EB-3D
产品说明书
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同义名 : | - |
| CAS号 : | 1839150-63-8 | |
| 货号 : | A1228334 | |
| 分子式 : | C30H36Br2N4O2 | |
| 纯度 : | 99%+ | |
| 分子量 : | 644.441 | |
| MDL号 : | MFCD32689452 | |
| 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 : |
DMSO: 50 mg/mL(77.59 mM)，配合低频超声助溶，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 H2O: 9 mg/mL(13.97 mM) |
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| 动物实验配方： |
| 生物活性 | |||
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| 描述 | Choline kinase (ChoK) catalyzes the phosphorylation of choline by ATP in the presence of Mg2+ to yield phosphocholine (PCho) and ADP. In humans, ChoKα1 and ChoKα2 derive from a single gene (chk-α) by alternative splicing. EB-3D, a potent and selective ChoKα inhibitor, shows an IC50 of 1 μM for human ChoKα1. In a panel of nine different human tumor-cell lines, EB-3D offered excellent antiproliferative activities against all cell lines with GI50 values ranging from 0.027 to 0.12 μM. The cell viability in the presence of EB-3D was also evaluated in Jurkat, HeLa and MDA-MB-231 cell lines. EB-3D significantly inhibited cell growth in three cell lines in a concentration-dependent manner. EB-3D induced a G1 arrest of the cell cycle, which occurred in a concentration-dependent manner in the three cell lines tested (Jurkat, MCF-7 and MDA-MB-231). Together with the G1 increase, a concomitant reduction was found in the S phase. Further, EB-3D at different concentrations after 72 h of incubation induced a modest increment in apoptotic cells only in Jurkat cells[1]. Experimental metastasis models obtained after the iv injection of murine E0771 or human MDA-MB-231 cells were treated with EB-3D at the dose of 2.5 mg/kg. After lung removal, the number of macrometastases as well as of micrometastases was significantly reduced in treated mice when compared with control lungs. In addition, a significant reduction of resected lung weight was appreciable after EB-3D treatment[2]. | ||
| 作用机制 | The 1-benzyl-4-(dimethylamino)pyridinium fragment of EB-3D performs a strong π-cation interaction with the Cho binding site[1]. | ||
| 实验方案 | |||
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| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
1.55mL 0.31mL 0.16mL |
7.76mL 1.55mL 0.78mL |
15.52mL 3.10mL 1.55mL |
| 参考文献 |
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