Chemical Structure : Epacadostat
CAS No.: 1204669-58-8
货号: 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.
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
10 mg | ¥780 | In stock | |
25 mg | ¥1280 | In stock | |
50 mg | ¥1980 | In stock | |
100 mg | ¥2980 | 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.
分子量 | 438.23 | |
分子式 | C11H13BrFN7O4S | |
外观性状 | Solid | |
储存条件 |
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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 |
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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