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EGFR抑制剂AZD9291的使用说明?

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EGFR抑制剂AZD9291的使用说明?
EGFR抑制剂AZD9291的使用说明?
药物简介:
AZD9291 是口服不可逆的,选择性的突变体EGFR抑制剂,其对外显子19缺失的 EGFR,L858R/T790M EGFR,和 WT EGFR的IC50分别为12.92,11.44 和493.8 nM.
体外研究:
AZD9291 shows significantly more potent inhibition of proliferation in mutant EGFR cell lines compared to wild-type in vitro.
体内研究:
AZD9291(5mg/kg p.o.) causes profound regression of tumors across EGFRm+ (PC9) and EGFRm+/T790M (H1975) tumor models with profound inhibition of EGFR phosphorylation and key downstream signaling pathways such as AKT and ERK in vivo.
参考:www.selleck.cn/products/azd9291.html