Epacadostat

产品编号 T3548Cas号 1204669-58-8

别名 INCB 024360, 艾卡哚司他, IDO Inhibitor 1

Epacadostat (INCB 024360) 是选择性的IDO1抑制剂，IC50=71.8 nM。

Epacadostat

产品编号 T3548别名 INCB 024360, 艾卡哚司他, IDO Inhibitor 1Cas号 1204669-58-8

Epacadostat (INCB 024360) 是选择性的IDO1抑制剂，IC50=71.8 nM。

规格	价格	库存
2 mg	¥ 256	现货
5 mg	¥ 412	现货
10 mg	¥ 661	现货
25 mg	¥ 1,230	现货
50 mg	¥ 1,890	现货
100 mg	¥ 2,990	现货
200 mg	¥ 4,390	现货
500 mg	¥ 6,900	现货
1 g	¥ 9,490	现货
2 g	¥ 12,800	现货
1 mL x 10 mM (in DMSO)	¥ 453	现货

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产品介绍

生物活性

产品描述	Epacadostat (INCB 024360) 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.
靶点活性	IDO1:10 nM
体外活性	在IFN-γ处理的人类HeLa细胞中，INCB024360强效抑制kynurenine生产。INCB024360还促进T细胞和自然杀伤性(NK)细胞的增长，提高IFN-gamma的产生，并减少向调节性T (T(reg))-样细胞的转化。[1]
体内活性	INCB024360（100 mg/kg，p.o.）通过抑制IDO1，降低了免疫完整但非免疫缺陷小鼠中的kyn生成和肿瘤生长。[1] 在携带CT26结肠癌的小鼠中，INCB024360（100 mg/kg，p.o.）同样通过减少犬尿氨酸来抑制表达IDO的肿瘤生长。[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].
别名	INCB 024360, 艾卡哚司他, IDO Inhibitor 1

化学信息

分子量	438.23
分子式	C₁₁H₁₃BrFN₇O₄S
CAS No.	1204669-58-8

储存&溶解度

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

溶解度信息

Ethanol: 53 mg/mL (120.94 mM)

DMSO: 50 mg/mL (114.1 mM)

溶液配制表

DMSO/Ethanol

	1mg	5mg	10mg	50mg
1 mM	2.2819 mL	11.4095 mL	22.8191 mL	114.0953 mL
5 mM	0.4564 mL	2.2819 mL	4.5638 mL	22.8191 mL
10 mM	0.2282 mL	1.1410 mL	2.2819 mL	11.4095 mL
20 mM	0.1141 mL	0.5705 mL	1.1410 mL	5.7048 mL
50 mM	0.0456 mL	0.2282 mL	0.4564 mL	2.2819 mL
100 mM	0.0228 mL	0.1141 mL	0.2282 mL	1.1410 mL