Aromatics, Heterocycles, Inhibitors, Pharmaceuticals, Intermediates & Fine Chemicals,
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AST-1306 is a selective irreversible inhibitor of the epidermal growth factor receptor (EGFR) 1 and 2. Studies show that AST-1306 inhibited the enzymatic activities of wild-type EGF) and ErbB2 as well as EGFR resistant mutant in both cell-free and cell-based systems. AST-1306 was more effective in inhibiting tumors with ErbB2-overexpressing cells than EGFR-overexpressing tumor.
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Xie, H. et al.: PLoS One, 6, e21487 (2011); Bai, F. et al.: Bioorg. Med. Chem. Lett., 22, 1365 (2012);