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CAS No. : 1204669-58-8
MCE 国际站:Epacadostat
产品活性:Epacadostat (INCB 024360) 是一种有效,选择性的 IDO1 抑制剂, IC50 为 71.8 nM。
研究领域:Metabolic Enzyme/Protease
作用靶点:Indoleamine 2,3-Dioxygenase (IDO)
In Vitro: In cellular assays, Epacadostat (INCB 024360) selectively inhibits human IDO1 with IC50 values of approximately 10 nM, demonstrating little activity against other related enzymes such as IDO2 or tryptophan 2,3-dioxygenase (TDO). Epacadostat (INCB 024360) also exhibits significant activity toward mouse IDO1, with an IC50 value of 52.4 nM±15.7 nM, in a similar assay using mouse IDO1-transfected HEK293/MSR cells.
In Vivo: Female Balb/c mice bearing CT26 tumors are treated orally twice daily for 12 d with Epacadostat at 100 mg/kg. Epacadostat (INCB 024360) suppresses kynurenine equivalently in plasma, tumors, and lymph nodes. In na ve C57BL/6 mice, 50 mg/kg Epacadostat (INCB 024360) decreases plasma kynurenine levels within 1 hour and those levels stay at least 50% suppressed through the 8-hour time course.
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