Crelosidenib (gentisate) is a selective oral inhibitor of mutant isocitrate dehydrogenase (IDH) enzymes, specifically targeting IDH1 R132H (IC50 of 6.27 nM), IDH1 R132C (IC50 of 3.71 nM), IDH2 R140Q (IC50 of 36.9 nM), and IDH2 R172K (IC50 of 11.5 nM). It demonstrates decreased activity against wild-type IDH enzymes. Crelosidenib is primarily utilized in research focusing on metabolic dysregulation and oncogenic pathways associated with IDH mutations in various cancers.
Crelosidenib (gentisate) is a selective oral inhibitor of mutant isocitrate dehydrogenase (IDH) enzymes, specifically targeting IDH1 R132H (IC50 of 6.27 nM), IDH1 R132C (IC50 of 3.71 nM), IDH2 R140Q (IC50 of 36.9 nM), and IDH2 R172K (IC50 of 11.5 nM). It demonstrates decreased activity against wild-type IDH enzymes. Crelosidenib is primarily utilized in research focusing on metabolic dysregulation and oncogenic pathways associated with IDH mutations in various cancers.
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