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Epacadostat

Epacadostat
Epacadostat (INCB 024360) is an oral, potent and selective IDO1 inhibitor with IC50 value of 71.8 nM.
Catalog No. T3548Cas No. 1204669-58-8
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Purity:100%
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Epacadostat

Catalog No. T3548Cas No. 1204669-58-8

Epacadostat (INCB 024360) is an oral, potent and selective IDO1 inhibitor with IC50 value of 71.8 nM.
All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.
Pack SizePriceAvailabilityQuantity
5 mg$39In Stock
10 mg$64In Stock
25 mg$89In Stock
50 mg$113In Stock
100 mg$197In Stock
200 mg$328In Stock
500 mg$553In Stock
1 g$796In Stock
2 g$1,090In Stock
1 mL x 10 mM (in DMSO)$43In Stock
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Product Introduction

Bioactivity
Description
Epacadostat (INCB 024360) is an oral, potent and selective IDO1 inhibitor with IC50 value of 71.8 nM.
Targets&IC50
IDO1:10 nM
In vitro
METHODS: Epacadostat (INCB 024360) (0.0001, 0.01, 1, 100, 10000nM) was used to treat SKOV-3 cells and the release of kynurenine was measured.
RESULTS Epacadostat (INCB 024360) inhibited the catalytic activity of IDO1 with an IC50 value of 17.63 nM ± 2.26 (pIC50 = 7.76 ± 0.06). [2]
In vivo
METHODS: Mice were injected subcutaneously with 200 μl TC-1 cells on the back. After the tumor was palpable, Epacadostat (INCB 024360) (50 mg/kg), IFN-γ (100 ng/mouse), and kynurenine (100 mg/kg) were injected intraperitoneally every day. Tumor volume was measured every 3 days.
RESULTS Intraperitoneal injection of Epacadostat (INCB 024360) caused a significant increase in tumor volume and tumor weight, and inhibited the expression of CD80 on macrophages in tumor tissues. [3]
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].
AliasINCB 024360, IDO Inhibitor 1
Chemical Properties
Molecular Weight438.23
FormulaC11H13BrFN7O4S
Cas No.1204669-58-8
Storage & Solubility Information
StoragePowder: -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
1mg5mg10mg50mg
1 mM2.2819 mL11.4095 mL22.8191 mL114.0953 mL
5 mM0.4564 mL2.2819 mL4.5638 mL22.8191 mL
10 mM0.2282 mL1.1410 mL2.2819 mL11.4095 mL
20 mM0.1141 mL0.5705 mL1.1410 mL5.7048 mL
50 mM0.0456 mL0.2282 mL0.4564 mL2.2819 mL
100 mM0.0228 mL0.1141 mL0.2282 mL1.1410 mL

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