Epacadostat (Synonyms: INCB 024360)

Name: Epacadostat
Brand: MedChemExpress
SKU: HY-15689
Rating: 5.0 (20 reviews)

Cat. No.: HY-15689 Purity: 99.66%: FAQs
Data Sheet SDS COA Handling Instructions Technical Support

Epacadostat (INCB 024360) is a potent and selective indoleamine 2,3-dioxigenase 1 (IDO1) inhibitor with an IC₅₀ of 71.8 nM.

For research use only. We do not sell to patients.

Epacadostat Chemical Structure

CAS No. : 1204669-58-8

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10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
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10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
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Customer Review

Based on 20 publication(s) in Google Scholar

Other Forms of Epacadostat:

Epacadostat (Standard) Get quote

19 Publications Citing Use of MCE Epacadostat

: Epacadostat purchased from MedChemExpress. Usage Cited in: Br J Pharmacol. 2018 Jul;175(14):3034-3049. [Abstract]; Western blot analysis of IDO1 protein levels for IFN-γ-stimulated HeLa cells that are treated with indicated compounds (e.g., Epacadostat).

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IDO1 IDO2 IDO

Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

Epacadostat (INCB 024360) is a potent and selective indoleamine 2,3-dioxigenase 1 (IDO1) inhibitor with an IC₅₀ of 71.8 nM^[1].

IC₅₀ & Target^[1]

IDO1

71.8 nM (IC₅₀)

