Home Metabolism IDO/TDO inhibitor Epacadostat (INCB024360)

Epacadostat (INCB024360)

Catalog No.S7910

For research use only.

Epacadostat (INCB024360) is a potent and selective indoleamine 2,3-dioxygenase (IDO1) inhibitor with IC50 of 10 nM and displays high selectivity over other related enzymes such as IDO2 or tryptophan 2,3-dioxygenase (TDO).

Epacadostat (INCB024360) Chemical Structure

CAS No. 1204669-58-8

Selleck's Epacadostat (INCB024360) has been cited by 34 publications

Purity & Quality Control

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Biological Activity

Description Epacadostat (INCB024360) is a potent and selective indoleamine 2,3-dioxygenase (IDO1) inhibitor with IC50 of 10 nM and displays high selectivity over other related enzymes such as IDO2 or tryptophan 2,3-dioxygenase (TDO).
Targets
IDO1 [1]
(immune cells)
10 nM
In vitro

In IFN-γ–treated human HeLa cells, INCB024360 potently inhibits kynurenine production. INCB024360 also promotes T and natural killer (NK)-cell growth, increases IFN-gamma production, and reduces conversion to regulatory T (T(reg))-like cells. [1]
Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
SKOV-3 cells MmezSpVv[3Srb36gZZN{[Xl? NIXiTWNKTE9iaX7obYJqfGmxbjygTWM2OH5zNT6zJI5O MWm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODFzMkGwPUc,OzBzMUKxNFk9N2F-
Jurkat NYPBcZZ7S2WubDD2bYFjcWyrdImgZZN{[Xl? NXPQTYc6PzJiaB?= NHv4SFhz\WS3Y3XkJJRp\SCwdX3i[ZIhd2ZidnnhZoxmKGOnbHzzMEBKSzVyIE2gOVAh|ryP NHft[Hc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEGxNlExQSd-M{CxNVIyODl:L3G+
OCI-AML2 MnXjSpVv[3Srb36gZZN{[Xl? MU\Jcohq[mm2aX;uJI9nKEmGT{GgbY4hUU[QZ3HtcYEue3SrbYXsZZRm\CCqdX3hckBQS0lvQV3MNkBk\WyuczDhd5Nme3OnZDDhd{Bz\WS3Y4Tpc44hcW5ia4nueZJmdmmwZTDwdo9lfWO2aX;uMEBKSzVyIE2gNE4xODN2IN88UU4> MoXZQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl{MkC3PFgoRjJ7MkKwO|g5RC:jPh?=
HeLa MV;GeY5kfGmxbjDhd5NigQ>? MV[0PEBpenN? M3;BcmlvcGmkaYTpc44hd2ZiSV\OMYdidW2jLYP0bY12dGG2ZXSgTWRQOSCjY4Tpeol1gSCrbjDoeY1idiCKZVzhJINmdGy|IIXzbY5oKExvdIL5dJRweGijbjDhd{B{fWK|dILheIUh[W[2ZYKgOFghcHK|IHL5JI1q[3KxcHzheIUhemWjZHXyJIFv[Wy7c3nzMEBKSzVyIE2gNE4xODdzIN88UU4> MU[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTl5MES4NEc,OjV7N{C0PFA9N2F-
HeLa M2DFOGZ2dmO2aX;uJIF{e2G7 NInKUow1QCCqcoO= NYH4RZhHUW6qaXLpeIlwdiCxZjDJSG8yKGmwIFnGUk1o[W2vYT3zeIlufWyjdHXkJIh2dWGwIFjlUIEh[2WubIOgZZN{\XO|ZXSgZZMh\GWlcnXhd4UhcW5ia4nueZJmdmmwZTDs[ZZmdHNiYX\0[ZIhPDhiaILzMEBKSzVyIE2gNE4xODd2IN88UU4> MkT0QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh3MkOwPVgoRjJ6NUKzNFk5RC:jPh?=
HEK293 MmLSSpVv[3Srb36gZZN{[Xl? MlvlN|AhdWmwcx?= NYfjR2dnUW6qaXLpeIlwdiCxZjDoeY1idiCLRF:xJIV5eHKnc4Pl[EBqdiCKRVuyPVMh[2WubIOgZZN{\XO|ZXSgZZMhemWmdXP0bY9vKGmwIHv5cpVz\W6rbnWgdJJw\HWldHnvckBi\nSncjCzNEBucW6|LDDFR|UxKD1iMD6wNFg4PCEQvF2u NYHxVVVoRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0OVY5ODFpPkK5OFU3QDBzPD;hQi=>
