化合物 T11213L T11213L

Product Introduction
Bioactivity


英文名: Epertinib

描述: Epertinib is a reversible and selective tyrosine kinase inhibitor of EGFR, HER2, and HER4 (IC50s: 1.48 nM, 7.15 nM, and 2.49 nM). It displays a strong antitumor activity.

体外活性: Epertinib displays inhibitory activity against the growth of cancer cell lines expressing EGFR and/or HER2 (IC50s: 8.3 nM (NCI-N87 (stomach)), 9.9 nM (BT-474 (breast)), and 14 nM (SK-BR-3 (breast))) [1]. Epertinib shows no effect on KDR, IGF1R, SRC, KIT, and PDGFRβ (IC50, >10000 nM). Epertinib inhibits relative phosphorylation of EGFR and HER2 in NCI-N87 cells (IC50s: 4.5 and 1.6 nM) and it also inhibits MDA-MB-361 cell growth (IC50: 26.5 nM) [2].

体内活性: Epertinib displays antitumor activity in nude mice bearing NCI-N87 xenograft via oral administration for 21 days ( ED50:10.2 mg/kg). Epertinib (50 mg/kg, p.o.) is four times more potent activity than GW572016 and completely inhibits the growth of cancer cells in mice [1] and it also obviously decreases the brain tumor volume in the breast cancer intraventricular injection mouse brain metastasis model [2].

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

关键字: Epertinib | S 22611 | S22611

相关产品: Canertinib | Antiproliferative agent-34 | Canertinib dihydrochloride | EGFR-IN-11 | Depatuxizumab | EGFR-IN-1 hydrochloride | CNX-2006 | Mutated EGFR-IN-2 | Sulforaphene | H-9 dihydrochloride

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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