产品说明书
PD173074
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同义名 : | - |
| CAS号 : | 219580-11-7 | |
| 货号 : | A150425 | |
| 分子式 : | C28H41N7O3 | |
| 纯度 : | 99%+ | |
| 分子量 : | 523.67 | |
| MDL号 : | MFCD08705327 | |
| 存储条件： |
粉末 Keep in dark place,Inert atmosphere,2-8°C 液体 -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : |
DMSO: 105 mg/mL(200.51 mM)，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： |
IP 2% DMSO+2% Tween80+40% PEG300+water 2 mg/mL clear PO 0.5% CMC-Na 35 mg/mL suspension |
| 生物活性 | |||
|---|---|---|---|
| 靶点 |
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| 描述 | Angiogenesis, playing a major role in the progression of human diseases such as diabetic retinopathy, atherosclerosis and cancer, involves the concerted action of a number of polypeptide factors such as VEGF, Ang1 and FGF. PD173074 is a selective dual inhibitor of both FGFR1 and VEGFR2 with IC50 value of 21.5nM (measured by kinase activity) and 100-200nM (measured by VEGFR2 auto-phosphorylation in NIH 3T3 cells), respectively. PD173074 inhibited auto-phosphorylation of FGFR1, induced by aFGF and heparin, of NIH-3T3 cells expressing FGFR1 endogenously in a dose-dependent manner with an IC50 in the range 1–5nM, as well as auto-phosphorylation of overexpressed VEGFR2 stimulated with VEGF (100ng/ml) with an IC50 of 100–200nM. Mice treated daily with PD173074 by intraperitoneal injection per day starting 3 days prior to pellet implantation exhibited inhibition of bFGF-induced neovascularization by 86% at a dose of 1mg/kg, as well as inhibition of VEGF induced neovascularization by 81% at a dose of 2mg/kg[1]. PD173704 can specifically and effectively inhibit multiple FGF-2-mediated responses of both oligodendrocyte progenitors, as well as differentiated oligodendrocytes with complete antagonization on two phenotypic alterations, downregulation of myelin proteins, and their re-entry into the cell cycle[2]. | ||
| 作用机制 | PD173074 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 |
| A204 | Growth Inhibition Assay | IC50=3.92075 μM | SANGER | ||
| A2058 | Growth Inhibition Assay | IC50=35.6061 μM | SANGER | ||
| A253 | Growth Inhibition Assay | IC50=15.3869 μM | SANGER | ||
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
1.91mL 0.38mL 0.19mL |
9.55mL 1.91mL 0.95mL |
19.10mL 3.82mL 1.91mL |
