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Epacadostat (INCB024360)

商品编号: TS3281
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详细介绍

l  基本信息

产品名称

Epacadostat

一般描述

Epacadostat is a potent and selective indoleamine 2,3-dioxygenase (IDO1) inhibitor with IC50 of 10 nM and displays high selectivity over other related enzymes such as IDO2 or tryptophan 2,3-dioxygenase (TDO).

别 称

INCB024360

纯 度

≥98.5%(HPLC)

CAS NO.

1204669-58-8

分子式

C11H13BrFN7O4S

分子量

438.23

适用范围

生物试剂,适用于细胞培养等

l  理化信息

外 观

固体

溶解性(25°C)

DMSO

≥50mg/ml

乙醇

≥50mg/ml

Very slightly soluble

l  生物学信息

生物活性/药理作用

Epacadostat is an orally available hydroxyamidine and inhibitor of indoleamine 2,3-dioxygenase (IDO1), with potential immunomodulating and antineoplastic activities. Epacadostat targets and binds to IDO1, an enzyme responsible for the oxidation of tryptophan into kynurenine. By inhibiting IDO1 and decreasing kynurenine in tumor cells, INCB024360 increases and restores the proliferation and activation of various immune cells, including dendritic cells (DCs), NK cells, and T-lymphocytes, as well as interferon (IFN) production, and a reduction in tumor-associated regulatory T cells (Tregs). Activation of the immune system, which is suppressed in many cancers, may inhibit the growth of IDO1-expressing tumor cells. IDO1 is overexpressed by a variety of tumor cell types and DCs.

l  存储

存储温度

-20°C

l  注意事项及免责声明

本产品仅用于实验研究,不得作为药物使用,不得用于家用或其它用途。

l  参考文献

1.    http://www.drugbank.ca

2.    https://ncit.nci.nih.gov

3.    https://www.ncbi.nlm.nih.gov