TC-E 5008

Catalog # Availability Size / Price Qty
5244/10
5244/50
Cat.No. 5244 - TC-E 5008 | C13H13NO2 | CAS No. 50405-58-8
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Description: Selective mutant isocitrate dehydrogenase 1 (mIDH1) inhibitor; phenotypically lethal

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

Product Details
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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.

Background References

  1. Crystallographic investigation and selective inhibition of mutant isocitrate dehydrogenase.
    Zheng et al.
    ACS Med.Chem.Lett., 2013;4:542

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