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Epacadostat

Name: Epacadostat
Brand: TargetMol
SKU: T3548
Price: 39 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T3548Cas No. 1204669-58-8

Alias INCB 024360, IDO Inhibitor 1

Epacadostat (INCB 024360) is an oral, potent and selective IDO1 inhibitor with IC50 value of 71.8 nM.

Epacadostat

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Purity: 99.93%

Catalog No. T3548Alias INCB 024360, IDO Inhibitor 1Cas No. 1204669-58-8

Epacadostat (INCB 024360) is an oral, potent and selective IDO1 inhibitor with IC50 value of 71.8 nM.

Pack Size	Price	USA Warehouse	Global Warehouse
5 mg	$39	In Stock	In Stock
10 mg	$64	In Stock	In Stock
25 mg	$89	In Stock	In Stock
50 mg	$113	In Stock	In Stock
100 mg	$197	In Stock	In Stock
200 mg	$328	In Stock	In Stock
500 mg	$553	In Stock	In Stock
1 g	$796	-	In Stock
2 g	$1,090	-	In Stock
1 mL x 10 mM (in DMSO)	$43	In Stock	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

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.

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Purity:99.93%

Color:White

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COA LCMS HNMR

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 (HeLa cells):7.4 nM, IDO1:10 nM, IDO1 (P1.HTR cells):54.46 nM ± 11.18 nM, IDO1 (HEK293 cells):52.4 nM ± 15.7 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].
Synonyms	INCB 024360, IDO Inhibitor 1

Chemical Properties

Molecular Weight	438.23
Formula	C₁₁H₁₃BrFN₇O₄S
Cas No.	1204669-58-8
Smiles	NS(=O)(=O)NCCNc1nonc1\C(Nc1ccc(F)c(Br)c1)=N\O
Relative Density.	2.01 g/cm3 (Predicted)

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

Ethanol: 53 mg/mL (120.94 mM), Sonication is recommended.

DMSO: 250 mg/mL (570.48 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 5 mg/mL (11.41 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

Ethanol/DMSO

	1mg	5mg	10mg	50mg
1 mM	2.2819 mL	11.4095 mL	22.8191 mL	114.0953 mL
5 mM	0.4564 mL	2.2819 mL	4.5638 mL	22.8191 mL
10 mM	0.2282 mL	1.1410 mL	2.2819 mL	11.4095 mL
20 mM	0.1141 mL	0.5705 mL	1.1410 mL	5.7048 mL
50 mM	0.0456 mL	0.2282 mL	0.4564 mL	2.2819 mL
100 mM	0.0228 mL	0.1141 mL	0.2282 mL	1.1410 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc