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CAS No.: 192705-79-6

PD-166866 Catalog No. CSN13927

Synonyms: PD166866

PD 166866 is a selective FGFR tyrosine kinase inhibitor with an IC50 of 52.4 nM.

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纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 FGFR

IC50:52.4nM
描述The FGFR (fibroblast growth factor receptor) family comprises four members, FGFR1, FGFR2, FGFR3 and FGFR4, ligand of which can induce cellular phosphorylation events, proliferation and potent antiangiogenic activity. PD166866 is a highly selective and nanomolar potent inhibitor of FGFR-1 tyrosine kinase with an IC50 value of 52.4nM (measure protein tyrosine kinase activity) and no effect on c-Src, platelet-derived growth factor receptor-b, EGFR or insulin receptor tyrosine kinases or on MAPK, PKC and CDK4 at concentrations as high as 50μM. Pre-treatment with PD 166866 on concentration of 10 or 100nM for 2h caused inhibition on autophosphorylation of FGFR1 induced by bFGF (25ng/ml) for 5 min in NIH 3T3 cells expressing endogenous FGFR1 and in L6 cells overexpressing the human FGFR1 tyrosine kinase, along with the inhibition of downstream p-ERK 1/2. Consistent with this, daily exposure to PD 166866 at concentrations 1-100nM for 8 consecutive days resulted in a concentration-related inhibition of bFGF-stimulated cell growth of L6 cells^[1]. Another mechanism action of PD166866 on negative control of cell proliferation maybe due to its activation of the apoptotic pathway, suggested by specific point as evaluation of DNA damage, lipoperoxidation of the cell membrane and increase of expression of PARP, an enzyme directly involved in DNA repair^[2].
作用机制PD 166866 is an ATP competitive inhibitor of FGFR1.^[1]
细胞研究
Cell Data
Cell Lines Concentration Assay Type Time Activity Description Data Sources
HUVEC cells - Function assay - Inhibition of microcapillary growth in HUVEC cells, IC50=0.1 μM 11063616
动物研究
剂量
Mice^[3] (i.p.): 20 mg/kg

给药途径
i.p.

Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
HUVEC cells	-	Function assay	-	Inhibition of microcapillary growth in HUVEC cells, IC50=0.1 μM	11063616

动物研究
剂量	Mice^[3] (i.p.): 20 mg/kg
给药途径	i.p.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.5224 mL
- 12.6122 mL
- 25.2243 mL
- 5 mM
- 0.5045 mL
- 2.5224 mL
- 5.0449 mL
- 10 mM
- 0.2522 mL
- 1.2612 mL
- 2.5224 mL

技术信息

CAS号

192705-79-6

储存条件

粉末: Keep in dark place,Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C20H24N6O3

运输

蓝冰

分子量

396.44

别名

PD166866

溶解度

DMSO	30.0 mg/mL (75.7 mM) warming
Water	Insoluble
Ethanol	8.0 mg/mL (20.2 mM) warming

动物实验配方

4% DMSO+30% PEG 300+2% Tween 80+water

4 mg/mL

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