产品描述:
XL647 is a multi-kinase inhibitor (IC50s = 0.3, 16, 1.5, 8.7, and 1.4 nM for EGFR, ErbB2, KDR, FLT4, and EphB4, respectively).{45304} It is selective for these kinases over a panel of 10 tyrosine kinases and 55 serine/threonine kinases at 10 μM. XL647 inhibits growth of A431 cells expressing wild-type EGFR and H1975 non-small cell lung cancer (NSCLC) cells expressing both the activating mutant EGFRL858R and the drug resistance-associated mutant EGFRT790M (IC50s = 13 and 920 nM, respectively). In vivo, XL647 (10, 30, and 100 mg/kg) inhibits tumor growth and EGFR phosphorylation in an H1975 mouse xenograft model in a dose-dependent manner.