Epacadostat (INCB024360)

For research use only.

Catalog No.S7910

29 publications

Epacadostat (INCB024360) Chemical Structure

CAS No. 1204669-58-8

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).

Selleck's Epacadostat (INCB024360) has been cited by 29 publications

Purity & Quality Control

Choose Selective IDO/TDO Inhibitors

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 M2eweWZ2dmO2aX;uJIF{e2G7 NX24PZBKUUSRIHnubIljcXSrb36sJGlEPTC-MUWuN{BvVQ>? NIfa[lk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEGxNlExQSd-M{CxNVIyODl:L3G+
Jurkat MlzmR4VtdCC4aXHibYxqfHliYYPzZZk> M{C5PVczKGh? MYry[YR2[2WmIITo[UBvfW2kZYKgc4YhfmmjYnzlJINmdGy|LDDJR|UxKD1iNUCg{txO M1rKZ|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyMUGyNVA6Lz5|MEGxNlExQTxxYU6=
OCI-AML2 NEHsZ2pHfW6ldHnvckBie3OjeR?= NYCycXZvUW6qaXLpeIlwdiCxZjDJSG8yKGmwIFnGUodidW2jLYP0bY12dGG2ZXSgbJVu[W5iT1PJMWFOVDJiY3XscJMh[XO|ZYPz[YQh[XNicnXkeYN1cW:wIHnuJIt6dnW{ZX7pcoUheHKxZIXjeIlwdixiSVO1NEA:KDBwMECzOEDPxE1w NWj1[Y5bRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkmyNlA4QDhpPkK5NlIxPzh6PD;hQi=>
HeLa M4DSOmZ2dmO2aX;uJIF{e2G7 MUS0PEBpenN? MnfGTY5pcWKrdHnvckBw\iCLRl6t[4FudWFvc4TpcZVt[XSnZDDJSG8yKGGldHn2bZR6KGmwIHj1cYFvKEinTHGgZ4VtdHNidYPpcochVC22conweI9xcGGwIHHzJJN2[nO2cnH0[UBi\nSncjC0PEBpenNiYomgcYlkem:ybHH0[UBz\WGmZYKgZY5idHm|aYOsJGlEPTBiPTCwMlAxPzFizszNMi=> NXezVIJRRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW5O|A1QDBpPkK1PVcxPDhyPD;hQi=>
HeLa MX7GeY5kfGmxbjDhd5NigQ>? MnPBOFghcHK| NYX2e2JoUW6qaXLpeIlwdiCxZjDJSG8yKGmwIFnGUk1o[W2vYT3zeIlufWyjdHXkJIh2dWGwIFjlUIEh[2WubIOgZZN{\XO|ZXSgZZMh\GWlcnXhd4UhcW5ia4nueZJmdmmwZTDs[ZZmdHNiYX\0[ZIhPDhiaILzMEBKSzVyIE2gNE4xODd2IN88UU4> NWeyVo53RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMki1NlMxQThpPkK4OVI{ODl6PD;hQi=>
HEK293 M1zGT2Z2dmO2aX;uJIF{e2G7 NH3GZXE{OCCvaX7z M2flUmlvcGmkaYTpc44hd2ZiaIXtZY4hUUSRMTDlfJBz\XO|ZXSgbY4hUEWNMkmzJINmdGy|IHHzd4V{e2WmIHHzJJJm\HWldHnvckBqdiCteX71doVvcW6nIIDyc4R2[3Srb36gZYZ1\XJiM{CgcYlveyxiRVO1NEA:KDBwMEC4O|Qh|ryPLh?= NWfNN|NKRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0OVY5ODFpPkK5OFU3QDBzPD;hQi=>
T-cells MVHGeY5kfGmxbjDhd5NigQ>? MmntNkBl[Xm| NWfzOFc5UW6qaXLpeIlwdiCxZjDJSG8yKGmwIFnGUodidW2jIHHu[EBNWFNvc4TpcZVt[XSnZDDoeY1idiCmZX7kdol1cWNiY3XscJMh[29vY4XseJVz\WRid3n0bEBpfW2jbjDUJINmdGy|IHHzd4V{e2WmIHHzJIlvcGmkaYTpc44hd2ZiVD3j[YxtKHC{b3zp[oVz[XSrb36gbY4heHKnc3XuZ4Uhd2Zic3;seYJt\SCjboTpMWNFOyCjboTpZo9lgSCjbnSgbJVu[W5icnXjc41jcW6jboSgTWwuOiCrbnP1ZoF1\WRiZn;yJFIh\GG7czygTWM2OCB;IECuNFE{KM7:TT6= M1u5[VxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7MkKwO|g5Lz5{OUKyNFc5QDxxYU6=
HEK293/MSR MXfGeY5kfGmxbjDhd5NigQ>? MWLJcohq[mm2aX;uJI9nKGi3bXHuJGlFVzFiZYjwdoV{e2WmIHnuJGhGUzJ7Mz;NV3Ih[2WubIOgZZN{\XO|ZXSgZZMhemWmdXP0bY9vKGmwIHv5cpVz\W6rbnWgdJJw\HWldHnvckBqdmO3YnH0[YQh\nKxIEKg[IF6eyxiSVO1NEA:KDBwMEG1JO69VS5? MoK5QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl{MkC3PFgoRjJ7MkKwO|g5RC:jPh?=
THP1 NXO5cnFYTnWwY4Tpc44h[XO|YYm= MY\Jcohq[mm2aX;uJI9nKEmGT{GgbY4hUU[QZ3HtcYEue3SrbYXsZZRm\CCqdX3hckBVUFBzIHPlcIx{KGG|c3Xzd4VlKGG|IILl[JVkfGmxbjDpckBsgW63cnXubY5mKHC{b3T1Z5RqdyCkeTDzdIVkfHKxcHjveI9u\XS{aXOgZY5idHm|aYOsJGlEPTBiPTCwMlAzOyEQvF2u MkfNQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl{MkC3PFgoRjJ7MkKwO|g5RC:jPh?=

... 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

Animal Research:[1] [2]
- Collapse
  • 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.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 87 mg/mL (198.52 mM)
Water Insoluble
Ethanol '53 mg/mL warmed
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

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 438.23
Formula

C11H13BrFN7O4S

CAS No. 1204669-58-8
Storage powder
in solvent
Synonyms N/A
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)
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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

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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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID