For research use only. Not Intended for Therapeutic Use!
|IC50:||0.5/3 nM (EGFR/Erb2)|
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AST-1306 TsOH is a novel irreversible inhibitor of EGFR and ErbB2 with IC50 of 0.5 nM and 3 nM, also effective in mutation EGFR T790M/L858R, more potent to ErbB2-overexpressing cells, 3000-fold selective for ErbB family than other kinases.
IC50 value: 0.5/3 nM (EGFR/Erb2)
Target: EGFR/Erb2;Mutant EGFR T790M/L858R
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. Further studies showed that AST-1306 inactivated pathways downstream of these receptors and thereby inhibited the proliferation of a panel of cancer cell lines. AST-1306 is a potent(pM) and selective inhibitor of EGFR and ErbB4 (IC50 = 500pM and 800 pM, respectively). AST-1306 blocks phosphorylation of EGFR and also prevents downstream pathways. AST-1306 also dose-dependently inhibits EGF-induced EGFR phosphorylation in the A549 cancer cell line.
. Xie H, Lin L, Tong L et al. AST1306, a novel irreversible inhibitor of the epidermal growth factor receptor 1 and 2, exhibits antitumor activity both in vitro and in vivo. PLoS One. 2011;6(7):e21487.