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Epacadostat (INCB024360) analogue IDO/TDO inhibitor

Name: Epacadostat (INCB024360) analogue
Brand: Selleck Chemicals
SKU: S7587
Availability: InStock
Rating: 5 (3 reviews)

Cat.No.S7587

Epacadostat (INCB024360) analogue (INCB14943) is a potent, competitive IDO1 (indoleamine-(2,3)-dioxygenase) inhibitor with IC50 of 67 nM.

Chemical Structure

Molecular Weight: 271.64

Jump to Mechanism of Action Cell Culture & Working Concentration Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: Purity: 100.00%

100.00

Related Targets	P450 (e.g. CYP17) Dehydrogenase PDE phosphatase PPAR HSP (HSP90) Vitamin Transferase Carbohydrate Metabolism Mitochondrial Metabolism Casein Kinase Serine/threonin kinase Lipoxygenase Phospholipase (e.g. PLA) Retinoid Receptor DPP ACE Peroxidases Fatty Acid Synthase FXR HMG-CoA Reductase Carbonic Anhydrase Lipase Decarboxylase DHFR Hydroxylase PCSK9 OXPHOS ROR Acyltransferase
Related Products	Epacadostat (INCB024360) IDO-IN-2 Indoximod Navoximod Linrodostat (BMS-986205) PF-06840003 LM10 IDO inhibitor 1 680C91

Cell Culture, Treatment & Working Concentration

Cell Lines	Assay Type	Activity Description
human HeLa cells	Function assay	Inhibition of indoleamine 2,3-dioxygenase in IFN-gamma-stimulated human HeLa cells assessed as kynurenine formation by spectrophotometry, IC50=19 nM
mouse B16 cells	Function assay	Inhibition of indoleamine 2,3-dioxygenase in mouse B16 cells assessed as kynurenine formation by spectrophotometry, IC50=46 nM
mouse P815B clone-6 cells	Function assay	Inhibition of human IDO1 transfected in mouse P815B clone-6 cells by HPLC analysis, IC50=60 nM
P815 clone 6 cells	Function assay	Inhibition of mouse IDO1 in P815 clone 6 cells by HPLC analysis, IC50=0.1 μM
HEK293 clone 6 cells	Function assay	Inhibition of human IDO1 transfected in HEK293 clone 6 cells by HPLC analysis
Click to View More Cell Line Experimental Data

Chemical Information, Storage & Stability

Molecular Weight	271.64	Formula	C₉H₇ClFN₅O₂	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	914471-09-3	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	INCB14943			Smiles	C1=CC(=C(C=C1N=C(C2=NON=C2N)NO)Cl)F

Solubility

In vitro
Batch:

DMSO : 54 mg/mL ( (198.79 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 54 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
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.
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.

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.

Mechanism of Action

Targets/IC₅₀/Ki	IDO1 ^[1] (Cell-free assay) 67 nM
In vitro	In HeLa cells, INCB024360 shows higher inhibitory activity on IDO1 with IC50 of 19 nM. ^[1] In coculture systems of human allogeneic lymphocytes with dendritic cells or tumor cells, INCB024360, via IDO1 inhibition, reverses T-cell suppression mediated by IDO-expressing HeLa cells or DCs, and increases the proliferation and functional activity of CD4+ T cells, CD8+ T cells, and NK cells. ^[2]
In vivo	In mice bearing GM-CSF-secreting B16 tumors, INCB024360 (75 mg/kg b.i.d) causes dose dependent inhibition of tumor growth. ^[1] INCB024360 significantly suppresses tumor growth in immunocompetent, but not immunodeficient, mice. ^[2]
References	https://pubmed.ncbi.nlm.nih.gov/19507862/ https://pubmed.ncbi.nlm.nih.gov/20197554/

Applications

Methods	Biomarkers	Images	PMID
Western blot	NMNAT2		28266613

Tech Support

Handling Instructions

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