Epacadostat

Epacadostat is an inhibitor of indoleamine 2,3-dioxygenase 1 (IDO1) with an IC50 value of 7.1 nM in HeLa cells that demonstrates little activity against the related enzymes IDO2 or tryptophan 2,3-dioxygenase (TDO). It has been shown to promote T and natural killer-cell growth, to increase IFN-gamma production, and to reduce conversion to regulatory T (Treg)-like cells in a coculture system of human allogeneic lymphocytes with either dendritic cells or tumor cells. Epacadostat can also inhibit tumor growth in tumor-bearing mice in a lymphocyte-dependent manner.Formal Name: [C(Z)]-4-[[2-[(aminosulfonyl)amino]ethyl]amino]-N-(3-bromo-4-fluorophenyl)-N'-hydroxy-1,2,5-oxadiazole-3-carboximidamide. CAS Number: 1204669-58-8. Synonyms: INCB024360. Molecular Formula: C11H13BrFN7O4S. Formula Weight: 438.2. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 30 mg/ml, DMSO: 30 mg/ml, DMSO:PBS (pH 7.2)(1:5): 0.16 mg/ml, Ethanol: 20 mg/ml. lambdamax: 290 nm. SMILES: O/N=C(C1=NON=C1NCCNS(N)(=O)=O)\NC2=CC=C(F)C(Br)=C2. InChi Code: InChI=1S/C11H13BrFN7O4S/c12-7-5-6(1-2-8(7)13)17-11(18-21)9-10(20-24-19-9)15-3-4-16-25(14,22)23/h1-2,5,16,21H,3-4H2,(H,15,20)(H,17,18)(H2,14,22,23). InChi Key: FBKMWOJEPMPVTQ-UHFFFAOYSA-N.