AGI-5198 is a potent (IC50 = 70 nM) inhibitor of mutant isocitrate dehydrogenase 1(IDH1). It is selective for the R132H-IDH1 mutant and does not affect wild type cells. This mutation results in loss-of-function for oxidative decarboxylation of isocitrate and gain-of-function for production of...
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AGI-5198 is a potent (IC50 = 70 nM) inhibitor of mutant isocitrate dehydrogenase 1(IDH1). It is selective for the R132H-IDH1 mutant and does not affect wild type cells. This mutation results in loss-of-function for oxidative decarboxylation of isocitrate and gain-of-function for production of the oncometabolite R-2-hydroxyglutarate (R-2HG) form alpha-ketoglutarate (2-OG)
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