1. Metabolic Enzyme/Protease
  2. Isocitrate Dehydrogenase (IDH)
  3. 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.

TC-E 5008 Chemical Structure

TC-E 5008 Chemical Structure

CAS No. : 50405-58-8

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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)

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.

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.

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Product Name:
TC-E 5008
Cat. No.:
HY-110144
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