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

Epacadostat  (Synonyms: INCB 024360)

目錄號: HY-15689 純度: 99.66%
COA 產(chǎn)品使用指南

Epacadostat (INCB 024360) 是一種有效，選擇性的 IDO1 抑制劑， IC50 為 71.8 nM。

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Epacadostat Chemical Structure

Epacadostat Chemical Structure

CAS No. : 1204669-58-8

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規(guī)格 價格 是否有貨 數(shù)量
10 mM * 1 mL in DMSO ￥550
In-stock
5 mg ￥500
In-stock
10 mg ￥800
In-stock
25 mg ￥1500
In-stock
50 mg ￥2300
In-stock
100 mg ￥3600
In-stock
200 mg ￥5488
In-stock
500 mg 現(xiàn)貨 詢價
1 g   詢價  
5 g   詢價  

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Customer Review

Other Forms of Epacadostat:

    Epacadostat purchased from MCE. Usage Cited in: Br J Pharmacol. 2018 Jul;175(14):3034-3049.  [Abstract]

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

    查看 Indoleamine 2,3-Dioxygenase (IDO) 亞型特異性產(chǎn)品:

    • 生物活性

    • 實(shí)驗參考方法

    • 純度 & 產(chǎn)品資料

    • 參考文獻(xiàn)

    生物活性

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

    IC50 & Target[1]

    IDO1

    71.8 nM (IC50)

