Olutasidenib

Olutasidenib is an inhibitor of mutant isocitrate dehydrogenase 1 (IDH1, IC50s = 0.021 and 0.114 µM for IDH1R132H and IDH1R132C, 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, IDH2R172K, and IDH2R140Q, respectively). Olutasidenib inhibits production of alpha-hydroxyglutaric acid (2-HG, Cay-25894, Cay-16374) in U87 cells expressing mutant IDH1R132H, IDH1R132C, IDH1R132L, IDH1R132G, and IDH1R132S 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-IDH1R132H and HCT116-IDH1R132C mouse xenograft models when administered at doses of 12.5, 25, and 50 mg/kg.Formal Name: 5-[[(1S)-1-(6-chloro-1,2-dihydro-2-oxo-3-quinolinyl)ethyl]amino]-1,6-dihydro-1-methyl-6-oxo-2-pyridinecarbonitrile. CAS Number: 1887014-12-1. Synonyms: FT-2102. Molecular Formula: C18H15ClN4O2. Formula Weight: 354.8. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMSO: soluble. lambdamax: 236, 335 nm. SMILES: O=C1C([C@H](C)NC2=CC=C(C#N)N(C)C2=O)=CC3=CC(Cl)=CC=C3N1. InChi Code: InChI=1S/C18H15ClN4O2/c1-10(21-16-6-4-13(9-20)23(2)18(16)25)14-8-11-7-12(19)3-5-15(11)22-17(14)24/h3-8,10,21H,1-2H3,(H,22,24)/t10-/m0/s1. InChi Key: NEQYWYXGTJDAKR-JTQLQIEISA-N.