Network Version
Epacadostat Data Sheet
| Product Name: | Epacadostat |
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|---|---|---|
| CAS No.: | 1204669-58-8 | |
| Cat. No.: | HY-15689 | |
| MWt: | 438.23 | |
| Formula: | C11H13BrFN7O4S | |
| Purity : | >98% | |
| Solubility: | DMSO : 100 mg/mL (ultrasonic) | |
| Mechanisms: | Target: Cancer Inflammation/Immunology | |
| Biological Activity: | ||
| Epacadostat (INCB 024360) is a potent and selective indoleamine 2,3-dioxigenase 1 (IDO1) inhibitor with an IC50 of 71.8 nM[1]. Epacadostat can effectively reduce Trp metabolism, entailing increased activation and maturation of dendritic cells, and enhanced proliferation of effector T cells and natural killer cells (NKs), as well as attenuated Tregs expansion. IC50 & Target:IC50: 71.8 nM±17.5 nM (IDO1), 7.1 nM±0.6 nM (IDO1, in HeLa cells)[1] 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[1]. 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[2]. | ||
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