Product Name

Epacadostat

General description

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).

Synonym

INCB024360

Purity

≥98.5%(HPLC)

CAS Number

1204669-58-8

Formula

C¹¹H¹³BrFN⁷O⁴S

Molecular Weight

438.23

Suitability

BioReagent, suitable for cell culture, etc.

l  Physical and Chemical Information

Appearance

Solid

Solubility(25°C)

DMSO

≥50mg/mL

Ethanol

≥50mg/mL

Water

Very slightly soluble

l  Biological Information

Biochem/Physiol  Actions

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  Storage

Storage temp.

-20°C

l  Precautions and Disclaimer

This product is for R&D use only, not for drug, household, or other uses.

l  References

1.    http://www.drugbank.ca

2.    https://ncit.nci.nih.gov

3.    https://www.ncbi.nlm.nih.gov