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INCB 024360
- Epacadostat
- Soluble in DMSO
- MF: C11H13BrFN7O4S
- MW: 438.23
Description
Potent competitive inhibitor of indoleamine 2,3-dioxygenase (IDO1, IC50 value 72 nM in vitro) with in vivo pharmacodynamic activity and efficacy in a mouse melanoma model; INCB024360 (Epacadostat) decreased kynurenine levels by >50% in plasma and inhibited B16-GM-CSF tumor growth in a dose dependent fashion.
An analog of INCB 024360 (Axon 2215) is available as well.
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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