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Epacadostat

Cat. No. M6136
Epacadostat Structure
Synonym:

INCB024360

Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
10mM/1mL In DMSO USD 100 In stock
5mg USD 80 In stock
25mg USD 300 In stock
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Quality Control
Biological Activity

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.

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

Protocol
Cell Experiment
Cell lines CEA-specific T-cell
Preparation method The IDO1 selective inhibitor epacadostat, obtained through a Cooperative Research and Development Agreement with Incyte Corporation (Wilmington, DE), was dissolved in DMSO and used at different concentrations as described. The concentration used in most experiments, 1.0 μM, was chosen to mimic the serum concentration observed in patients receiving 300 mg BID, where there was > 90% inhibition of IDO1.
Concentrations 0, 0.25 or 1.0 μM
Incubation time 48 h
Animal Experiment
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
Dosages ~100 mg/kg, twice a day
Administration p.o.
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 438.23
Formula C11H13BrFN7O4S
CAS Number 1204669-58-8
Purity 98.49%
Solubility 87 mg/mL in DMSO
Storage at -20°C
References

The IDO1 selective inhibitor epacadostat enhances dendritic cell immunogenicity and lytic ability of tumor antigen-specific T cells.
Jochems C, et al. Oncotarget. 2016 Jun 21;7(25):37762-37772. PMID: 27192116.

Potential Underprediction of Warfarin Drug Interaction From Conventional Interaction Studies and Risk Mitigation: A Case Study With Epacadostat, an IDO1 Inhibitor.
Shi JG, et al. J Clin Pharmacol. 2016 Nov;56(11):1344-1354. PMID: 26990117.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: Epacadostat, INCB024360 supplier, inhibitors

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