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

Epacadostat (Synonyms: INCB 024360)

製品番号: HY-15689 純度: 99.65%
取扱説明書

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

商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用としては使用しないように、十分ご注意ください。

Epacadostat 構造式

Epacadostat 構造式

CAS 番号 : 1204669-58-8

容量 価格(税別) 在庫状況 数量
無料サンプル (0.5-1 mg)   今すぐ申し込む  
10 mM * 1 mL in DMSO USD 55 在庫あり
Estimated Time of Arrival: December 31
5 mg USD 50 在庫あり
Estimated Time of Arrival: December 31
10 mg USD 80 在庫あり
Estimated Time of Arrival: December 31
25 mg USD 110 在庫あり
Estimated Time of Arrival: December 31
50 mg USD 140 在庫あり
Estimated Time of Arrival: December 31
100 mg USD 250 在庫あり
Estimated Time of Arrival: December 31
200 mg USD 400 在庫あり
Estimated Time of Arrival: December 31
500 mg USD 800 在庫あり
Estimated Time of Arrival: December 31
1 g USD 1200 在庫あり
Estimated Time of Arrival: December 31
2 g USD 2000 在庫あり
Estimated Time of Arrival: December 31
5 g   お問い合わせ  
10 g   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

カスタマーレビュー

Based on 7 publication(s) in Google Scholar

Top Publications Citing Use of Products

    Epacadostat 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).

    Indoleamine 2,3-Dioxygenase (IDO) アイソフォーム固有の製品をすべて表示:

    • 生物活性

    • プロトコル

    • 純度とドキュメンテーション

    • 参考文献

    • カスタマーレビュー

    製品説明

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

    IC50 & Target

    IDO1

    71.8 nM (IC50)

    体外実験

    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].

    体内実験

    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].

    臨床実験
    分子量

    438.23

    分子式

    C₁₁H₁₃BrFN₇O₄S

    CAS 番号

    1204669-58-8

    SMILES

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

    輸送条件

    Room temperature in continental US; may vary elsewhere.

    保管条件
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    溶剤 & 溶解度
    体外: 

    DMSO : 100 mg/mL (228.19 mM; Need ultrasonic)

    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.
    体内:
    • 1.

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: ≥ 2.5 mg/mL (5.70 mM); Clear solution

    • 2.

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

      Solubility: ≥ 2.5 mg/mL (5.70 mM); Clear solution

    • 3.

      Add each solvent one by one:  10% DMSO    90% corn oil

      Solubility: ≥ 2.5 mg/mL (5.70 mM); Clear solution

    *All of the co-solvents are provided by MCE.
    参考文献
    細胞実験
    [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 はこれらの方法の精度を確認していません。 こちらは参照専用です。

    動物実験
    [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 はこれらの方法の精度を確認していません。 こちらは参照専用です。

    参考文献

    純度: 99.65%

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    Keywords:

    EpacadostatINCB 024360INCB024360INCB-024360Indoleamine 2,3-Dioxygenase (IDO)Inhibitorinhibitorinhibit

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    製品名:
    Epacadostat
    製品番号:
    HY-15689
    数量:
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