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An EGFR inhibitor (IC50 = 2 nM); selective for EGFR over Abl, Abl2, and c-Src tyrosine kinases at 1,000 nM; inhibits EGFR-mediated tyrosine phosphorylation in A431 cells (IC50 = 45 nM); inhibits the growth of PC-9 and HCC827 NSCLC cells (IC50s = 50 = 8,800 nM), which do not; inhibits migration of HCC827 cells at 100 nM and increases apoptosis by 43.7% at 10 nM; reduces tumor growth in a variety of mouse xenograft models at 50-120 mg/kg per day
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