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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- No. CAS: 50405-58-8
- Fòrmula: C13H13NO2
- Peso molecular:215.25
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
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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.
Chemical Information
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No. CAS 50405-58-8
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Peso molecular 215.25
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Fòrmula C13H13NO2
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SMILES
ON1C(CC2=CC=CC=C2)=CC(C)=CC1=O
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
TC-E 5008 Related Classifications
HY-110144 Related Classifications
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