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| Cas No.: | 1204669-58-8 |
| Chemical Name: | Epacadostat |
| Synonyms: | HY-15689;Epacadostat;INCB-24360(INCB-024360);Epacadostat (INCB024360);IDO inhibitor 1;INCB024360;INCB-024360;INCB-24360;INCB 024360;Epacadostat(INCB 024360);AK174791;71596A9R13;N-(3-bromo-4-fluorophenyl)-N'-hydroxy-4-{[2-(sulfamoylamino)ethyl]amino}-1,2,5-oxadiazole-3-carboximidamide;Epacadostat [USAN:INN];Epacadostat; INCB024360;Epacadostat (JAN/USAN/INN);GTPL8221;FBKMWOJEPMPVTQ-UHFFFAOYSA-N;INCB 24360;BDBM222999;BCP1 |
| SMILES: | BrC1=C(C([H])=C([H])C(=C1[H])/N=C(/C1C(=NON=1)N([H])C([H])([H])C([H])([H])N([H])S(N([H])[H])(=O)=O)\N([H])O[H])F |
| Formula: | C11H13BrFN7O4S |
| M.Wt: | 438.2328 |
| Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
| Description: | Epacadostat (INCB 024360) is a potent and selective indoleamine 2,3-dioxigenase 1 (IDO1) inhibitor with an IC50 of 71.8 nM. |
| 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 naïve 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]. |
| 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]. |
MSDS
COA
| LOT NO. | DOWNLOAD |
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| 2018-0101 |
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| 2018-0101 |
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