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  2. Cell Cycle/DNA Damage
  3. Eukaryotic Initiation Factor (eIF)
  4. CMLD012612

CMLD012612 是一類含有異羥肟酸酯基團(tuán)的 amidino-rocaglate，并且是有效的真核生物起始因子 4A (eIF4A) 抑制劑。CMLD012612 抑制細(xì)胞翻譯，對(duì) NIH/3T3 細(xì)胞具有細(xì)胞毒性，IC50 值為 2 nM。CMLD012612 通過(guò)修飾RNA解旋酶 eIF4A 來(lái)抑制真核細(xì)胞翻譯起始，并具有有效的抗腫瘤活性。

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CMLD012612 Chemical Structure

CMLD012612 Chemical Structure

CAS No. : 2368900-35-8

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規(guī)格 價(jià)格 是否有貨
1 mg ￥16500
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5 mg 現(xiàn)貨 詢問價(jià)格 & 貨期

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  • 生物活性

  • 純度 & 產(chǎn)品資料

  • 參考文獻(xiàn)

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]
體外研究
(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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
體內(nèi)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].

MCE 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 號(hào)
性狀

固體

顏色

White to light yellow

運(yùn)輸條件

Room temperature in continental US; may vary elsewhere.
儲(chǔ)存方式
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
純度 & 產(chǎn)品資料
參考文獻(xiàn)

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產(chǎn)品名稱：
CMLD012612
目錄號(hào)：
HY-129767
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