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PD166866
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
PD166866图片
CAS NO:192705-79-6
规格:≥98%
包装与价格:
包装价格(元)
2mg电议
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议
250mg电议
500mg电议

产品介绍
理化性质和储存条件
Molecular Weight (MW)396.44
FormulaC20H24N6O3
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)
SMILES O=C(NC(C)(C)C)NC1=NC2=NC(N)=NC=C2C=C1C3=CC(OC)=CC(OC)=C3
Synonyms PD166866; PD166866; PD 166866
实验参考方法
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: PD166866, a member of a new structural class of tyrosine kinase inhibitors, the 6-aryl-pyrido[2,3-d]pyrimidines, 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.


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 modelFemale nude mice
Formulation & Dosage20 mg/kg; i.p. injection.
ReferencesJ 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.