1. Metabolic Enzyme/Protease
  2. Indoleamine 2,3-Dioxygenase (IDO)

INCB 024360 (Synonyms: Epacadostat)

Cat. No.: HY-15689 Purity: 99.65%
Handling Instructions

INCB 024360 is a potent and selective IDO1 inhibitor with IC50 of 71.8 nM±17.5 nM.

For research use only. We do not sell to patients.

INCB 024360 Chemical Structure

INCB 024360 Chemical Structure

CAS No. : 1204669-58-8

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Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 79 In-stock
Estimated Time of Arrival: December 31
5 mg USD 72 In-stock
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10 mg USD 108 In-stock
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50 mg USD 228 In-stock
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100 mg USD 348 In-stock
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200 mg USD 540 In-stock
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500 mg USD 1020 In-stock
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2 g USD 2520 In-stock
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Customer Review

    INCB 024360 purchased from MCE. Usage Cited in: Br J Pharmacol. 2018 Jul;175(14):3034-3049.

    Western blot analysis of IDO1 protein levels for IFN-γ-stimulated HeLa cells that are treated with indicated compounds (e.g., Epacadostat).

    View All Indoleamine 2,3-Dioxygenase (IDO) Isoform Specific Products:

    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    Description

    INCB 024360 is a potent and selective IDO1 inhibitor with IC50 of 71.8 nM±17.5 nM.

    IC50 & Target

    IC50: 71.8 nM±17.5 nM (IDO1), 7.1 nM±0.6 nM (IDO1, in HeLa cells)[1]

    In Vitro

    In cellular assays, INCB 024360 (INCB024360) selectively inhibits human IDO1 with IC50 values of approximately 10 nM, demonstrating little activity against other related enzymes such as IDO2 or tryptophan 2,3-dioxygenase (TDO). INCB 024360 also exhibits significant activity toward mouse IDO1, with an IC50 value of 52.4 nM±15.7 nM, in a similar assay using mouse IDO1-transfected HEK293/MSR cells[1].

    In Vivo

    Female Balb/c mice bearing CT26 tumors are treated orally twice daily for 12 d with INCB 024360 (INCB024360) at 100 mg/kg. INCB 024360 suppresses kynurenine equivalently in plasma, tumors, and lymph nodes. In naïve C57BL/6 mice, 50 mg/kg INCB024360 decreases plasma kynurenine levels within 1 hour and those levels stay at least 50% suppressed through the 8-hour time course[2].

    Clinical Trial
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 31 mg/mL (70.74 mM)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.2819 mL 11.4095 mL 22.8191 mL
    5 mM 0.4564 mL 2.2819 mL 4.5638 mL
    10 mM 0.2282 mL 1.1410 mL 2.2819 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      INCB 024360 (Epacadostat) is dissolved freshly in sodium citrate buffer prior to each experiment[3].

    References
    Cell Assay
    [1]

    To determine INCB 024360 activity against IDO in recombinant cells, HEK293/MSR cells are transiently transfected with full-length human or mouse IDO1, or mouse IDO2 cDNA, with Transit-293 transfection reagent or Lipofectamine 2000 reagents. INCB 024360 at different concentrations is added to the recovered transfected cells seeded at 2×104 cells per well in a 96-well plate (200 μL/well). The cells are incubated for 2 days, and kyn in the supernatants is measured as described in the HeLa cell assay. The tryptophan 2,3-dioxygenase (TDO) assay is performed similarly with HEK293/MSR cells transfected with a human TDO expression vector[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Administration
    [2]

    Mice[2]
    The female C57BL/6 mice are dosed orally with 50 mg/kg INCB 024360. C57BL/6 wild-type or Ido1-/--deficient mice are administered a single oral dose of INCB 024360, at which point food is removed from the cages until after the 8-h time point. At various time points after dosing, mice are euthanized and blood is collected by cardiac puncture. Plasma is analyzed for the presence of INCB023843, INCB 024360, tryptophan, and kynurenine according to the methods below. Data are analyzed using one-way ANOVA with Dunnett's posttest for statistical significance.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    References
    Molecular Weight

    438.23

    Formula

    C₁₁H₁₃BrFN₇O₄S

    CAS No.

    1204669-58-8

    SMILES

    BrC1=C(F)C=CC(N/C(C2=NON=C2NCCNS(N)(=O)=O)=N\O)=C1

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Shipping

    Room temperature in continental US; may vary elsewhere

    Purity: 99.65%

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    Product Name:
    INCB 024360
    Cat. No.:
    HY-15689
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    INCB 024360

    Cat. No.: HY-15689