TC-E 5008
TC-E 5008 is a potent mutant IDH1 inhibitor with Ki values of 190 nM and 120 nM for R132H and R132C IDH1 mutants, respectively. TC-E 5008 exhibits very weak activity against WT-IDH1 with a Ki value of 12.3 μM. TC-E 5008 has anti-proliferative activity on multiple ER positive breast cancer cell lines.
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- CAS 番号: 50405-58-8
- 分子式: C13H13NO2
- 分子量:215.25
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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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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R132H IDH1 190 nM (Ki) |
R132C IDH1 120 nM (Ki) |
WT IDH1 12.3 μM (Ki) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HT-1080 | EC50 |
2.4 μM
Compound: 2
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Inhibition of IDH1 R132C mutant in human HT1080 cells assessed as production of D-2-hydroxyglutaric acid formation after 48 hrs by HPLC-MS method
Inhibition of IDH1 R132C mutant in human HT1080 cells assessed as production of D-2-hydroxyglutaric acid formation after 48 hrs by HPLC-MS method
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[PMID: 23795241] |
| HT-1080 | IC50 |
>30 μM
Compound: 2
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Inhibition of IDH1 R132C mutant in human HT1080 cells assessed as reduction in D2HG production incubated for 48 hrs by HPLC-MS method
Inhibition of IDH1 R132C mutant in human HT1080 cells assessed as reduction in D2HG production incubated for 48 hrs by HPLC-MS method
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[PMID: 25271760] |
| Vero | CC50 |
>100 μM
Compound: 6f
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Cytotoxicity against African green monkey Vero cells assessed as reduction in cell viability incubated for 24 hrs by MTS assay
Cytotoxicity against African green monkey Vero cells assessed as reduction in cell viability incubated for 24 hrs by MTS assay
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[PMID: 35635945] |
| WI-38 | EC50 |
>50 μM
Compound: 2
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Cytotoxicity against human WI38 cells assessed as growth inhibition after 48 hrs by MTS assay
Cytotoxicity against human WI38 cells assessed as growth inhibition after 48 hrs by MTS assay
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[PMID: 23795241] |
| WI-38 | EC50 |
>50 μM
Compound: 2
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Inhibition of cell proliferation of human WI38 cells by CCK8 assay
Inhibition of cell proliferation of human WI38 cells by CCK8 assay
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[PMID: 25271760] |
TC-E 5008 (compound 2; 48 h) inhibits the production of D2HG with an EC50 value of 2.4 μM in HT1080 fibrosarcoma cells , which harbor an IDH1(R132C) mutation[1].
TC-E 5008 (2-10 μM; 72 h) has anti-proliferative activity on multiple ER positive breast cancer cell lines[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MCF-7, ZR-75, T-47D, MDA-MB-23 cells
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Concentration:2, 4, 6, 8, 10 μM
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Incubation Time:72 h
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Result:Had anti-proliferative activity.
化学情報
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CAS 番号 50405-58-8
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分子量 215.25
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分子式 C13H13NO2
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SMILES
ON1C(CC2=CC=CC=C2)=CC(C)=CC1=O
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
TC-E 5008 関連分類
HY-110144 関連分類
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