Epacadostat (INCB 024360) is an oral, potent and selective IDO1 inhibitor with IC50 value of 71.8 nM.

IDO1:10 nM

方法：Epacadostat (INCB 024360)（0.0001，0.01,1,100,10000nM） 处理 SKOV-3 细胞，处理后释放出犬尿氨酸的的倍数。
结果：Epacadostat (INCB 024360) 抑制了 IDO1 的催化活性，IC50值为17.63 nM ± 2.26（pIC50 = 7.76 ± 0.06）。[2]

方法：小鼠在背部皮下注射200μl TC-1细胞等到肿瘤触及到后每天腹腔注射Epacadostat (INCB 024360) （50mg/kg）、IFN-γ（100ng/只）、犬尿氨酸（100mg/kg），每3天检测一次肿瘤体积。
结果：腹膜内注射Epacadostat (INCB 024360) 引起肿瘤体积，肿瘤重量的显着增加，同时抑制肿瘤组织中巨噬细胞的CD80表达。[3]

INCB 024360 (INCB024360) is dissolved in DMSO and stored, and then diluted with appropriate media before use[1]. To determine INCB 024360 activity against IDO in recombinant cells, HEK293/MSR cells are transiently transfected with full-length human or mouse IDO1, or mouse IDO2 cDNA, with Transit-293 transfection reagent or Lipofectamine 2000 reagents. INCB 024360 at different concentrations is added to the recovered transfected cells seeded at 2×104 cells per well in a 96-well plate (200 μL/well). The cells are incubated for 2 days, and kyn in the supernatants is measured as described in the HeLa cell assay. The tryptophan 2,3-dioxygenase (TDO) assay is performed similarly with HEK293/MSR cells transfected with a human TDO expression vector[1].