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Epacadostat
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Epacadostat图片
CAS NO:1204669-58-8
包装与价格:
包装价格(元)
2 mg电议
5 mg电议
10 mg电议
25 mg电议
50 mg电议
100 mg电议
200 mg电议
500 mg电议
1 mL*10 mM(in DMSO)电议

产品名称
艾卡哚司他
INCB 024360
IDO inhibitor 1
产品介绍
EpacadoSTAT 是选择性的IDO1抑制剂,IC50=71.8 nM。

产品描述

Epacadostat is an oral-available inhibitor of indoleamine 2, 3-dioxygenase (IDO1), increasing the proliferation and activation of various immune cells and reducing tumor-associated regulatory T cells.

体外活性

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. [1]

体内活性

INCB024360 (100 mg/kg, p.o.), via IDO1 inhibition, suppresses kyn generation and tumor growth in immunocompetent, but not immunodeficient, mice. [1] In mice bearing CT26 colon carcinoma, INCB024360 (100 mg/kg, p.o.) also inhibits the growth of IDO-expressing tumors by reducing kynurenine. [2]

细胞实验

INCB 024360 (INCB024360) is dissolved in DMSO and stored, and then diluted with appropriate media before use[1]. To determine INCB 024360 activity against IDO in recombinant cells, HEK293/MSR cells are transiently transfected with full-length human or mouse IDO1, or mouse IDO2 cDNA, with Transit-293 transfection reagent or Lipofectamine 2000 reagents. INCB 024360 at different concentrations is added to the recovered transfected cells seeded at 2×104 cells per well in a 96-well plate (200 μL/well). The cells are incubated for 2 days, and kyn in the supernatants is measured as described in the HeLa cell assay. The tryptophan 2,3-dioxygenase (TDO) assay is performed similarly with HEK293/MSR cells transfected with a human TDO expression vector[1].

Cas No.

1204669-58-8

分子式

C11H13BrFN7O4S

分子量

438.23

别名

艾卡哚司他;INCB 024360;IDO Inhibitor 1

储存和溶解度

Ethanol:53 mg/mL (120.94 mM)
DMSO:79 mg/mL(180.8 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years