CMLD012612,99.52%
产品编号：Bellancom-129767| CAS NO：2368900-35-8| 分子式：C31H33N3O7| 分子量：559.61
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CMLD012612
| 产品介绍 | CMLD012612 是一类含有异羟肟酸酯基团的 amidino-rocaglate，并且是有效的真核生物起始因子 4A (eIF4A) 抑制剂。CMLD012612 抑制细胞翻译，对 NIH/3T3 细胞具有细胞毒性，IC50 值为 2 nM。CMLD012612 通过修饰RNA解旋酶 eIF4A 来抑制真核细胞翻译起始，并具有有效的抗肿瘤活性。 | |||||||||
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| 生物活性 | CMLD012612 is an amidino-rocaglate containing a hydroxamate group and is a potent eukaryotic initiation factor 4A (eIF4A) inhibitor. CMLD012612 inhibits cell translation and is cytotoxic to NIH/3T3 cells with an IC50 value of 2 nM. CMLD012612 inhibits eukaryotic translation initiation by modifying the behavior of the RNA helicase (eIF4A) and possesses potent anti-neoplastic activity. | |||||||||
| 体外研究 |
The IC50 of CMLD012612 toward NIH/3T3 cells is 2 nM. The primary mechanism of action of CMLD012612 is dependent on eIF4A1, since eIF4A1em1jp cells are at least 10-fold more resistant than parental NIH/3T3 cells. The sensitivity of eIF4A1em1jp cells to CMLD012612 observed at higher concentrations may be due to the presence of wild-type eIF4A2 in the cells. 西域 has not independently confirmed the accuracy of these methods. They are for reference only. | |||||||||
| 体内研究 |
CMLD012612 (0.5 mg/kg; intraperitoneal injection; for 3 hours; female C57BL/6 mice) treatment effectively suppresses liver polysomes 3 hours after injection, indicating inhibitory activity toward protein synthesis. 西域 has not independently confirmed the accuracy of these methods. They are for reference only.
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| 体内研究 |
CMLD012612 (0.5 mg/kg; intraperitoneal injection; for 3 hours; female C57BL/6 mice) treatment effectively suppresses liver polysomes 3 hours after injection, indicating inhibitory activity toward protein synthesis. 西域 has not independently confirmed the accuracy of these methods. They are for reference only.
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| 性状 | Solid | |||||||||
| 溶解性数据 | ||||||||||
| 运输条件 | Room temperature in continental US; may vary elsewhere. | |||||||||
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| 参考文献 |
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