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).
3 Customer Reviews
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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.
e Tumor growth kinetics of RIl-175 tumors for control mice, epacadostat, anti-PD-1, or combination therapy of anti-PD-1 and epacadostat. f Tumors weight was recorded as grams (g) of tumor tissue. *P < 0.05, **P < 0.01, ***P < 0.001, ****P < 0.0001
Cancer Immunol Immunother, 2018, 67(8):1305-1315. Epacadostat (INCB024360) purchased from Selleck.
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EMT6 cells were treated with miR-18a mimic or miR-18a plus INCB for 48 h; the protein levels were detected immunocytochemistry (n=3) and immunofluorescence (n=3) (B).
Mol Immunol, 2018, 103:144-155. 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 |
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Clinical Trial Information
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT03832673 | Not yet recruiting | Muscle-invasive Bladder Cancer | Fondazione IRCCS Istituto Nazionale dei Tumori Milano | April 2019 | Phase 2 |
| NCT03532295 | Not yet recruiting | Glioma|Glioblastoma | Washington University School of Medicine|Incyte Corporation|Pfizer | April 30 2019 | Phase 1|Phase 2 |
| NCT03832673 | Not yet recruiting | Muscle-invasive Bladder Cancer | Fondazione IRCCS Istituto Nazionale dei Tumori Milano | April 2019 | Phase 2 |
| NCT03532295 | Not yet recruiting | Glioma|Glioblastoma | Washington University School of Medicine|Incyte Corporation|Pfizer | April 30 2019 | Phase 1|Phase 2 |
| NCT03471286 | Recruiting | Solid Tumor | Sidney Kimmel Comprehensive Cancer Center at Johns Hopkins|Incyte Corporation | April 2019 | Phase 1 |
| NCT03707457 | Not yet recruiting | Glioblastoma|Glioblastoma Multiforme | Sidney Kimmel Comprehensive Cancer Center at Johns Hopkins|Bristol-Myers Squibb | April 2019 | 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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