CMLD012612

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CMLD012612 

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。

CMLD012612

CMLD012612 Chemical Structure

CAS No. : 2368900-35-8

规格 价格 是否有货
1 mg ￥16500 询问价格 & 货期
5 mg ￥36000 询问价格 & 货期

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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[1].

IC50 & Target

eIF4A[1]
体外研究
(In Vitro)

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[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究
(In Vivo)

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[1].
When administered to mice bearing myr-Akt/Em-Myc lymphomas, CMLD012612 (0.2 mg/kg; intraperitoneal injection; daily; for 5 days; female C57BL/6 mice) treatment effectively synergizes with Doxorubicin, leading to complete tumor loss[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Female C57BL/6 mice[1]
Dosage: 0.5 mg/kg
Administration: Intraperitoneal injection; for 3 hours
Result: Effectively suppressed liver polysomes 3 hours after injection.

分子量

559.61

Formula

C31H33N3O7
CAS 号

2368900-35-8
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Chu J, et al. Amidino-Rocaglates: A Potent Class of eIF4A Inhibitors. Cell Chem Biol. 2019 Nov 21;26(11):1586-1593.

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