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抑制劑描述：

產(chǎn)品名稱：Epacadostat (INCB024360)

產(chǎn)品別名：INCB-024360,INCB 024360

英文別名：INCB-024360;INCB 024360

靶點(diǎn)：IDO1

CAS：1204669-58-8

純度：>98%

外觀：Powder

保存方法：store at -20℃ for one year（Powder）； in DMSO or others solvent store at 2-4℃ for two weeks, at -20℃ for six months.

描述：

Epacadostat (INCB024360) is a potent and selective indoleamine 2,3-dioxygenase (IDO1) inhibitor with IC50 of 10 nM. Phase 2.

溶解性：DMSO：87 mg/mL (198.52 mM)
Ethanol：53 mg/mL warmed (120.94 mM)

體外研究：

In IFN-γ–treated human HeLa cells, INCB024360 potently inhibits kynurenine production. INCB024360 also promotes T and natural killer (NK)-cell growth, increases IFN-gamma production, and reduces conversion to regulatory T (T(reg))-like cells.

體內(nèi)研究：INCB024360 (100 mg/kg, p.o.), via IDO1 inhibition, suppresses kyn generation and tumor growth in immunocompetent, but not immunodeficient, mice. In mice bearing CT26 colon carcinoma, INCB024360 (100 mg/kg, p.o.) also inhibits the growth of IDO-expressing tumors by reducing kynurenine.

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