AST1306, A Novel Irreversible Inhibitor of the Epidermal Growth Factor Receptor 1 and 2, Exhibits Antitumor Activity Both In Vitro and In Vivo

@inproceedings{Xie2011AST1306AN,
  title={AST1306, A Novel Irreversible Inhibitor of the Epidermal Growth Factor Receptor 1 and 2, Exhibits Antitumor Activity Both In Vitro and In Vivo},
  author={Hua Xie and Liping Lin and Linjiang Tong and Yong Jiang and Mingyue Zheng and Zhuo Chen and Xiaoyan Jiang and Xiaowei Zhang and Xiaowei Ren and Wenchao Qu and Yang Yang and Hua Wan and Yi Chen and Jian-ping Zuo and Hualiang Jiang and Mei-yu Geng and Jian Ding},
  booktitle={PloS one},
  year={2011}
}
Despite the initial response to the reversible, ATP-competitive quinazoline inhibitors that target ErbB-family, such a subset of cancer patients almost invariably develop resistance. Recent studies have provided compelling evidence that irreversible ErbB inhibitors have the potential to override this resistance. Here, we found that AST1306, a novel anilino-quinazoline compound, inhibited the enzymatic activities of wild-type epidermal growth factor receptor (EGFR) and ErbB2 as well as EGFR… CONTINUE READING

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