TC-E 5008

Cat. No. 5244

TC-E 5008 C13H13NO2 [50405-58-8]

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Chemical Name: 1-Hydroxy-4-methyl-6-(phenylmethyl)-2-(1H)pyridinone

Biological Activity

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

M.Wt:
215.25
Formula:
C13H13NO2
Solubility:
Soluble to 100 mM in DMSO and to 100 mM in ethanol
Storage:
Store at +4°C
CAS No:
50405-58-8

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.

Certificate of Analysis / Product Datasheet / Safety Datasheet

References are publications that support the products' biological activity.

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, supplier, TC-E5008, selective, mutant, isocitrate, dehydrogenase, 1, (IDH1), inhibitors, inhibits, phenotypically, lethal, cancer, gliomas, D-2-hydroxyglutaric, acid, Tocris Bioscience, Other Dehydrogenase Inhibitor products

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