1. Epacadostat

Epacadostat (Synonyms: INCB 024360)

目录号: HY-15689 纯度: 99。65%
产品使用指南

Epacadostat (INCB 024360) 是一种有效,选择性的 IDO1 抑制剂, IC50 为 71.8 nM±17.5 nM。

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Epacadostat Chemical Structure

Epacadostat Chemical Structure

CAS No. : 1204669-58-8

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MCE 顾客使用本产品发表的科研文献

    Epacadostat purchased from MCE. Usage Cited in:

    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:

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    • 实验参考方法

    • 技术信息

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    • 参考文献

    Description

    Epacadostat (INCB 024360) is a potent and selective indoleamine 2,3-dioxigenase 1 (IDO1) inhibitor with an IC50 of 71.8 nM.

    IC50 & Target[1]

    IDO1

    71.8 nM (IC50)

    In Vitro

    In cellular assays, Epacadostat (INCB 024360) 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). Epacadostat (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 Epacadostat at 100 mg/kg. Epacadostat (INCB 024360) suppresses kynurenine equivalently in plasma, tumors, and lymph nodes. In naïve C57BL/6 mice, 50 mg/kg Epacadostat (INCB 024360) decreases plasma kynurenine levels within 1 hour and those levels stay at least 50% suppressed through the 8-hour time course[2].

    Clinical Trial
    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    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
    *请根据产品在不同溶剂中的溶解度,选择合适的溶剂配制储备液。
    In Vivo:
    • 1.

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

    References
    • [1].

      [2].

      [3].

    Cell Assay
    [1]

    To determine Epacadostat 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. Epacadostat (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 Epacadostat. C57BL/6 wild-type or Ido1-/--deficient mice are administered a single oral dose of Epacadostat (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 Epacadostat (INCB 024360), tryptophan, and kynurenine according to the methods below.

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

    References
    • [1].

      [2].

      [3].

    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

    Shipping

    Room temperature in continental US; may vary elsewhere

    Purity: 99.65%

    • [1].

      [2]。

      [3].

    • 摩尔计算器

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    The molarity calculator equation

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    This equation is commonly abbreviated as: C1V1 = C2V2

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    × = ×
    C1   V1   C2   V2

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    Inquiry Information

    产品名称:
    Epacadostat
    目录号:
    HY-15689
    需求量:

    Epacadostat

    Cat. No.: HY-15689

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