CMLD012612
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.
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- CAS 番号: 2368900-35-8
- 分子式: C31H33N3O7
- 分子量:559.61
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保管条件:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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生物活性
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化学情報
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
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eIF4 |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| NIH3T3 | IC50 |
2 nM
Compound: 10; CMLDO12612
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Cytotoxicity against mouse NIH/3T3 cells assessed as reduction in cell viability incubated for 4 days by SRB assay
Cytotoxicity against mouse NIH/3T3 cells assessed as reduction in cell viability incubated for 4 days by SRB assay
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[PMID: 33592144] |
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female C57BL/6 mice[1]
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Dosage:0.5 mg/kg
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Administration:Intraperitoneal injection; for 3 hours
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Result:Effectively suppressed liver polysomes 3 hours after injection.
化学情報
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CAS 番号 2368900-35-8
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性状 Solid
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分子量 559.61
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分子式 C31H33N3O7
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Color White to light yellow
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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
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
純度とドキュメンテーション
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データシート (284 KB)
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SDS (251 KB)
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- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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取扱説明書 (2659 KB)
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
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