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

CMLD012612 

目录号: HY-129767
产品使用指南

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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CMLD012612 Chemical Structure

CMLD012612 Chemical Structure

CAS No. : 2368900-35-8

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Description

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]

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].

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].

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.
Molecular Weight

559.61

Formula

C₃₁H₃₃N₃O₇

CAS No.

2368900-35-8

SMILES

CC1=N[C@@]2(O)[C@H](C(N(OC)C)=O)[C@@H](C3=CC=CC=C3)[C@]4(C5=CC=C(OC)C=C5)OC6=C(C(OC)=CC(OC)=C6)[C@@]42N1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

References
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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

Keywords:

CMLD012612CMLD 012612CMLD-012612Eukaryotic Initiation Factor (eIF)Inhibitorinhibitorinhibit

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CMLD012612
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HY-129767
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