶解性 DMSO 100 mg/mL Water <1 mg/mL Ethanol <1 mg/mL 储存温度 储存温度-20°C 分子量 555.55 分子式 C27H28F3N7O3 PubChem CID 57335384