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.
For research use only. We do not sell to patients.
- CAS No.: 50405-58-8
- Formula: C13H13NO2
- Molecular Weight:215.25
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Storage:
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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Biological Activity
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Chemical Information
- Protocols
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
Description
IC50 & Target
[1]|
R132H IDH1 190 nM (Ki) |
R132C IDH1 120 nM (Ki) |
WT IDH1 12.3 μM (Ki) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
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| 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] |
In Vitro
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. Further protocols information, click here.
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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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CAS No. 50405-58-8
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Molecular Weight 215.25
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Formula C13H13NO2
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SMILES
ON1C(CC2=CC=CC=C2)=CC(C)=CC1=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
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Breast Cancer Modeling
Breast cancer is a heterogeneous cancer, and it has been distinguished into four subtypes: luminal A, luminal B, HER2-positive and basal-like. Molecular mutations, epigenetic alterations, hormone exposure and immune microenvironment are related to the progression of breast cancer.
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Cell Viability Determination by MTT Colorimetric Assay
The following protocol uses the MTT colorimetric assay as a classic literature-established method for assessing cell viability/metabolic activity in cultured mammalian cells. MTT[3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide] is reduced by metabolically active cells to a colored formazan product; the amount of formazan is quantified spectrophotometrically and provides an indirect measure of metabolically active viable cells. Importantly, MTT reduction reflects cellular oxidoreductase/metabolic activity rather than an absolute direct count of living cells, so changes in cellular metabolism can alter the signal independently of cell number.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
TC-E 5008 Related Classifications
HY-110144 Related Classifications
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