    細(xì)胞效力
    (Cellular Effect)
    Cell Line Type Value Description References
    A549 IC50
    > 100 μM
    Compound: 2; INCB024360
    Antiproliferative activity against human A549 cells after 48 hrs by CCK-8 assay
    Antiproliferative activity against human A549 cells after 48 hrs by CCK-8 assay
    		[PMID: 29670692]
    CT26 IC50
    > 100 μM
    Compound: 2; INCB024360
    Antiproliferative activity against mouse CT26 cells after 48 hrs by CCK-8 assay
    Antiproliferative activity against mouse CT26 cells after 48 hrs by CCK-8 assay
    		[PMID: 29670692]
    CT26 IC50
    > 100 μM
    Compound: 1
    Cytotoxicity against mouse CT26 cells assessed as reduction in cell viability measured after 72 hrs by CCK8 assay
    Cytotoxicity against mouse CT26 cells assessed as reduction in cell viability measured after 72 hrs by CCK8 assay
    		[PMID: 33482599]
    CT26 IC50
    47.09 μM
    Compound: Epacadostat
    Cytotoxicity against mouse CT26 cells assessed as reduction in cell viability by CCK8 assay
    Cytotoxicity against mouse CT26 cells assessed as reduction in cell viability by CCK8 assay
    		[PMID: 34854662]
    HCT-116 IC50
    > 100 μM
    Compound: 2; INCB024360
    Antiproliferative activity against human HCT116 cells after 48 hrs by CCK-8 assay
    Antiproliferative activity against human HCT116 cells after 48 hrs by CCK-8 assay
    		[PMID: 29670692]
    HCT-116 IC50
    > 50 μM
    Compound: Epacadostat
    Cytotoxicity against human HCT-116 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay
    Cytotoxicity against human HCT-116 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay
    		[PMID: 34147748]
    HCT-116 IC50
    37.1 μM
    Compound: Epacadostat
    Cytotoxicity against human HCT-116 cells assessed as reduction in cell viability by CCK8 assay
    Cytotoxicity against human HCT-116 cells assessed as reduction in cell viability by CCK8 assay
    		[PMID: 34854662]
    HEK293 IC50
    0.242 μM
    Compound: INCB024360
    Inhibition of TDO (unknown origin) expressed in HEK293 cells using L-Trp as substrate after 8 hrs
    Inhibition of TDO (unknown origin) expressed in HEK293 cells using L-Trp as substrate after 8 hrs
    		[PMID: 30321802]
    HEK293 IC50
    0.26 μM
    Compound: INCB24360
    Inhibition of human TDO transfected in HEK293 cells assessed as reduction in kynurenine production using L-tryptophan as substrate incubated for 12 hrs
    Inhibition of human TDO transfected in HEK293 cells assessed as reduction in kynurenine production using L-tryptophan as substrate incubated for 12 hrs
    		[PMID: 31580660]
    HEK293 IC50
    12.6 nM
    Compound: 1
    Inhibition of recombinant human IDO1 expressed in HEK293 cells assessed as N-formylkynurenine formation by measuring kynurenine level incubated for 12 hrs by microplate reader analysis
    Inhibition of recombinant human IDO1 expressed in HEK293 cells assessed as N-formylkynurenine formation by measuring kynurenine level incubated for 12 hrs by microplate reader analysis
    		[PMID: 31233921]
    HeLa IC50
    > 100 μM
    Compound: 1
    Cytotoxicity against human HeLa cells assessed as reduction in cell viability measured after 72 hrs by CCK8 assay
    Cytotoxicity against human HeLa cells assessed as reduction in cell viability measured after 72 hrs by CCK8 assay
    		[PMID: 33482599]
    HeLa IC50
    0.007 μM
    Compound: INCB24360
    Inhibition of IDO1 in IFN-gamma stimulated human HeLa cells assessed as reduction in kynurenine production incubated for 18 hrs
    Inhibition of IDO1 in IFN-gamma stimulated human HeLa cells assessed as reduction in kynurenine production incubated for 18 hrs
    		[PMID: 31580660]
    HeLa IC50
    0.016 μM
    Compound: Epacadostat
    Inhibition of IDO1 in IFN-gamma stimulated human HeLa cells assessed as reduction in kynurenine production using L-tryptophan as substrate incubated for 24 hrs
    Inhibition of IDO1 in IFN-gamma stimulated human HeLa cells assessed as reduction in kynurenine production using L-tryptophan as substrate incubated for 24 hrs
    		[PMID: 31610376]
    HeLa IC50
    0.07 μM
    Compound: INCB24360
    Inhibition of IDO1 in human HeLa cells using L-tryptophan as substrate after 20 hrs
    Inhibition of IDO1 in human HeLa cells using L-tryptophan as substrate after 20 hrs
    		[PMID: 30469041]
    HeLa IC50
    10 nM
    Compound: 1; INCB24360
    Inhibition of IDO1 in human HeLa cells using L-tryptophan as substrate incubated for 48 hrs
    Inhibition of IDO1 in human HeLa cells using L-tryptophan as substrate incubated for 48 hrs
    		[PMID: 31445231]
    HeLa IC50
    10.3 nM
    Compound: INCB024360
    Inhibition of IDO1 in IFN-gamma stimulated human HeLa cells assessed as reduction in kynurenine production incubated for 24 hrs relative to control
    Inhibition of IDO1 in IFN-gamma stimulated human HeLa cells assessed as reduction in kynurenine production incubated for 24 hrs relative to control
    		[PMID: 30858027]
    HeLa IC50
    12.5 nM
    Compound: Epacadostat
    Inhibition of IDO1 in IFN-gamma stimulated human HeLa cells using L-tryptophan as substrate incubated for 48 hrs by fluorescence assay
    Inhibition of IDO1 in IFN-gamma stimulated human HeLa cells using L-tryptophan as substrate incubated for 48 hrs by fluorescence assay
    		[PMID: 32832022]
    HeLa IC50
    7.1 nM
    Compound: 1; INCB024360
    Inhibition of IFN-gamma-stimulated IDO1 activity in human HeLa cells using L-tryptophan as substrate after 48 hrs by microplate reader analysis
    Inhibition of IFN-gamma-stimulated IDO1 activity in human HeLa cells using L-tryptophan as substrate after 48 hrs by microplate reader analysis
    		[PMID: 25970480]
    HeLa IC50
    7.1 nM
    Compound: INCB24360
    Inhibition of IFN-gamma stimulated IDO1 in human HeLa cells assessed as reduction in formation of kynurenine incubated for 48 hrs in presence of IFNgamma by microplate reader assay
    Inhibition of IFN-gamma stimulated IDO1 in human HeLa cells assessed as reduction in formation of kynurenine incubated for 48 hrs in presence of IFNgamma by microplate reader assay
    		[PMID: 31580660]
    HeLa IC50
    7.4 nM
    Compound: 4f; INCB24360
    Inhibition of IDO1 in IFN-gamma-stimulated human HeLa cells assessed as decrease in kynurenine levels after 48 hrs
    Inhibition of IDO1 in IFN-gamma-stimulated human HeLa cells assessed as decrease in kynurenine levels after 48 hrs
    		[PMID: 28523098]
    HeLa EC50
    8 nM
    Compound: Epacadostat
    Inhibition of IDO1 in IFN-gamma stimulated human HeLa cells assessed as reduction in kynurenine formation using L-tryptophan as substrate incubated for 24 hrs by UV-spectrophotometry
    Inhibition of IDO1 in IFN-gamma stimulated human HeLa cells assessed as reduction in kynurenine formation using L-tryptophan as substrate incubated for 24 hrs by UV-spectrophotometry
    		[PMID: 32088128]
    HepG2 IC50
    > 50 μM
    Compound: Epacadostat
    Cytotoxicity against human HepG2 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay
    Cytotoxicity against human HepG2 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay
    		[PMID: 34147748]
    HGC-27 IC50
    > 50 μM
    Compound: Epacadostat
    Cytotoxicity against human HGC-27 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay
    Cytotoxicity against human HGC-27 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay
    		[PMID: 34147748]
    HT-29 IC50
    > 100 μM
    Compound: 2; INCB024360
    Antiproliferative activity against human HT-29 cells after 48 hrs by CCK-8 assay
    Antiproliferative activity against human HT-29 cells after 48 hrs by CCK-8 assay
    		[PMID: 29670692]
    HT-29 IC50
    62.96 μM
    Compound: Epacadostat
    Cytotoxicity against human HT-29 cells assessed as reduction in cell viability by CCK8 assay
    Cytotoxicity against human HT-29 cells assessed as reduction in cell viability by CCK8 assay
    		[PMID: 34854662]
    Lewis lung carcinoma cell line IC50
    > 100 μM
    Compound: 2; INCB024360
    Antiproliferative activity against mouse LLC cells after 48 hrs by CCK-8 assay
    Antiproliferative activity against mouse LLC cells after 48 hrs by CCK-8 assay
    		[PMID: 29670692]
    MCF7 IC50
    > 50 μM
    Compound: Epacadostat
    Cytotoxicity against human MCF7 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay
    Cytotoxicity against human MCF7 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay
    		[PMID: 34147748]
    THP-1 IC50
    5.6 nM
    Compound: INCB024360
    Inhibition of IDO1 in IFN-gamma/LPS stimulated human THP-1 cells assessed as reduction in kynurenine production after 24 hrs
    Inhibition of IDO1 in IFN-gamma/LPS stimulated human THP-1 cells assessed as reduction in kynurenine production after 24 hrs
    		[PMID: 30858027]
    U-87MG ATCC IC50
    > 50 μM
    Compound: Epacadostat
    Cytotoxicity against human U87 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay
    Cytotoxicity against human U87 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay
    		[PMID: 34147748]
    U-87MG ATCC IC50
    0.26 μM
    Compound: INCB024360
    Inhibition of TDO in human U87 MG cells using L-Trp as substrate after 8 hrs
    Inhibition of TDO in human U87 MG cells using L-Trp as substrate after 8 hrs
    		[PMID: 30321802]
    體外研究
    (In Vitro)

