TC-E 5008

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Cat.No. 5244 - TC-E 5008 | C13H13NO2 | CAS No. 50405-58-8
Description: Selective mutant isocitrate dehydrogenase 1 (mIDH1) inhibitor; phenotypically lethal
Alternative Names: SYC 435
Chemical Name: 1-Hydroxy-4-methyl-6-(phenylmethyl)-2-(1H)pyridinone
Literature (4)

Biological Activity for TC-E 5008

TC-E 5008 is a selective mutant isocitrate dehydrogenase 1 (mIDH1) inhibitor (Ki = 120-190 nM). Displays >60-fold selectivity for mIDH1 (found in ~75% of gliomas) over wild type IDH1. Also inhibits D-2-hydroxyglutaric acid in cells expressing mIDH1 (EC50 = 2.4 μM). Does not display cytotoxicity towards non-cancerous human cells. Phenotypically lethal.

Technical Data for TC-E 5008

M. Wt 215.25
Formula C13H13NO2
Storage Store at +4°C
CAS Number 50405-58-8
PubChem ID 13590964
Smiles O=C1C=C(C)C=C(CC2=CC=CC=C2)N1O

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for TC-E 5008

Solvent Max Conc. mg/mL Max Conc. mM
DMSO 21.52 100
ethanol 21.52 100

Preparing Stock Solutions for TC-E 5008

The following data is based on the product molecular weight 215.25. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 4.65 mL 23.23 mL 46.46 mL
5 mM 0.93 mL 4.65 mL 9.29 mL
10 mM 0.46 mL 2.32 mL 4.65 mL
50 mM 0.09 mL 0.46 mL 0.93 mL

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References for TC-E 5008

References are publications that support the biological activity of the product.

Zheng et al (2013) Crystallographic investigation and selective inhibition of mutant isocitrate dehydrogenase. ACS Med.Chem.Lett. 4 542 PMID: 23795241

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Keywords: TC-E 5008, TC-E 5008 supplier, TC-E5008, selective, mutant, isocitrate, dehydrogenase, 1, (IDH1), inhibitors, inhibits, phenotypically, lethal, cancer, gliomas, D-2-hydroxyglutaric, acid, SYC435, SYC, 435, Isocitrate, 5244, Tocris Bioscience

Citations for TC-E 5008

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