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AST-1306 is a selective, irreversible inhibitor of ErbB2 and EGFR with IC50 values of 0.5nM and 3nM, respectively [1].

AST-1306 is designed and synthesized based on the chemical structure of lapatinib. The molecular docking method shows AST-1306 binds to the ATP-binding pocket of the kinases and form covalent bind with certain amino acids. AST-1306 can inhibit EGFR and ErbB2 in a cell-free assay with more than 3000-fold selectivity to other kinases. Besides the wild-type EGFR, AST-1306 also inhibits EGFR mutant T790M/L858R both in a cell-free assay and in HIH3T3 cells. The growth of the cells is suppressed by AST-1306 due to the inhibition of the phosphorylation of EGFR. It also occurs in some human cancer cells. Experiments have proved that AST-1306 notly inhibits the phosphorylation of EGFR and ErbB2 and subsequently decreases the downstream pathways of these kinases in A549 cells, Calu-3 cells and SK-OV-3 cells. Moreover, AST-1306 potently inhibits the tumor growth both in ErbB2-overexpressing xenograft models and FVB-2/Nneu transgenic mouse model [1].

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