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Pack Size | Price | Availability | Quantity |
---|---|---|---|
5 mg | $39 | In Stock | |
10 mg | $64 | In Stock | |
25 mg | $89 | In Stock | |
50 mg | $113 | In Stock | |
100 mg | $197 | In Stock | |
200 mg | $328 | In Stock | |
500 mg | $553 | In Stock | |
1 g | $796 | In Stock | |
2 g | $1,090 | In Stock | |
1 mL x 10 mM (in DMSO) | $43 | In Stock |
Description | Epacadostat (INCB 024360) is an oral-available inhibitor of indoleamine 2, 3-dioxygenase (IDO1), increasing the proliferation and activation of various immune cells and reducing tumor-associated regulatory T cells. |
Targets&IC50 | IDO1:10 nM |
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] |
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] |
Cell Research | INCB 024360 (INCB024360) is dissolved in DMSO and stored, and then diluted with appropriate media before use[1]. To determine INCB 024360 activity against IDO in recombinant cells, HEK293/MSR cells are transiently transfected with full-length human or mouse IDO1, or mouse IDO2 cDNA, with Transit-293 transfection reagent or Lipofectamine 2000 reagents. INCB 024360 at different concentrations is added to the recovered transfected cells seeded at 2×104 cells per well in a 96-well plate (200 μL/well). The cells are incubated for 2 days, and kyn in the supernatants is measured as described in the HeLa cell assay. The tryptophan 2,3-dioxygenase (TDO) assay is performed similarly with HEK293/MSR cells transfected with a human TDO expression vector[1]. |
Alias | INCB 024360, IDO Inhibitor 1 |
Molecular Weight | 438.23 |
Formula | C11H13BrFN7O4S |
Cas No. | 1204669-58-8 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | Ethanol: 53 mg/mL (120.94 mM) DMSO: 50 mg/mL (114.1 mM) | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO/Ethanol
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