PD 166326 is a pyridopyrimidine-type inhibitor of receptor tyrosine kinases that inhibits c-abl (IC50 = 8 nM) and Bcr/Abl-dependent cell growth (IC50 = 0.4 nM). In addition to targeting a select group of receptor tyrosine kinases, PD 166326 also potently inhibits c-src (IC50 = 6 nM). Orally administered PD 166326 is well tolerated and effectively blocks Bcr/Abl kinase activity in vivo. Moreover, PD 166326 affects a distinct set of kinases from those targeted by imatinib mesylate (STI571) and can reduce the growth of some imatinib-resistant cells both in vitro and in vivo in animal models of chronic myelogenous leukemia.
产品描述
A pyridopyrimidine-type inhibitor of receptor tyrosine kinases that inhibits c-abl (IC50 = 8 nM) and Bcr/Abl-dependent cell growth (IC50 = 0.4 nM); also potently inhibits c-src (IC50 = 6 nM); effectively blocks Bcr/Abl kinase activity in vivo