PD-166866

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

Research Areas >> Cancer

FGFR1:52.4 nM (IC50)

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].

PD 166866 is dissolved in DMSO. PD 166866 or vehicle (0.5% DMSO, final concentration) are added every day to triplicate cultures of cells together with 25 ng/mL bFGF to stimulate FGF-driven growth. In some experiments, PD 166866 is added every day to triplicate cultures of cells together with 30 ng/mL PDGF-BB to stimulate PDGF-driven growth. Cell number is measured by Coulter counting on days 1, 3, 6 or 8 after drug exposure[1]

[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.

Nintedanib (BIBF 1120) | Infigratinib (BGJ398) | AZD4547 | PD173074 | Erdafitinib(JNJ-42756493) | FGF-401 | SU 5402 | Heparan Sulfate | Lucitanib | LY2784544 | BLU554 | Dovitinib (TKI-258, CHIR-258) | Rogaratinib | LY2874455 | BLU-9931