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首页-小分子抑制剂&激动剂-Metabolic Enzyme/Protease-Indoleamine 2,3-Dioxygenase (IDO)-Epacadostat
Epacadostat

Chemical Structure : Epacadostat

CAS No.: 1204669-58-8

Epacadostat (INCB024360, INCB24360)

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.

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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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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

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.

物理化学性质&存储条件

分子量 438.23
分子式 C11H13BrFN7O4S
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

(Z)-N-(3-Bromo-4-fluorophenyl)-N'-hydroxy-4-[2-(sulfamoylamino)ethylamino]-1,2,5-oxadiazole-3-carboxamidine

参考文献

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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