Epacadostat (INCB024360)

Catalog No.S7910 Batch:S791013

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Technical Data

Formula

C11H13BrFN7O4S
Molecular Weight 438.23 CAS No. 1204669-58-8
Solubility (25°C)* In vitro DMSO 88 mg/mL (200.8 mM)
Ethanol 22 mg/mL (50.2 mM)
Water Insoluble
In vivo (Add solvents to the product individually and in order)
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O
4.35mg/ml Taking the 1 mL working solution as an example, add 50 μL 87 mg/ml clarified DMSO stock solution to 400 μL PEG300, mix evenly to clarify it; add 50 μL Tween80 to the above system, mix evenly to clarify it; then continue to add 500 μL ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or insoluble.
* 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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

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]
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)

Kinase Assay:

[1]
  • IDO enzyme assays

    Human IDO with an N-terminal His tag is expressed in E.coli and purified to homogeneity. IDO catalyzes the oxidative cleavage of the pyrrole ring of the indole nucleus of tryptophan to yield N’-formylkynurenine. The assays are performed at room temperature using 20 nM IDO and 2 mM D-Trp in the presence of 20 mM ascorbate, 3.5 µM methylene blue and 0.2 mg/mL catalase in 50 mM potassium phosphate buffer (pH 6.5). The initial reaction rates are recorded by continuously following the absorbance increase at 321 nm due to the formation of N’-formlylkynurenine.
Cell Assay:

[3]
  • Cell lines

    Jurkat cells

  • Concentrations

    50 μM

  • Incubation Time

    72 h

  • Method

    Jurkat cells were incubated with serially diluted epacadostat for 72 h. Their viability was measured and analyzed as percentage of the non-treated control.
Animal Study:

[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.

Customer Product Validation

Data from [Data independently produced by , , FEBS J, 2016, doi: 10.1111/febs.13966.]

Data from [Data independently produced by , , Cancer Immunol Immunother, 2018, 67(8):1305-1315]

Data from [Data independently produced by , , Mol Immunol, 2018, 103:144-155]

Selleck's Epacadostat (INCB024360) has been cited by 55 publications

Loss of tumor suppressors promotes inflammatory tumor microenvironment and enhances LAG3+T cell mediated immune suppression [ Nat Commun, 2024, 15(1):5873] PubMed: 38997291
Metabolic landscape of head and neck squamous cell carcinoma informs a novel kynurenine/Siglec-15 axis in immune escape [ Cancer Commun (Lond), 2024, 10.1002/cac2.12545] PubMed: 38734931
Single-cell RNA sequencing highlights the immunosuppression of IDO1+ macrophages in the malignant transformation of oral leukoplakia [ Theranostics, 2024, 14(12):4787-4805] PubMed: 39239507
Tryptophan deficiency induced by indoleamine 2,3-dioxygenase 1 results in glucose transporter 1-dependent promotion of aerobic glycolysis in pancreatic cancer [ MedComm (2020), 2024, 5(5):e555] PubMed: 38706741
Epacadostat stabilizes the apo-form of IDO1 and signals a pro-tumorigenic pathway in human ovarian cancer cells [ Front Immunol, 2024, 15:1346686] PubMed: 38333210
IDO1 Inhibitor RY103 Suppresses Trp-GCN2-Mediated Angiogenesis and Counters Immunosuppression in Glioblastoma [ Pharmaceutics, 2024, 16(7)870] PubMed: 39065567
Selective inhibition of indoleamine and tryptophan 2,3-dioxygenases: Comparative study on kynurenine pathway in cell lines via LC-MS/MS-based targeted metabolomics [ J Pharm Biomed Anal, 2024, 237:115750] PubMed: 37804639
Blocking Tryptophan Catabolism Reduces Triple-Negative Breast Cancer Invasive Capacity [ Cancer Res Commun, 2024, 4(10):2699-2713] PubMed: 39311710
Targeting Tryptophan Catabolism in Ovarian Cancer to Attenuate Macrophage Infiltration and PD-L1 Expression [ Cancer Res Commun, 2024, 4(3):822-833] PubMed: 38451784
An adverse tumor-protective effect of IDO1 inhibition [ Cell Rep Med, 2023, 4(2):100941] PubMed: 36812891

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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