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甲磺酸奥希替尼Osimertinib mesylate (AZD-9291 mesylate) 是不可逆的突变体选择性 EGFR 抑制剂;对EGFRL858R 和EGFRL858R/T790M 的 IC50 值分别为12 和 1 nM。
中文别名:
奥希替尼甲磺酸盐; 甲磺酸奥斯替尼; 迈瑞替尼甲磺酸盐; AZD9291(甲磺酸盐);
[1]. Cross DA, et al. AZD9291, an irreversible EGFR TKI, overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer. Cancer Discov. 2014 Sep;4(9):1046-61.
[2]. Finlay MR, et al. Discovery of a potent and selective EGFR inhibitor (AZD9291) of both sensitizing and T790M resistancemutations that spares the wild type form of the receptor. J Med Chem. 2014 Oct 23;57(20):8249-67.
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