Epacadostat (INCB024360)

Catalog No.S7910

Epacadostat (INCB024360) Chemical Structure

Molecular Weight(MW): 438.23

Epacadostat (INCB024360) 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).

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1 Customer Review

  • Macrophages were treated with 2 μM obatoclax, 0.1 μM SNS-032, 3 μM SaliPhe, 0.1 μM JNJ872, 1 μM gemcitabine, 1 μM epacadostat or 1 μM NLG919 or remained non-treated and infected with mock or IAV (moi 3). After 24 h cell viability was measured by CTG and results were plotted. Mean ± SD, n=3.

    FEBS J, 2016, doi: 10.1111/febs.13966.. Epacadostat (INCB024360) purchased from Selleck.

Purity & Quality Control

Choose Selective IDO Inhibitors

Biological Activity

Description Epacadostat (INCB024360) 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).
Targets
IDO1 [1]
(immune cells)
10 nM
In vitro

In IFN-γ–treated human HeLa cells, INCB024360 potently inhibits kynurenine production. INCB024360 also promotes T and natural killer (NK)-cell growth, increases IFN-gamma production, and reduces conversion to regulatory T (T(reg))-like cells. [1]

In vivo INCB024360 (100 mg/kg, p.o.), via IDO1 inhibition, suppresses kyn generation and tumor growth in immunocompetent, but not immunodeficient, mice. [1] In mice bearing CT26 colon carcinoma, INCB024360 (100 mg/kg, p.o.) also inhibits the growth of IDO-expressing tumors by reducing kynurenine. [2]

Protocol

Animal Research:[1] [2]
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  • Animal Models: Female C57BL/6 or Balb/c nu/nu mice bearing PAN02 pancreatic tumors
  • Formulation: 3% N,N–Dimethylacetamide, 10% (2-Hydroxypropyl) β-Cyclodextrin
  • Dosages: ~100 mg/kg, twice a day
  • Administration: p.o.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 87 mg/mL (198.52 mM)
Ethanol 53 mg/mL warmed (120.94 mM)
Water Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
10%DMSO+90%PEG400
For best results, use promptly after mixing.
30mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 438.23
Formula

C11H13BrFN7O4S

CAS No. 1204669-58-8
Storage powder
in solvent
Synonyms N/A

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03260894 Active not recruiting Renal Cell Carcinoma (RCC) Incyte Corporation|Merck Sharp & Dohme Corp. December 7 2017 Phase 3
NCT03516708 Not yet recruiting Rectal Cancer Washington University School of Medicine|Incyte Corporation October 31 2018 Phase 1|Phase 2
NCT03532295 Not yet recruiting Glioma|Glioblastoma Washington University School of Medicine|Incyte Corporation August 31 2018 Phase 1|Phase 2
NCT02042430 Active not recruiting Stage III Fallopian Tube Cancer AJCC v7|Stage III Ovarian Cancer AJCC v6 and v7|Stage III Primary Peritoneal Cancer AJCC v7|Stage IIIA Fallopian Tube Cancer AJCC v7|Stage IIIA Ovarian Cancer AJCC v6 and v7|Stage IIIA Primary Peritoneal Cancer AJCC v7|Stage IIIB Fallopian Tube Cancer AJCC v7|Stage IIIB Ovarian Cancer AJCC v6 and v7|Stage IIIB Primary Peritoneal Cancer AJCC v7|Stage IIIC Fallopian Tube Cancer AJCC v7|Stage IIIC Ovarian Cancer AJCC v6 and v7|Stage IIIC Primary Peritoneal Cancer AJCC v7|Stage IV Fallopian Tube Cancer AJCC v6 and v7|Stage IV Ovarian Cancer AJCC v6 and v7|Stage IV Primary Peritoneal Cancer AJCC v7 National Cancer Institute (NCI) December 31 2013 Early Phase 1
NCT03182894 Withdrawn Metastatic Colorectal Cancer James J Lee|Incyte Corporation|Merck Sharp & Dohme Corp.|University of Pittsburgh September 30 2018 Phase 1|Phase 2
NCT03347123 Recruiting Solid Tumors Incyte Corporation January 29 2018 Phase 1|Phase 2

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID