Epacadostat

Epacadostat (INCB 024360) is a potent and selective indoleamine 2,3-dioxigenase 1 (IDO1) inhibitor with an IC50 of 71.8 nM[1]. Epacadostat can effectively reduce Trp metabolism, entailing increased activation and maturation of dendritic cells, and enhanced proliferation of effector T cells and natural killer cells (NKs), as well as attenuated Tregs expansion.

Product Specifications

CAS Number

[1204669-58-8]

Product Name Alternative

INCB 024360

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Indoleamine 2,3-Dioxygenase (IDO)

Type

Reference compound

Related Pathways

Metabolic Enzyme/Protease

Applications

COVID-19-immunoregulation

Field of Research

Inflammation/Immunology; Cancer

Assay Protocol

https://www.medchemexpress.com/INCB-024360.html

Concentration

10mM

Purity

99.65

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

BrC1=C(F)C=CC(N/C(C2=NON=C2NCCNS(N)(=O)=O)=N\O)=C1

Molecular Formula

C11H13BrFN7O4S

Molecular Weight

438.23

Precautions

H302, H315, H319, H335

References & Citations

[1]Liu X, et al. Selective inhibition of IDO1 effectively regulates mediators of antitumor immunity. Blood. 2010 Apr 29;115 (17) :3520-30.|[2]Koblish HK, et al. Hydroxyamidine inhibitors of indoleamine-2,3-dioxygenase potently suppress systemic tryptophan catabolism and the growth of IDO-expressing tumors. Mol Cancer Ther. 2010 Feb;9 (2) :489-98.|[3]Fu R, et al. LW106, a novel indoleamine 2,3-dioxygenase 1 inhibitor, suppresses tumour progression by limiting stroma-immune crosstalk and cancer stem cell enrichment in tumour micro-environment. Br J Pharmacol. 2018 Jul;175 (14) :3034-3049.