Home Metabolism IDO/TDO inhibitor Epacadostat (INCB024360) For research use only.

Epacadostat (INCB024360)

Epacadostat (INCB024360) is a potent and selective indoleamine 2,3-dioxygenase (IDO1) inhibitor with IC50 of 10 nM and displays high selectivity over other related enzymes such as IDO2 or tryptophan 2,3-dioxygenase (TDO).

Epacadostat (INCB024360) Chemical Structure

Epacadostat (INCB024360) Chemical Structure

CAS: 1204669-58-8

Selleck's Epacadostat (INCB024360) has been cited by 48 publications

Purity & Quality Control

Batch: Purity: 99.82%
99.82

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Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
SKOV-3 cells Function assay IDO inhibition, IC50~15.3 nM 30112109
Jurkat Cell viability assay 72 h reduced the number of viable cells, IC50 = 50 μM 30112109
OCI-AML2 Function assay Inhibition of IDO1 in IFNgamma-stimulated human OCI-AML2 cells assessed as reduction in kynurenine production, IC50 = 0.0034 μM. 29220788
HeLa Function assay 48 hrs Inhibition of IFN-gamma-stimulated IDO1 activity in human HeLa cells using L-tryptophan as substrate after 48 hrs by microplate reader analysis, IC50 = 0.0071 μM. 25970480
HeLa Function assay 48 hrs Inhibition of IDO1 in IFN-gamma-stimulated human HeLa cells assessed as decrease in kynurenine levels after 48 hrs, IC50 = 0.0074 μM. 28523098
HEK293 Function assay 30 mins Inhibition of human IDO1 expressed in HEK293 cells assessed as reduction in kynurenine production after 30 mins, EC50 = 0.00874 μM. 29456801
T-cells Function assay 2 days Inhibition of IDO1 in IFNgamma and LPS-stimulated human dendritic cells co-cultured with human T cells assessed as inhibition of T-cell proliferation in presence of soluble anti-CD3 antibody and human recombinant IL-2 incubated for 2 days, IC50 = 0.013 μM. 29220788
HEK293/MSR Function assay Inhibition of human IDO1 expressed in HEK293/MSR cells assessed as reduction in kynurenine production incubated fro 2 days, IC50 = 0.015 μM. 29220788
THP1 Function assay Inhibition of IDO1 in IFNgamma-stimulated human THP1 cells assessed as reduction in kynurenine productio by spectrophotometric analysis, IC50 = 0.023 μM. 29220788
Click to View More Cell Line Experimental Data

Biological Activity

Description Epacadostat (INCB024360) is a potent and selective indoleamine 2,3-dioxygenase (IDO1) inhibitor with IC50 of 10 nM and displays high selectivity over other related enzymes such as IDO2 or tryptophan 2,3-dioxygenase (TDO).
Targets
IDO1 [1]
(immune cells)
10 nM
In vitro
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]
Kinase Assay IDO enzyme assays
Human IDO with an N-terminal His tag is expressed in E.coli and purified to homogeneity. IDO catalyzes the oxidative cleavage of the pyrrole ring of the indole nucleus of tryptophan to yield N’-formylkynurenine. The assays are performed at room temperature using 20 nM IDO and 2 mM D-Trp in the presence of 20 mM ascorbate, 3.5 µM methylene blue and 0.2 mg/mL catalase in 50 mM potassium phosphate buffer (pH 6.5). The initial reaction rates are recorded by continuously following the absorbance increase at 321 nm due to the formation of N’-formlylkynurenine.
Cell Research Cell lines Jurkat cells
Concentrations 50 μM
Incubation Time 72 h
Method

Jurkat cells were incubated with serially diluted epacadostat for 72 h. Their viability was measured and analyzed as percentage of the non-treated control.
In Vivo
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]
Animal Research Animal Models Female C57BL/6 or Balb/c nu/nu mice bearing PAN02 pancreatic tumors
Dosages ~100 mg/kg, twice a day
Administration p.o.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03589651 Completed Unresectable or Metastatic Solid Tumors Incyte Corporation August 17 2018 Phase 1
NCT03361228 Terminated Solid Tumors Incyte Corporation March 1 2018 Phase 1|Phase 2

Chemical lnformation & Solubility

Molecular Weight 438.23 Formula

C11H13BrFN7O4S
CAS No. 1204669-58-8 SDF Download Epacadostat (INCB024360) SDF
Smiles C1=CC(=C(C=C1N=C(C2=NON=C2NCCNS(=O)(=O)N)NO)Br)F
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 88 mg/mL ( (200.8 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 44 mg/mL

Water : Insoluble


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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