PD166866

Description: PD166866, a member of a new structural class of tyrosine kinase inhibitors, the 6-aryl-pyrido2, 3-dpyrimidines, is a a new nanomolar potent and selective small molecule inhibitor of FGFR (fibroblast growth factor-1 receptor) tyrosine kinase inhibitor with an IC50 of 52.4 nM. PD 166866 is a potent inhibitor of FGFR autophosphorylation in NIH 3T3 cells expressing endogenous FGFR-1 and in L6 cells overexpressing the human FGFR-1 tyrosine kinase. PD 166866 also inhibits bFGF-induced tyrosine phosphorylation of the 44- and 42-kDa (ERK 1/2) mitogen-activated protein kinase isoforms in L6 cells. PD 166866has potential use as antiproliferative/antiangiogenic agent for such therapeutic targets as tumor growth and neovascularization of atherosclerotic plaques.

References: J Exp Clin Cancer Res. 2009; 28:151; J Pharmacol Exp Ther. 1998; 286(1):569-77.