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INCB 024360
- Epacadostat
- Soluble in DMSO
- MF: C11H13BrFN7O4S
- MW: 438.23
Description
INCB 024360 is a potent competitive indoleamine 2,3-dioxygenase 1 (IDO1) inhibitor with an in vitro IC50 value of 72 nM.
IDO1 converts tryptophan into kynurenine and contributes to immune suppression in tumors. INCB 024360 (Epacadostat) is useful for studying kynurenine pathway inhibition, tumor immunology and pharmacodynamic biomarker responses.
Key Features
- Competitive inhibitor of IDO1
- IC50: 72 nM in vitro
- Reduces kynurenine pathway activity in reported models
- Relevant to cancer immunotherapy research
Applications
- IDO1 enzyme assays
- Kynurenine pathway studies
- Tumor immune evasion models
- Immuno-oncology pharmacodynamic research
Note: An analog of INCB 024360 is available as Axon 2215.
More Information
| Parent CAS No. | 1204669-58-8 |
|---|---|
| Chemical Name | (Z)-N-(3-bromo-4-fluorophenyl)-N'-hydroxy-4-(2-(sulfamoylamino)ethylamino)-1,2,5-oxadiazole-3-carboximidamide |
| SMILES | C1(F)C=CC(N/C(=NO)/C2C(NCCNS(=O)(N)=O)=NON=2)=CC=1Br |
| MFCD | N.A. |
| InChi | InChI=1S/C11H13BrFN7O4S/c12-7-5-6(1-2-8(7)13)17-11(18-21)9-10(20-24-19-9)15-3-4-16-25(14,22)23/h1-2,5,16,21H,3-4H2,(H,15,20)(H,17,18)(H2,14,22,23) |
| InChiKey | FBKMWOJEPMPVTQ-UHFFFAOYSA-N |
| CID | 135564890 |
| Short Description | IDO1 inhibitor |
References
- C. Sheridan. IDO inhibitors move center stage in immuno-oncology. Nat Biotechnol. 2015 Apr;33(4):321-2.
- U.F. Röhrig et al. Challenges in the Discovery of Indoleamine 2,3-Dioxygenase 1 (IDO1) Inhibitors. J Med Chem. 2015 May 26.
- X. Liu et al. Selective inhibition of IDO1 effectively regulates mediators of antitumor immunity. Blood. 2010 Apr 29;115(17):3520-30.
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