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Epacadostat

Catalog No. T3548 CAS 1204669-58-8

Synonyms: INCB 024360, IDO Inhibitor 1

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.

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Epacadostat, CAS 1204669-58-8

Pack Size	Availability	Price/USD
5 mg	In stock	$ 39.00
10 mg	In stock	$ 64.00
25 mg	In stock	$ 89.00
50 mg	In stock	$ 113.00
100 mg	In stock	$ 197.00
200 mg	In stock	$ 328.00
500 mg	In stock	$ 553.00
1 g	In stock	$ 796.00
2 g	In stock	$ 1,090.00
1 mL * 10 mM (in DMSO)	In stock	$ 43.00

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Purity: 100%

Purity: 99.92%

Purity: 99.74%

Purity: 98.56%

Purity: 98.08%

Purity: 98%

Biological Description

Chemical Properties

Storage & Solubility Information

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].

Synonyms	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

Solubility Information

Ethanol: 53 mg/mL (120.94 mM)

DMSO: 79 mg/mL(180.8 mM)

References and Literature

1. Liu X, et al. Blood. 2010, 115(17), 3520-3530. 2. Koblish HK, et al. Mol Cancer Ther. 2010, 9(2), 489-498.

Citations

1. Nguyen D J M, Theodoropoulos G, Li Y Y, et al. Targeting the kynurenine pathway for the treatment of cisplatin resistant lung cancer. Molecular Cancer Research. 2019: molcanres. 0239.2019

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Active Compound Library Anti-Cancer Clinical Compound Library Anti-Cancer Drug Library Inhibitor Library Drug Repurposing Compound Library Anti-Cancer Metabolism Compound Library Bioactive Compounds Library Max Bioactive Compound Library Anti-Metabolism Disease Compound Library Metabolism Compound Library

Related Products

Related compounds with same targets

IACS-8968 IDO-IN-8 PF-06840003 IDO1-IN-5 IACS-8968 R-enantiomer IDO-IN-11 IDO-IN-5 BMS-986242

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Keywords

Epacadostat 1204669-58-8 Metabolism IDO Indoleamine 2,3-Dioxygenase (IDO) inhibit INCB024360 INCB-024360 Inhibitor INCB 024360 IDO Inhibitor 1 inhibitor

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