Cayman Olutasidenib

Olutasidenib is an inhibitor of mutant isocitrate dehydrogenase 1 (IDH1; IC₅₀s = 0.021 and 0.114 µM for IDH1^R132H and IDH1^R132C, respectively). It is selective for mutant IDH1 over wild-type IDH1 and mutant IDH2 (IC₅₀s = 22.4, 27.3, and >100 μM for wild-type IDH1, IDH2^R172K, and IDH2^R140Q, respectively). Olutasidenib inhibits production of ɑ-hydroxyglutaric acid (2-HG; Item Nos. | ) in U87 cells expressing mutant IDH1^R132H, IDH1^R132C, IDH1^R132L, IDH1^R132G, and IDH1^R132S with IC₅₀ values of 0.009, 0.039, 0.042, 0.006, and 0.009 µM, respectively. It reduces intratumor 2-HG levels in HCT116-IDH1^R132H and HCT116-IDH1^R132C mouse xenograft models when administered at doses of 12.5, 25, and 50 mg/kg.

WARNING This product is not for human or veterinary use.