Article
AC0010, an Irreversible EGFR Inhibitor Selectively Targeting Mutated EGFR and Overcoming T790M-Induced Resistance in Animal Models and Lung Cancer Patients.
Molecular cancer therapeutics - 1 Nov 2016
Xu Xiao, Mao Long, Xu Wanhong, Tang Wei, Zhang Xiaoying, Xi Biao, Xu Rongda, Fang Xin, Liu Jia, Fang Ce, Zhao Li, Wang Xiaobo, Jiang Ji, Hu Pei, Zhao Hongyun, Zhang Li
Abstract excerpt
AC0010 is a pyrrolopyrimidine-based irreversible EGFR inhibitor, structurally distinct from previously reported pyrimidine-based irreversible EGFR inhibitors, such as osimertinib and rociletinib. AC0010 selectively inhibits EGFR-active and T790M mutations with up to 298-fold increase in potency compared with wild-type EGFR. In a xenograft model, oral administration of AC0010 at a daily dose of 500 mg/kg resulted...
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