化合物 T11157 T11157

Product Introduction
Bioactivity


英文名: EGFR-IN-1

描述: EGFR-IN-1, an orally active and irreversible selective inhibitor targeting L858R/T790M mutant EGFR, exhibits strong antiproliferative and antitumor activity, particularly against H1975 cells and first line mutant HCC827 cells. This compound potently inhibits Gefitinib-resistant EGFR L858R/T790M mutations with a 100-fold selectivity over the wild-type EGFR.

体外活性: EGFR-IN-1 highly selective against a panel of 100 kinases.EGFR-IN-1 (10 μM; 72 hours) displays strong antiproliferative activity against the H1975 and HCC827 cells with IC50s of 4 and 28 nM, respectively. EGFR-IN-1 inhibits p-EGFR in H1975 and HCC827 cells with IC50s of 4 and 9 nM, respectively.

体内活性: EGFR-IN-1 shows a >50% inhibition of phosphorylation of EGFR for >12 h. EGFR-IN-1 reaches maximal concentration of 0.10 μM at 2 h and systemic exposure (AUC0-inf.) is 0.33 μM.EGFR-IN-1 (30 mg/kg; p.o.; daily for 2 weeks) displays significant tumor growth inhibition with no observed loss in body weight. EGFR-IN-1 evaluates in a time course PD experiment upon oral dosing at 30 mg/kg.

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

关键字: EGFR IN 1 | EGFR-IN-1 | EGFRIN1

相关产品: BEBT-109 | Cloperastine fendizoate | PD153035 hydrochloride | Tyrphostin A1 | Chalcone | Naluzotan | DZD1516 | LY 456236 hydrochloride | EGFR-IN-82 | Naquotinib

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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