Description |
A cell-permeable aminopyrimidine oxime compound that potently inhibits EGFR/ErbB1/HER1, ErbB2/HER2/neu, and ErbB4/HER4 kinase activity (IC 50 = 22, 38 and 21 nM, respectively) in an ATP-competitive manner and effectively suppresses cellular receptor phosphorylation (IC 50 = 223 and 107 nM against basal HER2 and EGF-induced EFGR phosphorylation, respectively, in SKBR3 and A431 cultures) as well as HER2- and EGFR-dependent cancer cell proliferations (IC 50 <1µM), while exhibiting much reduced or little activity against a panel of 202 other kniases
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