ERK5-IN-2
产品说明书
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同义名 : | - |
| CAS号 : | 1888305-96-1 | |
| 货号 : | A1164824 | |
| 分子式 : | C17H11BrFN3O2 | |
| 纯度 : | 99%+ | |
| 分子量 : | 388.19 | |
| MDL号 : | MFCD32174287 | |
| 存储条件： |
Pure form Inert atmosphere, room temperature In solvent -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : | - | |
| 动物实验配方： |
| 生物活性 | |||
|---|---|---|---|
| 描述 | Extracellular signal-regulated kinase 5 (ERK5), a member of the mitogen-activated protein kinase (MAPK) family, is ubiquitously expressed in mammalian tissues and cell types, where it is activated by extracellular stimuli, including several growth factors and cellular stresses[1]. ERK5-IN-2 is an orally active, sub-micromolar, selective ERK5 inhibitor with IC50s of 0.82 μM, 3 μM for ERK5 and ERK5 MEF2D, respectively[2]. An anti-angiogenic effect was apparent with Matrigel plugs from mice treated with ERK5-IN-2 (100 mg/kg, p.o.) twice daily for 7 days[2]. In a human tumour xenograft model (A2780 cells), ERK5-IN-2 (100 mg/kg, p.o.) treatment twice-daily for 10 days led to significant tumour volume reduction by 57% when compared to the control group[2]. | ||
| 作用机制 | ERK5-IN-2 binds in the ERK5 ATP-binding site. | ||
| 实验方案 | |||
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| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
2.58mL 0.52mL 0.26mL |
12.88mL 2.58mL 1.29mL |
25.76mL 5.15mL 2.58mL |
| 参考文献 |
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