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 μ
M). Does not display cytotoxicity towards non-cancerous human cells. Phenotypically lethal.
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Crystallographic investigation and selective inhibition of mutant isocitrate dehydrogenase.
Zheng et al.
ACS Med.Chem.Lett., 2013;4:542