| Identification | Back Directory | [Name]
Epacadostat (INCB024360) | [CAS]
1204669-58-8 | [Synonyms]
CS-1617
INCB02436
INCN024360
Epacadostat
(1204669-37-3)
Epacadostat(INCN024360)
INCB-24360(INCB-024360)
Epacadostat(INCB024360)
INCB 024360 ， Epacadostat
IDO inhibitor(INCB024360)
INCB024360;INCB-024360;INCB 024360
Epacadostat (INCB24360, INCB024360)
N-(3-Bromo-4-fluoro-phenyl)-N'-hydroxy-4-[2-(sulfamoylamino)ethylamino]-1,2,5-oxadiazole-3-carboxamidine
(Z)-N-(3-bromo-4-fluorophenyl)-N'-hydroxy-4-[2-(sulfamoylamino)ethylamino]-1,2,5-oxadiazole-3-carboxamidine
(Z)-N-(3-bromo-4-fluorophenyl)-N'-hydroxy-4-((2-(sulfamoylamino)ethyl)amino)-1,2,5-oxadiazole-3-carboximidamide
[C(Z)]-4-[[2-[(Aminosulfonyl)amino]ethyl]amino]-N-(3-bromo-4-fluorophenyl)-N'-hydroxy-1,2,5-oxadiazole-3-carboximidamide
1,2,5-Oxadiazole-3-carboximidamide, 4-[[2-[(aminosulfonyl)amino]ethyl]amino]-N-(3-bromo-4-fluorophenyl)-N'-hydroxy-, [C(Z)]- | [Molecular Formula]
C11H13BrFN7O4S | [MDL Number]
MFCD26142934 | [MOL File]
1204669-58-8.mol | [Molecular Weight]
438.233 |
| Chemical Properties | Back Directory | [Melting point ]
159 - 161°C | [Boiling point ]
700.9±70.0 °C(Predicted) | [density ]
2.01±0.1 g/cm3(Predicted) | [storage temp. ]
-20°C | [solubility ]
Soluble in DMSO (up to at least 25 mg/ml) | [form ]
solid | [pka]
7.65±0.69(Predicted) | [color ]
White | [Stability:]
Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months. |
| Hazard Information | Back Directory | [Description]
Epacadostat is an inhibitor of indoleamine 2,3-dioxygenase 1 (IDO1) with an IC50 value of 7.1 nM in HeLa cells that demonstrates little activity against the related enzymes IDO2 or tryptophan 2,3-dioxygenase (TDO).1 It has been shown to promote T and natural killer-cell growth, to increase IFN-γ production, and to reduce conversion to regulatory T (Treg)-like cells in a coculture system of human allogeneic lymphocytes with either dendritic cells or tumor cells.1 Epacadostat can also inhibit tumor growth in tumor-bearing mice in a lymphocyte-dependent manner.1 | [Uses]
Epacadostat is a potent and novel indoleamine 2,3-dioxygenase (IDO1) inhibitor with IC50 of 10 nM. It has high selectivity over IDO2 and tryptophan 2,3-dioxygenase (TDO). | [target]
IDO1 | [References]
1) Liu?et al.?(2010),?Selective inhibition of IDO1 effectively regulates mediators of antitumor immunity;?Blood?115?3520
2) Koblish?et al.?(2010),?Hydroxyamidine Inhibitors of Indolamine-2,3-dioxygenase Potently Suppress Systemic Tryptophan Catabolism and the Growth of IDO-Expressing Tumors;?Mol. Cancer Ther.?9?489
3) Jochems?et al.?(2016),?The IDO1 selective inhibitor epacadostat enhances dendritic cell immunogenicity and lytic ability of tumor antigen-specific T cells;?Oncotarget?7?37762
4) Yentz and Smith (2018),?Indoleamine-2,3-dioxygenase Inhibition as a Strategy to Augment Cancer Immunotherapy;?BioDrugs?32?311
5) Zhu??et al.?(2019),?Indoleamine Dioxygenase Inhibitors: Clinical Rationale and Current Development;?Curr. Oncol. Rep.?21?2
6) Mitchell?et al.?(2018),?Epacadostat Plus Pembrolizumab in Patients with Advanced Solid Tumors: Phase I Results From a Multicenter, Open-Label Phase I/II Trial (ECHO-202/KEYNOTE-037);?J. Clin. Oncol.?36?3223 |
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