产品说明书
PD-166866
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同义名 : | - |
| CAS号 : | 192705-79-6 | |
| 货号 : | A339638 | |
| 分子式 : | C20H24N6O3 | |
| 纯度 : | 98% | |
| 分子量 : | 396.443 | |
| MDL号 : | MFCD12922514 | |
| 存储条件： |
粉末 Keep in dark place,Sealed in dry,2-8°C 液体 -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : |
DMSO: 3 mg/mL(7.57 mM)，配合低频超声，并水浴加热至45℃助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO |
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| 动物实验配方： |
4% DMSO+30% PEG 300+2% Tween 80+water 4 mg/mL |
| 生物活性 | |||
|---|---|---|---|
| 靶点 |
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| 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 | |||||
|---|---|---|---|---|---|
| 细胞系 | 浓度 | 检测类型 | 检测时间 | 活动说明 | 数据源 |
| HUVEC cells | Function assay | Inhibition of microcapillary growth in HUVEC cells, IC50=0.1 μM | 11063616 | ||
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
|
1 mM 5 mM 10 mM |
2.52mL 0.50mL 0.25mL |
12.61mL 2.52mL 1.26mL |
25.22mL 5.04mL 2.52mL |
