product name PD-166866
Description: PD166866 is a novel, potent and selective FGFR 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.
References: J Exp Clin Cancer Res. 2009;28:151; J Pharmacol Exp Ther. 1998;286(1):569-77.
396.44
Formula
C20H24N6O3
CAS No.
192705-79-6
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 14 mg/mL (35.3 mM)
Water: <1 mg/mL
Ethanol: 3 mg/mL (7.6 mM)
Solubility (In vivo)
Synonyms
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19420984
| In Vitro |
In vitro activity: 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. Kinase Assay: Cell Assay: 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. |
|---|---|
| In Vivo | |
| Animal model | Female nude mice |
| Formulation & Dosage | 20 mg/kg; i.p. injection. |
| References | J Exp Clin Cancer Res. 2009;28:151; J Pharmacol Exp Ther. 1998;286(1):569-77; Biochem Biophys Res Commun. 2016;474(1):1-7. |
