Name | Epacadostat |
Synonyms | INCN024360 Epacadostat INCB-24360(INCB-024360) Epacadostat(INCB024360) Epacadostat(INCN024360) 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 |
CAS | 1204669-58-8 |
Molecular Formula | C11H13BrFN7O4S |
Molar Mass | 438.2328 |
Density | 2.01±0.1 g/cm3(Predicted) |
Melting Point | 159 - 161°C |
Boling Point | 700.9±70.0 °C(Predicted) |
Water Solubility | Soluble in DMSO (up to at least 25 mg/ml) |
Solubility | DMSO: ≥ 31 mg/mL |
Appearance | Morphological solid color White |
pKa | 7.65±0.69(Predicted) |
Storage Condition | -20°C |
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. |
Use | Epacadostat (INCB024360) is a potent selective indoleamine 2, 3-dioxygenase (IDO1) inhibitor with an IC50 of 10 nM. Its selectivity for IDO1 is higher than other related enzymes such as IDO2 or TDO. Icadostadine INCB-24360 can be used in analytical chemistry for content determination, identification, pharmacological experiments, etc. Epacadostat (INCB024360) is a potent selective indoleamine 2, 3-dioxygenase (IDO1) inhibitor with an IC50 of 10 nM. Its selectivity for IDO1 is higher than other related enzymes such as IDO2 or TDO. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.282 ml | 11.409 ml | 22.819 ml |
5 mM | 0.456 ml | 2.282 ml | 4.564 ml |
10 mM | 0.228 ml | 1.141 ml | 2.282 ml |
5 mM | 0.046 ml | 0.228 ml | 0.456 ml |
Target | Value |
IDO1 (immune cells) |
10 nM |
In vitro studies
In IFN-& gamma;-treated human HeLa cells, INCB024360 effectively inhibited canine urea production. INCB024360 also promotes the growth of T and natural killer (NK) cells, increases IFN-& gamma; production, and reduces conversion to regulatory T (T(reg))-like cells.
In vivo study INCB024360 (100 mg/kg, p.o.), inhibited kyn production and tumor growth in immunocompetent mice by IDO1 inhibition, but was ineffective in immunodeficient mice. In mice loaded with CT26 colon cancer, INCB024360 (100 mg/kg, p.o.) also inhibited the growth of IDO-expressing tumors by reducing canine urea.