Epacadostat (INCB024360) analogue

Catalog No.S7587 Synonyms: INCB14943

For research use only.

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

Epacadostat (INCB024360) analogue Chemical Structure

CAS No. 914471-09-3

Selleck's Epacadostat (INCB024360) analogue has been cited by 1 Publication

Purity & Quality Control

Choose Selective IDO/TDO Inhibitors

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 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]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human HeLa cells M17iUmZ2dmO2aX;uJIF{e2G7 M{jOZWlvcGmkaYTpc44hd2ZiaX7kc4xm[W2rbnWgNkw{NWSrb4j5[4Vv[XOnIHnuJGlHVi2pYX3tZU1{fGmvdXzheIVlKGi3bXHuJGhmVGFiY3XscJMh[XO|ZYPz[YQh[XNia4nueZJmdmmwZTDmc5Ju[XSrb36gZpkhe3CnY4Tyc5Bpd3SxbXX0dpktKEmFNUC9NVkhdk1? MXmxPVUxPzh4Mh?=
mouse B16 cells MX;GeY5kfGmxbjDhd5NigQ>? NF7uUG5KdmirYnn0bY9vKG:oIHnu[I9t\WGvaX7lJFItOy2maX;4fYdmdmG|ZTDpckBud3W|ZTDCNVYh[2WubIOgZZN{\XO|ZXSgZZMhc3mwdYLlcolv\SCob4LtZZRqd25iYomgd5Bm[3S{b4Doc5RwdWW2comsJGlEPTB;NE[gcm0> M{jOdlE6PTB5OE[y
mouse P815B clone-6 cells Ml3LSpVv[3Srb36gZZN{[Xl? NIPKTGRKdmirYnn0bY9vKG:oIHj1cYFvKEmGT{GgeJJidnOoZXP0[YQhcW5ibX;1d4UhWDhzNVKgZ4xwdmVvNjDj[YxteyCkeTDIVGxEKGGwYXz5d4l{NCCLQ{WwQVYxKG6P Mnz6NlI3OTZ7MEK=
P815 clone 6 cells NX7qXFh1TnWwY4Tpc44h[XO|YYm= M2jmfGlvcGmkaYTpc44hd2ZibX;1d4UhUUSRMTDpckBRQDF3IHPsc45mKDZiY3XscJMh[nliSGDMR{BidmGueYPpd{whUUN3ME2wMlEh|ryP M2TaN|IzPjF4OUCy
HEK293 clone 6 cells MUTGeY5kfGmxbjDhd5NigQ>? M2\2dmlvcGmkaYTpc44hd2ZiaIXtZY4hUUSRMTD0doFve2[nY4Tl[EBqdiCKRVuyPVMh[2yxbnWgOkBk\WyuczDifUBJWEyFIHHuZYx6e2m| NIfaT5AzOjZzNkmwNi=>
Assay
Methods Test Index PMID
Western blot NMNAT2 28266613
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]

Protocol (from reference)

Animal Research:

[1]

  • Animal Models: Mice bearing GM-CSF-secreting B16 tumors
  • Dosages: 75 mg/kg b.i.d
  • Administration: s.c.

Solubility (25°C)

In vitro

In vivo

Add solvents to the product individually and in order
(Data is from Selleck tests instead of citations):
5% DMSO+45% PEG 300+ddH2O
For best results, use promptly after mixing.

22mg/mL

Chemical Information

Molecular Weight 271.64
Formula

C9H7ClFN5O2

CAS No. 914471-09-3
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles C1=CC(=C(C=C1N=C(C2=NON=C2N)NO)Cl)F

In vivo Formulation Calculator (Clear solution)

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

mg/kg g μL

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.

Molarity Calculator

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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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