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Chemical Structure : Epacadostat
CAS No.: 1204669-58-8
Catalog No.: PC-22836Not For Human Use, Lab Use Only.
Epacadostat (INCB24360, INCB024360) is a hihgly potent and selective, oral bioavailable indoleamine-2,3-dioxygenase 1 (IDO1) inhibitor with IC50 of 73 nM.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 10 mg | $78 | In stock | |
| 25 mg | $128 | In stock | |
| 50 mg | $198 | In stock | |
| 100 mg | $298 | In stock | |
| 250 mg | Get quote |
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Epacadostat (INCB24360, INCB024360) is a hihgly potent and selective, oral bioavailable indoleamine-2,3-dioxygenase 1 (IDO1) inhibitor with IC50 of 73 nM.
Epacadostat is highly potent IDO1 inhibitor in cells (HeLa IC50=7.4 nM) and in an IFN-γ induced whole blood (WB) assay (IC50=125 nM).
Epacadostat displays high selectivity (>1,000-fold) over the related dioxygenases, TDO and IDO2.
Epacadostat (50 mg/kg) reduced kynurenine levels in wild-type mice to basal levels present in IDO null mice (∼400 nM kynurenine). Epacadostat is efficacious in rodent models of melanoma and well-tolerated in preclinical IND toxicology studies.
| M.Wt | 438.23 | |
| Formula | C11H13BrFN7O4S | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
(Z)-N-(3-Bromo-4-fluorophenyl)-N'-hydroxy-4-[2-(sulfamoylamino)ethylamino]-1,2,5-oxadiazole-3-carboxamidine |
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1. Yue EW, et al. ACS Med Chem Lett. 2017 Mar 6;8(5):486-491.
2. Prendergast GC, et al. Cancer Res. 2017 Dec 15;77(24):6795-6811.
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