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

Epacadostat (INCB024360) analogue

Synonyms: INCB14943

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

Epacadostat (INCB024360) analogue Chemical Structure

Epacadostat (INCB024360) analogue Chemical Structure

CAS No. 914471-09-3

Purity & Quality Control

Epacadostat (INCB024360) analogue Related Products

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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 19507862
mouse B16 cells Function assay Inhibition of indoleamine 2,3-dioxygenase in mouse B16 cells assessed as kynurenine formation by spectrophotometry, IC50=46 nM 19507862
mouse P815B clone-6 cells Function assay Inhibition of human IDO1 transfected in mouse P815B clone-6 cells by HPLC analysis, IC50=60 nM 22616902
P815 clone 6 cells Function assay Inhibition of mouse IDO1 in P815 clone 6 cells by HPLC analysis, IC50=0.1 μM 22616902
HEK293 clone 6 cells Function assay Inhibition of human IDO1 transfected in HEK293 clone 6 cells by HPLC analysis 22616902
Click to View More Cell Line Experimental Data

Biological Activity

Description Epacadostat (INCB024360) analogue (INCB14943) is a potent, competitive IDO1 (indoleamine-(2,3)-dioxygenase) inhibitor with IC50 of 67 nM.
Targets
IDO1 [1]
(Cell-free assay)
67 nM
In vitro
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]
Experimental Result Images Methods Biomarkers Images PMID
Western blot NMNAT2 28266613
In Vivo
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]
Animal Research Animal Models Mice bearing GM-CSF-secreting B16 tumors
Dosages 75 mg/kg b.i.d
Administration s.c.

Chemical Information & Solubility

Molecular Weight 271.64 Formula

C9H7ClFN5O2
CAS No. 914471-09-3 SDF Download Epacadostat (INCB024360) analogue SDF
Smiles C1=CC(=C(C=C1N=C(C2=NON=C2N)NO)Cl)F
Storage (From the date of receipt)

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


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In vivo
Batch:

Add solvents to the product individually and in order.


In vivo Formulation Calculator

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In vivo Formulation Calculator (Clear solution)

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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
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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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