Epacadostat (INCB024360)
Catalog No.S7910
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).
1 Customer Review
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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
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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). | ||
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| 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] |
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| 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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Solubility (25°C)
| In vitro | DMSO | 87 mg/mL (198.52 mM) |
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| 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 |
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| Formula | C11H13BrFN7O4S |
| CAS No. | 1204669-58-8 |
| Storage | powder |
| in solvent | |
| Synonyms | N/A |
Bio Calculators
Molarity Calculator
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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)
*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).
Dilution Calculator
Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:
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This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )
* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).
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Definitions of molecular mass, molecular weight, molar mass and molar weight:
Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
Molarity Calculator
Clinical Trial Information
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT03516708 | Not yet recruiting | Rectal Cancer | Washington University School of Medicine|Incyte Corporation | January 31 2019 | Phase 1|Phase 2 |
| NCT03532295 | Not yet recruiting | Glioma|Glioblastoma | Washington University School of Medicine|Incyte Corporation | January 31 2019 | Phase 1|Phase 2 |
| NCT03491579 | Withdrawn | AML|Relapse | University Hospital Inselspital Berne | December 2018 | Phase 1 |
| NCT03402880 | Withdrawn | Extensive Stage Small Cell Lung Carcinoma | City of Hope Medical Center|Addario Lung Cancer Medical Institute | December 2018 | Phase 2 |
| NCT03325465 | Not yet recruiting | Squamous Cell Carcinoma of the Head and Neck | University of Chicago | November 2018 | Phase 2 |
| NCT03707457 | Not yet recruiting | Glioblastoma|Glioblastoma Multiforme | Sidney Kimmel Comprehensive Cancer Center at Johns Hopkins|Bristol-Myers Squibb | November 2018 | Phase 1 |
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.
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