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	> 100 μM Compound: 2; INCB024360	Antiproliferative activity against human A549 cells after 48 hrs by CCK-8 assay Antiproliferative activity against human A549 cells after 48 hrs by CCK-8 assay	[PMID: 29670692]
CT26	IC₅₀	> 100 μM Compound: 2; INCB024360	Antiproliferative activity against mouse CT26 cells after 48 hrs by CCK-8 assay Antiproliferative activity against mouse CT26 cells after 48 hrs by CCK-8 assay	[PMID: 29670692]
CT26	IC₅₀	> 100 μM Compound: 1	Cytotoxicity against mouse CT26 cells assessed as reduction in cell viability measured after 72 hrs by CCK8 assay Cytotoxicity against mouse CT26 cells assessed as reduction in cell viability measured after 72 hrs by CCK8 assay	[PMID: 33482599]
CT26	IC₅₀	47.09 μM Compound: Epacadostat	Cytotoxicity against mouse CT26 cells assessed as reduction in cell viability by CCK8 assay Cytotoxicity against mouse CT26 cells assessed as reduction in cell viability by CCK8 assay	[PMID: 34854662]
HCT-116	IC₅₀	> 100 μM Compound: 2; INCB024360	Antiproliferative activity against human HCT116 cells after 48 hrs by CCK-8 assay Antiproliferative activity against human HCT116 cells after 48 hrs by CCK-8 assay	[PMID: 29670692]
HCT-116	IC₅₀	> 50 μM Compound: Epacadostat	Cytotoxicity against human HCT-116 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay Cytotoxicity against human HCT-116 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay	[PMID: 34147748]
HCT-116	IC₅₀	37.1 μM Compound: Epacadostat	Cytotoxicity against human HCT-116 cells assessed as reduction in cell viability by CCK8 assay Cytotoxicity against human HCT-116 cells assessed as reduction in cell viability by CCK8 assay	[PMID: 34854662]
HEK293	IC₅₀	0.242 μM Compound: INCB024360	Inhibition of TDO (unknown origin) expressed in HEK293 cells using L-Trp as substrate after 8 hrs Inhibition of TDO (unknown origin) expressed in HEK293 cells using L-Trp as substrate after 8 hrs	[PMID: 30321802]
HEK293	IC₅₀	0.26 μM Compound: INCB24360	Inhibition of human TDO transfected in HEK293 cells assessed as reduction in kynurenine production using L-tryptophan as substrate incubated for 12 hrs Inhibition of human TDO transfected in HEK293 cells assessed as reduction in kynurenine production using L-tryptophan as substrate incubated for 12 hrs	[PMID: 31580660]
HEK293	IC₅₀	12.6 nM Compound: 1	Inhibition of recombinant human IDO1 expressed in HEK293 cells assessed as N-formylkynurenine formation by measuring kynurenine level incubated for 12 hrs by microplate reader analysis Inhibition of recombinant human IDO1 expressed in HEK293 cells assessed as N-formylkynurenine formation by measuring kynurenine level incubated for 12 hrs by microplate reader analysis	[PMID: 31233921]
HeLa	IC₅₀	> 100 μM Compound: 1	Cytotoxicity against human HeLa cells assessed as reduction in cell viability measured after 72 hrs by CCK8 assay Cytotoxicity against human HeLa cells assessed as reduction in cell viability measured after 72 hrs by CCK8 assay	[PMID: 33482599]
HeLa	IC₅₀	0.007 μM Compound: INCB24360	Inhibition of IDO1 in IFN-gamma stimulated human HeLa cells assessed as reduction in kynurenine production incubated for 18 hrs Inhibition of IDO1 in IFN-gamma stimulated human HeLa cells assessed as reduction in kynurenine production incubated for 18 hrs	[PMID: 31580660]
HeLa	IC₅₀	0.016 μM Compound: Epacadostat	Inhibition of IDO1 in IFN-gamma stimulated human HeLa cells assessed as reduction in kynurenine production using L-tryptophan as substrate incubated for 24 hrs Inhibition of IDO1 in IFN-gamma stimulated human HeLa cells assessed as reduction in kynurenine production using L-tryptophan as substrate incubated for 24 hrs	[PMID: 31610376]
HeLa	IC₅₀	0.07 μM Compound: INCB24360	Inhibition of IDO1 in human HeLa cells using L-tryptophan as substrate after 20 hrs Inhibition of IDO1 in human HeLa cells using L-tryptophan as substrate after 20 hrs	[PMID: 30469041]
HeLa	IC₅₀	10 nM Compound: 1; INCB24360	Inhibition of IDO1 in human HeLa cells using L-tryptophan as substrate incubated for 48 hrs Inhibition of IDO1 in human HeLa cells using L-tryptophan as substrate incubated for 48 hrs	[PMID: 31445231]
