Epacadostat, IDO1 inhibitor (TBI4499)

Description

Product Details

Formal Name: N-(3-Bromo-4-fluorophenyl)-N’-hydroxy-4-{[2-(sulfamoylamino)ethyl]amino}-1,2,5-oxadiazole-3-carboximidamide

Alternate Names: INCB024360

Molecular Formula: C₁₁H₁₃BrFN₇O₄S

Formula Weight: 438.20

CAS Number: 1204669-58-8

Purity: >98%

Formulation: powder

Solubility: Soluble in DMSO (up to at least 25 mg/ml)

Storage: -20°C

Stability: ≥ 1 year.

Applications

IDO1 inhibitor

Functions

Epacadostat is a potent (IC50 = 10nM) and selective inhibitor of indoleamine-2,3-dioxygenase 1 (IDO1) with no activity at IDO2 or TDO. It restored tryptophan levels and significantly impaired kynurenine generation in CT26 colon carcinoma (IC50 = 76 nM) and PAN02 pancreatic carcinoma (IC50 = 27 nM) cells. Epacadostat increases the number and activity of tumor-infiltrating lymphocytes as well as increasing the ratio of effector T cells to regulatory T cells. Because of these immune system enhancing properties, it is being investigated as a synergistic agent for use with other immuno-oncology agents such as anti-PD-1 and anti-CTL4 antibodies.

Application Procedures

First dissolved in DMSO (up to at least 25 mg/ml), then diluted to aqueous buffer. Solutions in DMSO may be stored at -20°C for up to 3 months.