AST-1306 from BOC Sciences

AST-1306 functions as an irreversible inhibitor, most likely through covalent interaction with Cys797 and Cys805 in the catalytic domains of EGFR and ErbB2, respectively. It inactivated pathways downstream of these receptors and thereby inhibited the proliferation of a panel of cancer cell lines. It blocks phosphorylation of EGFR and also prevents downstream pathways. It also dose-dependently inhibits EGF-induced EGFR phosphorylation in the A549 cancer cell line