Epacadostat

SKU: orb1304077

Description

Epacadostat (INCB 024360) is a potent and selective small molecule inhibitor of indoleamine 2,3-dioxygenase 1 (IDO1), exhibiting an IC50 of 71.8 nM. It is widely used in cancer immunology research to investigate the tumor microenvironment and has been evaluated in both in vitro assays and in vivo preclinical models.

Research Area

Immunology & Inflammation

Key Properties

• CAS Number: 1204669-58-8
• MW: 438.2
• Purity: >98%
• Formula: C₁₁H₁₃BrFN₇O₄S
• SMILES: NS(=O)(=O)NCCNc1nonc1\C(Nc1ccc(F)c(Br)c1)=N\O
• Target: Tryptophan
• Solubility: Soluble in DMSO (up to at least 25 mg/ml)

Bioactivity

• Target IC50:
  IDO1 (HeLa cells):7.4 nM|IDO1 (P1.HTR cells):54.46 nM ± 11.18 nM|IDO1:10 nM|IDO1 (HEK293 cells):52.4 nM ± 15.7 nM
• In Vivo:
  METHODS: Mice were injected subcutaneously with 200 μl TC-1 cells on the back. After the tumor was palpable, Epacadostat (INCB 024360) (50 mg/kg), IFN-γ (100 ng/mouse), and kynurenine (100 mg/kg) were injected intraperitoneally every day. Tumor volume was measured every 3 days. RESULTS Intraperitoneal injection of Epacadostat (INCB 024360) caused a significant increase in tumor volume and tumor weight, and inhibited the expression of CD80 on macrophages in tumor tissues.
• In Vitro:
  METHODS: Epacadostat (INCB 024360) (0.0001, 0.01, 1, 100, 10000nM) was used to treat SKOV-3 cells and the release of kynurenine was measured. RESULTS Epacadostat (INCB 024360) inhibited the catalytic activity of IDO1 with an IC50 value of 17.63 nM ± 2.26 (pIC50 = 7.76 ± 0.06).
• Cell Research:
  INCB 024360 (INCB024360) is dissolved in DMSO and stored, and then diluted with appropriate media before use. 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.

Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

INCB024360

Compound Identifiers

PubChem CID

135564890