HeLa	IC₅₀	10.3 nM Compound: INCB024360	Inhibition of IDO1 in IFN-gamma stimulated human HeLa cells assessed as reduction in kynurenine production incubated for 24 hrs relative to control Inhibition of IDO1 in IFN-gamma stimulated human HeLa cells assessed as reduction in kynurenine production incubated for 24 hrs relative to control	[PMID: 30858027]
HeLa	IC₅₀	12.5 nM Compound: Epacadostat	Inhibition of IDO1 in IFN-gamma stimulated human HeLa cells using L-tryptophan as substrate incubated for 48 hrs by fluorescence assay Inhibition of IDO1 in IFN-gamma stimulated human HeLa cells using L-tryptophan as substrate incubated for 48 hrs by fluorescence assay	[PMID: 32832022]
HeLa	IC₅₀	7.1 nM Compound: 1; INCB024360	Inhibition of IFN-gamma-stimulated IDO1 activity in human HeLa cells using L-tryptophan as substrate after 48 hrs by microplate reader analysis Inhibition of IFN-gamma-stimulated IDO1 activity in human HeLa cells using L-tryptophan as substrate after 48 hrs by microplate reader analysis	[PMID: 25970480]
HeLa	IC₅₀	7.1 nM Compound: INCB24360	Inhibition of IFN-gamma stimulated IDO1 in human HeLa cells assessed as reduction in formation of kynurenine incubated for 48 hrs in presence of IFNgamma by microplate reader assay Inhibition of IFN-gamma stimulated IDO1 in human HeLa cells assessed as reduction in formation of kynurenine incubated for 48 hrs in presence of IFNgamma by microplate reader assay	[PMID: 31580660]
HeLa	IC₅₀	7.4 nM Compound: 4f; INCB24360	Inhibition of IDO1 in IFN-gamma-stimulated human HeLa cells assessed as decrease in kynurenine levels after 48 hrs Inhibition of IDO1 in IFN-gamma-stimulated human HeLa cells assessed as decrease in kynurenine levels after 48 hrs	[PMID: 28523098]
HeLa	EC₅₀	8 nM Compound: Epacadostat	Inhibition of IDO1 in IFN-gamma stimulated human HeLa cells assessed as reduction in kynurenine formation using L-tryptophan as substrate incubated for 24 hrs by UV-spectrophotometry Inhibition of IDO1 in IFN-gamma stimulated human HeLa cells assessed as reduction in kynurenine formation using L-tryptophan as substrate incubated for 24 hrs by UV-spectrophotometry	[PMID: 32088128]
HepG2	IC₅₀	> 50 μM Compound: Epacadostat	Cytotoxicity against human HepG2 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay Cytotoxicity against human HepG2 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay	[PMID: 34147748]
HGC-27	IC₅₀	> 50 μM Compound: Epacadostat	Cytotoxicity against human HGC-27 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay Cytotoxicity against human HGC-27 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay	[PMID: 34147748]
HT-29	IC₅₀	> 100 μM Compound: 2; INCB024360	Antiproliferative activity against human HT-29 cells after 48 hrs by CCK-8 assay Antiproliferative activity against human HT-29 cells after 48 hrs by CCK-8 assay	[PMID: 29670692]
HT-29	IC₅₀	62.96 μM Compound: Epacadostat	Cytotoxicity against human HT-29 cells assessed as reduction in cell viability by CCK8 assay Cytotoxicity against human HT-29 cells assessed as reduction in cell viability by CCK8 assay	[PMID: 34854662]
Lewis lung carcinoma cell line	IC₅₀	> 100 μM Compound: 2; INCB024360	Antiproliferative activity against mouse LLC cells after 48 hrs by CCK-8 assay Antiproliferative activity against mouse LLC cells after 48 hrs by CCK-8 assay	[PMID: 29670692]
MCF7	IC₅₀	> 50 μM Compound: Epacadostat	Cytotoxicity against human MCF7 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay Cytotoxicity against human MCF7 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay	[PMID: 34147748]
THP-1	IC₅₀	5.6 nM Compound: INCB024360	Inhibition of IDO1 in IFN-gamma/LPS stimulated human THP-1 cells assessed as reduction in kynurenine production after 24 hrs Inhibition of IDO1 in IFN-gamma/LPS stimulated human THP-1 cells assessed as reduction in kynurenine production after 24 hrs	[PMID: 30858027]
U-87MG ATCC	IC₅₀	> 50 μM Compound: Epacadostat	Cytotoxicity against human U87 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay Cytotoxicity against human U87 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay	[PMID: 34147748]
U-87MG ATCC	IC₅₀	0.26 μM Compound: INCB024360	Inhibition of TDO in human U87 MG cells using L-Trp as substrate after 8 hrs Inhibition of TDO in human U87 MG cells using L-Trp as substrate after 8 hrs	[PMID: 30321802]

