PD166866 is a selective FGFR1 tyrosine kinase inhibitor with an IC50 of 52.4 nM.
CAS：192705-79-6
分子式：C20H24N6O3
分子量：396.44
纯度：98%
存储：Store at -20°C

Background:

PD166866 is a selective FGFR1 tyrosine kinase inhibitor with an IC50 of 52.4 nM.

PD 166866 inhibits human full-length FGFR-1 tyrosine kinase with an IC50 value of 52.4 nM and is characterized as an ATP competitive inhibitor of the FGFR-1. 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. Daily exposure of PD 166866 to L6 cells at concentrations from 1 to 100 nM results in a concentration-related inhibition of bFGF-stimulated cell growth for 8 consecutive days with an IC50 value of 24 nM[1].

参考文献:
[1]. Panek RL, et al. In vitro biological characterization and antiangiogenic effects of PD 166866, a selective inhibitor of the FGF-1 receptor tyrosine kinase. J Pharmacol Exp Ther. 1998 Jul;286(1):569-77.