    在細(xì)胞測定中，Epacadostat (INCB 024360) 選擇性抑制人 IDO1，IC50 值約為 10 nM，表明對其他相關(guān)酶 (例如 IDO2 或色氨酸 2，3-雙加氧酶 (TDO)) 幾乎沒有活性。Epacadostat (INCB 024360) 也對小鼠 IDO1 表現(xiàn)出顯著活性，IC50 值為 52.4 nM±15.7 nM，在使用小鼠 IDO1 轉(zhuǎn)染的 HEK293/MSR 細(xì)胞的類似測定中[1]。

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    體內(nèi)研究
    (In Vivo)

    攜帶 CT26 腫瘤的雌性 Balb/c 小鼠用 100 mg/kg 的 Epacadostat 口服處理，每天兩次，持續(xù) 12 天。Epacadostat (INCB 024360) 在血漿、腫瘤和淋巴結(jié)中等效地抑制犬尿氨酸。在初始 C57BL/6 小鼠中，50 mg/kg Epacadostat (INCB 024360) 可在 1 小時內(nèi)降低血漿犬尿氨酸水平，并且這些水平在 8 小時的時間過程中保持至少 50% 的抑制[2]。

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

    438.23

    Formula

    C11H13BrFN7O4S
    CAS 號
    性狀

    固體

    顏色

    White to gray

    運(yùn)輸條件

    Room temperature in continental US; may vary elsewhere.
    儲存方式
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    溶解性數(shù)據(jù)
    細(xì)胞實(shí)驗： 

    DMSO 中的溶解度 : 100 mg/mL (228.19 mM; 超聲助溶; 吸濕的 DMSO 對產(chǎn)品的溶解度有顯著影響，請使用新開封的 DMSO)

    配制儲備液
    濃度 溶劑體積 質(zhì)量 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
    查看完整儲備液配制表

    * 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
    儲備液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C儲存時，請在2年內(nèi)使用， -20°C儲存時，請在1年內(nèi)使用。

    • 摩爾計算器

    • 稀釋計算器

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    質(zhì)量
    =
    濃度
    ×
    體積
    ×
    分子量 *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    濃度 (start)

    C1

    ×
    體積 (start)

    V1

    =
    濃度 (final)

    C2

    ×
    體積 (final)

    V2

    動物實(shí)驗：

    請根據(jù)您的 實(shí)驗動物和給藥方式 選擇適當(dāng)?shù)娜芙夥桨浮?

