ETP-45658
产品说明书
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同义名 : | - |
| CAS号 : | 1198357-79-7 | |
| 货号 : | A952617 | |
| 分子式 : | C16H17N5O2 | |
| 纯度 : | 99%+ | |
| 分子量 : | 311.34 | |
| MDL号 : | MFCD29081201 | |
| 存储条件： |
Pure form Sealed in dry,2-8°C 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 | |||
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| 描述 | ETP-45658 is a potent PI3K nhibitor, with IC50s of 22.0 nM, 39.8 nM, 129.0 nM and 717.3 nM for PI3Kα, PI3Kδ, PI3Kβ and PI3Kγ, respectively. ETP-45658 had modest, but significant activity toward the class IV PI3-related kinase mTOR and DNA PK with IC50 values of 152 nM and 70.6 nM, respectively. ETP-45658 inhibits the proliferation of MCF7, PC3, 786-O, HTC116, and U251 cells, with EC50s of 0.48 μM, 0.49 μM, 2.62 μM, 3.53 μM, and 5.56 μM, respectively. Treatment with ETP-45658 at 10μM for 4h decreased in the phosphorylation of FOXO3a, Gsk3-β and p70 S6K in U2OS cells. ETP-45658 was a potent inducer of GFP-FOXO nuclear translocation with EC50 value of 45 nM. Treatment with ETP-45658 from 5 nM to 11.1μM. 11.1μM for 1 h induced a dose-dependent increase of GFP-FOXO nuclear translocation in U2foxRELOC cells. Treatment with ETP-45658 at 10μM for 24 h induced a clear G1 arrest of PC3 cells. Treatment with ETP-45658 at 10 μM for 1h decreased the expression of cyclin D1 and p-Akt on serine 473 in U2OS cells[1]. ETP-45658 potently inhibited cell proliferation within a broad range of human cancer cells, most potently suppressing the growth of breast cancer cells via inhibiting cell cycle[2]. ETP 45658 also reduced glucolipotoxicity-induced β-cell death. It decreased markers of glucolipotoxicity including caspase activation, mitochondrial depolarization, and increased calcium flux[3]. | ||
| 实验方案 | |||
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| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
3.21mL 0.64mL 0.32mL |
16.06mL 3.21mL 1.61mL |
32.12mL 6.42mL 3.21mL |
| 参考文献 |
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