In Vitro

In cellular assays, Epacadostat (INCB 024360) selectively inhibits human IDO1 with IC₅₀ values of approximately 10 nM, demonstrating little activity against other related enzymes such as IDO2 or tryptophan 2,3-dioxygenase (TDO). Epacadostat (INCB 024360) also exhibits significant activity toward mouse IDO1, with an IC₅₀ value of 52.4 nM±15.7 nM, in a similar assay using mouse IDO1-transfected HEK293/MSR cells^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Female Balb/c mice bearing CT26 tumors are treated orally twice daily for 12 d with Epacadostat at 100 mg/kg. Epacadostat (INCB 024360) suppresses kynurenine equivalently in plasma, tumors, and lymph nodes. In na ve C57BL/6 mice, 50 mg/kg Epacadostat (INCB 024360) decreases plasma kynurenine levels within 1 hour and those levels stay at least 50% suppressed through the 8-hour time course^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

Molecular Weight

438.23

Formula

C₁₁H₁₃BrFN₇O₄S

CAS No.

1204669-58-8

Appearance

Solid

Color

White to gray

SMILES

BrC1=C(F)C=CC(N/C(C2=NON=C2NCCNS(N)(=O)=O)=N\O)=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (228.19 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.2819 mL	11.4095 mL	22.8191 mL
5 mM	0.4564 mL	2.2819 mL	4.5638 mL
10 mM	0.2282 mL	1.1410 mL	2.2819 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 5% DMSO 40% PEG300 5% Tween-80 50% Saline
Solubility: ≥ 2.62 mg/mL (5.98 mM); Clear solution
Protocol 2

Add each solvent one by one: 5% DMSO 95% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.62 mg/mL (5.98 mM); Clear solution
Protocol 3

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.70 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 4

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (5.70 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 5

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (5.70 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

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μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.66%

Select Batch:

Data Sheet (284 KB) SDS (394 KB)

COA (257 KB) LCMS (110 KB)

Handling Instructions (2659 KB)

References

[1]. Liu X, et al. Selective inhibition of IDO1 effectively regulates mediators of antitumor immunity. Blood. 2010 Apr 29;115(17):3520-30. [Content Brief]

[2]. Koblish HK, et al. Hydroxyamidine inhibitors of indoleamine-2,3-dioxygenase potently suppress systemic tryptophan catabolism and the growth of IDO-expressing tumors. Mol Cancer Ther. 2010 Feb;9(2):489-98. [Content Brief]

[3]. Fu R, et al. LW106, a novel indoleamine 2,3-dioxygenase 1 inhibitor, suppresses tumour progression by limiting stroma-immune crosstalk and cancer stem cell enrichment in tumour micro-environment. Br J Pharmacol. 2018 Jul;175(14):3034-3049. [Content Brief]

Cell Assay ^[1]	To determine Epacadostat 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. Epacadostat (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]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[2]	Mice^[2] The female C57BL/6 mice are dosed orally with 50 mg/kg Epacadostat. C57BL/6 wild-type or Ido1^-/--deficient mice are administered a single oral dose of Epacadostat (INCB 024360), at which point food is removed from the cages until after the 8-h time point. At various time points after dosing, mice are euthanized and blood is collected by cardiac puncture. Plasma is analyzed for the presence of Epacadostat (INCB 024360), tryptophan, and kynurenine according to the methods below. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References	[1]. Liu X, et al. Selective inhibition of IDO1 effectively regulates mediators of antitumor immunity. Blood. 2010 Apr 29;115(17):3520-30. [Content Brief] [2]. Koblish HK, et al. Hydroxyamidine inhibitors of indoleamine-2,3-dioxygenase potently suppress systemic tryptophan catabolism and the growth of IDO-expressing tumors. Mol Cancer Ther. 2010 Feb;9(2):489-98. [Content Brief] [3]. Fu R, et al. LW106, a novel indoleamine 2,3-dioxygenase 1 inhibitor, suppresses tumour progression by limiting stroma-immune crosstalk and cancer stem cell enrichment in tumour micro-environment. Br J Pharmacol. 2018 Jul;175(14):3034-3049. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.2819 mL	11.4095 mL	22.8191 mL	57.0477 mL
	5 mM	0.4564 mL	2.2819 mL	4.5638 mL	11.4095 mL
	10 mM	0.2282 mL	1.1410 mL	2.2819 mL	5.7048 mL
	15 mM	0.1521 mL	0.7606 mL	1.5213 mL	3.8032 mL
	20 mM	0.1141 mL	0.5705 mL	1.1410 mL	2.8524 mL
	25 mM	0.0913 mL	0.4564 mL	0.9128 mL	2.2819 mL
	30 mM	0.0761 mL	0.3803 mL	0.7606 mL	1.9016 mL
	40 mM	0.0570 mL	0.2852 mL	0.5705 mL	1.4262 mL
	50 mM	0.0456 mL	0.2282 mL	0.4564 mL	1.1410 mL
	60 mM	0.0380 mL	0.1902 mL	0.3803 mL	0.9508 mL
	80 mM	0.0285 mL	0.1426 mL	0.2852 mL	0.7131 mL
	100 mM	0.0228 mL	0.1141 mL	0.2282 mL	0.5705 mL

Epacadostat Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Epacadostat1204669-58-8INCB 024360INCB024360INCB-024360Indoleamine 2,3-Dioxygenase (IDO)Inhibitorinhibitorinhibit

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Epacadostat (Synonyms: INCB 024360)

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Epacadostat Related Antibodies

19 Publications Citing Use of MCE Epacadostat

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•Related Small Molecules:

•Related Proteins:

View All Indoleamine 2,3-Dioxygenase (IDO) Isoform Specific Products:

Biological Activity

Protocol

Purity & Documentation

References

Customer Review

Epacadostat Related Antibodies

Molarity Calculator

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Complete Stock Solution Preparation Table

Epacadostat Related Classifications

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