2. Metabolic Enzyme/Protease
  3. Isocitrate Dehydrogenase (IDH)
  4. 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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TC-E 5008 Chemical Structure

TC-E 5008 Chemical Structure

CAS No. : 50405-58-8

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TC-E 5008 Related Antibodies

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Description

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[1][2].

IC50 & Target[1]

R132H IDH1

190 nM (Ki)

R132C IDH1

120 nM (Ki)

WT IDH1

12.3 μM (Ki)

Cellular Effect
Cell Line Type Value Description References
HT-1080 IC50
> 30 μM
Compound: 2
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
[PMID: 25271760]
HT-1080 EC50
2.4 μM
Compound: 2
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
[PMID: 23795241]
Vero CC50
> 100 μM
Compound: 6f
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
[PMID: 35635945]
WI-38 EC50
> 50 μM
Compound: 2
Inhibition of cell proliferation of human WI38 cells by CCK8 assay
Inhibition of cell proliferation of human WI38 cells by CCK8 assay
[PMID: 25271760]
WI-38 EC50
> 50 μM
Compound: 2
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
[PMID: 23795241]
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.

TC-E 5008 Related Antibodies

Cell Proliferation Assay[2]

Cell Line: MCF-7, ZR-75, T-47D, MDA-MB-23 cells
Concentration: 2, 4, 6, 8, 10 μM
Incubation Time: 72 h
Result: Had anti-proliferative activity.
Molecular Weight

215.25

Formula

C13H13NO2
CAS No.
SMILES

ON1C(CC2=CC=CC=C2)=CC(C)=CC1=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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TC-E 5008 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

TC-E 500850405-58-8Isocitrate Dehydrogenase (IDH)mutant IDH1R132HR132Cbreast cancerInhibitorinhibitorinhibit

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