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Epacadostat (INCB024360)

Name: Epacadostat (INCB024360)
Brand: Selleck Chemicals
SKU: S7910
Rating: 5 (56 reviews)

Catalog No.S7910 Purity:99.82%

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

CAS No. 1204669-58-8

Purity & Quality Control

Batch: Purity: 99.82%

99.82

Epacadostat (INCB024360) Related Products

Related Targets	TDO IDO	Click to Expand
Related Products	IDO-IN-2 Indoximod Navoximod Linrodostat (BMS-986205) PF-06840003 LM10 IDO inhibitor 1 Epacadostat (INCB024360) analogue 680C91	Click to Expand
Related Compound Libraries	Metabolism Compound Library Anti-cancer Metabolism Compound Library Glutamine Metabolism Compound Library Carbohydrate Metabolism Compound Library Lipid Metabolism Compound Library	Click to Expand

Cell Data

Cell Lines	Assay Type	Incubation Time	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

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
Kinase Assay	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
Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2024-05-22)
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

References

Chemical Information & 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)	3 years-20°Cpowder	Storage of Stock Solutions Aliquot the stock solutions to avoid repeated freeze-thaw cycles	1 year-80°Cin solvent
Storage (From the date of receipt)	3 years-20°Cpowder		1 month-20°Cin solvent

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

Molecular Weight Calculator

In vivo Batch: Add solvents to the product individually and in order.				In vivo Formulation Calculator
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	1.625mg/ml (3.71mM)	Taking the 1 mL working solution as an example, add 50 μL of 32.5 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	4.350mg/ml (9.93mM)	Taking the 1 mL working solution as an example, add 50 μL 87 mg/ml clarified DMSO stock solution to 400 μL PEG300, mix evenly to clarify it; add 50 μL Tween80 to the above system, mix evenly to clarify it; then continue to add 500 μL ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

Preparing Stock Solutions

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
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Dilution Calculator Molecular Weight Calculator

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

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

Tel: +1-832-582-8158 Ext:3
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