T-cells MlzoSpVv[3Srb36gZZN{[Xl? NHvtcpAzKGSjeYO= Mnq5TY5pcWKrdHnvckBw\iCLRF:xJIlvKEmITnfhcY1iKGGwZDDMVHMue3SrbYXsZZRm\CCqdX3hckBl\W6mcnn0bYMh[2WubIOgZ48u[3WudIXy[YQhf2m2aDDoeY1idiCWIHPlcIx{KGG|c3Xzd4VlKGG|IHnubIljcXSrb36gc4YhXC2lZXzsJJBzd2yrZnXyZZRqd25iaX6gdJJme2WwY3Wgc4Yhe2:udXLs[UBidnSrLVPEN{BidnSrYn;kfUBidmRiaIXtZY4hemWlb33ibY5idnRiSVytNkBqdmO3YnH0[YQh\m:{IEKg[IF6eyxiSVO1NEA:KDBwMEGzJO69VS5? MXG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTJ{MEe4PEc,Ojl{MkC3PFg9N2F-
HEK293/MSR M4rIbWZ2dmO2aX;uJIF{e2G7 NW\ZSHJwUW6qaXLpeIlwdiCxZjDoeY1idiCLRF:xJIV5eHKnc4Pl[EBqdiCKRVuyPVMwVVOUIHPlcIx{KGG|c3Xzd4VlKGG|IILl[JVkfGmxbjDpckBsgW63cnXubY5mKHC{b3T1Z5Rqd25iaX7jeYJifGWmIH\yc{AzKGSjeYOsJGlEPTBiPTCwMlAyPSEQvF2u NF\RXG49[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUKyNFc5QCd-MkmyNlA4QDh:L3G+
THP1 MlnVSpVv[3Srb36gZZN{[Xl? M{HZVmlvcGmkaYTpc44hd2ZiSVTPNUBqdiCLRl7nZY1u[S2|dHnteYxifGWmIHj1cYFvKFSKUEGgZ4VtdHNiYYPz[ZN{\WRiYYOgdoVlfWO2aX;uJIlvKGu7boXy[Y5qdmVicILv[JVkfGmxIHL5JJNx\WO2cn;wbI91d22ndILpZ{BidmGueYPpd{whUUN3MDC9JFAvODJ|IN88UU4> MV68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTJ{MEe4PEc,Ojl{MkC3PFg9N2F-
Click to View More Cell Line Experimental Data
In vivo INCB024360 (100 mg/kg, p.o.), via IDO1 inhibition, suppresses kyn generation and tumor growth in immunocompetent, but not immunodeficient, mice. [1] In mice bearing CT26 colon carcinoma, INCB024360 (100 mg/kg, p.o.) also inhibits the growth of IDO-expressing tumors by reducing kynurenine. [2]

Protocol (from reference)

Animal Research:[1] [2]
  • Animal Models: Female C57BL/6 or Balb/c nu/nu mice bearing PAN02 pancreatic tumors
  • Dosages: ~100 mg/kg, twice a day
  • Administration: p.o.

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+40% PEG 300+5% TWEEN 80+50 % ddH2O
For best results, use promptly after mixing.

 4.35mg/mL

Chemical Information

Molecular Weight 438.23
Formula

C11H13BrFN7O4S
CAS No. 1204669-58-8
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles C1=CC(=C(C=C1N=C(C2=NON=C2NCCNS(=O)(=O)N)NO)Br)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

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03589651 Active not recruiting Drug: Retifanlimab|Drug: Epacadostat|Drug: INCB050465 Unresectable or Metastatic Solid Tumors Incyte Corporation August 17 2018 Phase 1
NCT03361228 Terminated Drug: INCB001158|Drug: Epacadostat|Drug: Pembrolizumab Solid Tumors Incyte Corporation March 1 2018 Phase 1|Phase 2

(data from https://clinicaltrials.gov, updated on 2022-08-01)

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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