Cas No.: | 192705-79-6 |
Chemical Name: | PD-166866,PD 166866 |
Synonyms: | PD-166866,PD 166866 |
SMILES: | O=C(NC(C)(C)C)NC1=NC2=NC(N)=NC=C2C=C1C3=CC(OC)=CC(OC)=C3 |
Formula: | C20H24N6O3 |
M.Wt: | 396.19 |
Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
Description: | PD166866 is a selective FGFR1 tyrosine kinase inhibitor with an IC50 of 52.4 nM. |
In Vitro: | 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]. |