    以下溶解方案都請先按照 In Vitro 方式配制澄清的儲備液，再依次添加助溶劑：
    ——為保證實(shí)驗結(jié)果的可靠性，澄清的儲備液可以根據(jù)儲存條件，適當(dāng)保存；體內(nèi)實(shí)驗的工作液，建議您現(xiàn)用現(xiàn)配，當(dāng)天使用；
    以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的方式助溶

    • 方案 一

      請依序添加每種溶劑： 5% DMSO    40% PEG300    5% Tween-80    50% Saline

      Solubility: ≥ 2.62 mg/mL (5.98 mM); 澄清溶液

    • 方案 二

      請依序添加每種溶劑： 5% DMSO    95% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.62 mg/mL (5.98 mM); 澄清溶液

    動物溶解方案計算器
    請輸入動物實(shí)驗的基本信息：

    給藥劑量

    mg/kg

    動物的平均體重

    g

    每只動物的給藥體積

    μL

    動物數(shù)量

    只
    由于實(shí)驗過程有損耗，建議您多配一只動物的量
    請輸入您的動物體內(nèi)配方組成：
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    如果您的動物是免疫缺陷鼠或者體弱鼠，建議 DMSO 中的在最后工作液體系中的占比盡量不超過 2%。
    方案所需 助溶劑 包括：DMSO， ，均可在 MCE 網(wǎng)站選購。 ，Tween 80，均可在 MCE 網(wǎng)站選購。
    計算結(jié)果
    工作液所需濃度 : mg/mL
    儲備液配制方法 : mg 藥物溶于 μL  DMSO（母液濃度為 mg/mL）。
    您所需的儲備液濃度超過該產(chǎn)品的實(shí)測溶解度，以下方案僅供參考，如有需要，請與 MCE 中國技術(shù)支持聯(lián)系。
    動物實(shí)驗體內(nèi)工作液的配制方法 : 取 μL DMSO 儲備液，加入 μL 。 μL ，混合均勻至澄清，再加 μL Tween 80，混合均勻至澄清，再加 μL 生理鹽水。
    連續(xù)給藥周期超過半月以上，請謹(jǐn)慎選擇該方案。
    請確保第一步儲備液溶解至澄清狀態(tài)，從左到右依次添加助溶劑。您可采用超聲加熱 （超聲清洗儀，建議頻次 20-40 kHz），渦旋吹打等方式輔助溶解。
    純度 & 產(chǎn)品資料

    純度: 99.66%

    參考文獻(xiàn)
    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.
    參考文獻(xiàn)

    完整儲備液配制表

    * 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
    儲備液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C儲存時，請在2年內(nèi)使用， -20°C儲存時，請在1年內(nèi)使用。

    可選溶劑 濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.2819 mL 11.4095 mL 22.8191 mL 57.0477 mL
    5 mM 0.4564 mL 2.2819 mL 4.5638 mL 11.4095 mL
    10 mM 0.2282 mL 1.1410 mL 2.2819 mL 5.7048 mL
    15 mM 0.1521 mL 0.7606 mL 1.5213 mL 3.8032 mL
    20 mM 0.1141 mL 0.5705 mL 1.1410 mL 2.8524 mL
    25 mM 0.0913 mL 0.4564 mL 0.9128 mL 2.2819 mL
    30 mM 0.0761 mL 0.3803 mL 0.7606 mL 1.9016 mL
    40 mM 0.0570 mL 0.2852 mL 0.5705 mL 1.4262 mL
    50 mM 0.0456 mL 0.2282 mL 0.4564 mL 1.1410 mL
    60 mM 0.0380 mL 0.1902 mL 0.3803 mL 0.9508 mL
    80 mM 0.0285 mL 0.1426 mL 0.2852 mL 0.7131 mL
    100 mM 0.0228 mL 0.1141 mL 0.2282 mL 0.5705 mL
    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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    產(chǎn)品名稱：
    Epacadostat
    目錄號：
    HY-15689
    需求量：