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  2. Epigenetics Anti-infection
  3. Epigenetic Reader Domain HIV
  4. Apabetalone

Apabetalone  (Synonyms: 阿帕他隆; RVX-208; RVX000222)

目錄號: HY-16652 純度: 99.47%
COA 產(chǎn)品使用指南 技術(shù)支持

Apabetalone (RVX-208) 是一種 BET 轉(zhuǎn)錄抑制劑，作用于 BD1 和 BD2，IC50 分別為 87 μM 和 0.51 μM。

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Apabetalone Chemical Structure

Apabetalone Chemical Structure

CAS No. : 1044870-39-4

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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
1 mg ￥250
In-stock
5 mg ￥500
In-stock
10 mg ￥830
In-stock
25 mg ￥1438
In-stock
50 mg ￥2088
In-stock
100 mg ￥3225
In-stock
200 mg   詢價  
500 mg   詢價  

* Please select Quantity before adding items.

Customer Review

    Apabetalone purchased from MCE. Usage Cited in: Biochim Biophys Acta. 2016 Dec;1859(12):1527-1537.  [Abstract]

    RVX208 increases CTGF and CYR61 expression and TAZ protein level in HCT116 cells.

    查看 HIV 亞型特異性產(chǎn)品:

    • 生物活性

    • 實驗參考方法

    • 純度 & 產(chǎn)品資料

    • 參考文獻(xiàn)

    生物活性

    Apabetalone (RVX-208) is an inhibitor of BET transcriptional regulators with selectivity for the second bromodomain. The IC50s are 87 μM and 0.51 μM for BD1 and BD2, respectively[1].

    IC50 & Target

    IC50: 510±41 nM (BD2), 87±10 μM (BD1)[1]
    細(xì)胞效力
    (Cellular Effect)
    Cell Line Type Value Description References
    697 EC50
    > 5 μM
    Compound: 3; RVX-208
    Cytotoxicity against human 697 cells assessed as reduction in cell viability after 5 days by CellTiter-Glo assay
    Cytotoxicity against human 697 cells assessed as reduction in cell viability after 5 days by CellTiter-Glo assay
    		[PMID: 29170024]
    A-375 IC50
    240.9 μM
    Compound: RVX-208
    Antiproliferative activity against human A375 cells assessed as reduction in cell growth measured after 48 hrs by MTT assay
    Antiproliferative activity against human A375 cells assessed as reduction in cell growth measured after 48 hrs by MTT assay
    		[PMID: 30926312]
    A549 IC50
    53.1 μM
    Compound: RVX-208
    Antiproliferative activity against human A549 cells assessed as reduction in cell growth measured after 48 hrs by MTT assay
    Antiproliferative activity against human A549 cells assessed as reduction in cell growth measured after 48 hrs by MTT assay
    		[PMID: 30926312]
    CCRF-CEM EC50
    > 5 μM
    Compound: RVX-028
    Cytotoxicity against human CCRF-CEM cells assessed as reduction in cell viability incubated for 72 hrs
    Cytotoxicity against human CCRF-CEM cells assessed as reduction in cell viability incubated for 72 hrs
    		[PMID: 35348328]
    DLD-1 IC50
    > 10 μM
    Compound: RVX-208
    Antiproliferative activity against human DLD1 cells assessed as reduction in cell viability measured after 24 to 48 hrs by MTT assay
    Antiproliferative activity against human DLD1 cells assessed as reduction in cell viability measured after 24 to 48 hrs by MTT assay
    		[PMID: 32153186]
    HCT-116 IC50
    12.83 μM
    Compound: RVX-208
    Antiproliferative activity against human HCT116 cells assessed as reduction in cell viability measured after 24 to 48 hrs by MTT assay
    Antiproliferative activity against human HCT116 cells assessed as reduction in cell viability measured after 24 to 48 hrs by MTT assay
    		[PMID: 32153186]
    HepG2 IC50
    103 μM
    Compound: RVX-208
    Antiproliferative activity against human HepG2 cells assessed as reduction in cell growth measured after 48 hrs by MTT assay
    Antiproliferative activity against human HepG2 cells assessed as reduction in cell growth measured after 48 hrs by MTT assay
    		[PMID: 30926312]
    HL-60 IC50
    > 20 μM
    Compound: 2; RVX-208
    Cytotoxicity against human HL60 cells assessed as decrease in cell viability after 24 hrs by MTT assay
    Cytotoxicity against human HL60 cells assessed as decrease in cell viability after 24 hrs by MTT assay
    		[PMID: 27266999]
    HT-29 IC50
    235.8 μM
    Compound: RVX-208
    Antiproliferative activity against human HT-29 cells assessed as reduction in cell growth measured after 48 hrs by MTT assay
    Antiproliferative activity against human HT-29 cells assessed as reduction in cell growth measured after 48 hrs by MTT assay
    		[PMID: 30926312]
    K562 EC50
    > 5 μM
    Compound: RVX-028
    Cytotoxicity against human K562 cells assessed as reduction in cell viability incubated for 72 hrs
    Cytotoxicity against human K562 cells assessed as reduction in cell viability incubated for 72 hrs
    		[PMID: 35348328]
    L02 IC50
    > 100 μM
    Compound: RVX-208
    Cytotoxicity against human LO2 cells assessed as reduction in cell growth measured after 24 hrs by MTT assay
    Cytotoxicity against human LO2 cells assessed as reduction in cell growth measured after 24 hrs by MTT assay
    		[PMID: 30926312]
    LOUCY EC50
    > 5 μM
    Compound: 3; RVX-208
    Cytotoxicity against human Loucy cells assessed as reduction in cell viability after 5 days by CellTiter-Glo assay
    Cytotoxicity against human Loucy cells assessed as reduction in cell viability after 5 days by CellTiter-Glo assay
    		[PMID: 29170024]
    MCF7 IC50
    > 300 μM
    Compound: RVX-208
    Antiproliferative activity against human MCF7 cells assessed as reduction in cell growth measured after 48 hrs by MTT assay
    Antiproliferative activity against human MCF7 cells assessed as reduction in cell growth measured after 48 hrs by MTT assay
    		[PMID: 30926312]
    MCF7 IC50
    140.1 μM
    Compound: 2a; RVX-208
    Antiproliferative activity against human MCF7 cells after 24 hrs by MTT assay
    Antiproliferative activity against human MCF7 cells after 24 hrs by MTT assay
    		[PMID: 29172540]
    MDA-MB-231 IC50
    155.4 μM
    Compound: 2a; RVX-208
    Antiproliferative activity against human MDA-MB-231 cells after 24 hrs by MTT assay
    Antiproliferative activity against human MDA-MB-231 cells after 24 hrs by MTT assay
    		[PMID: 29172540]
    MOLM-14 EC50
    6.7 μM
    Compound: RVX-028
    Cytotoxicity against human MOLM-14 cells assessed as reduction in cell viability incubated for 72 hrs
    Cytotoxicity against human MOLM-14 cells assessed as reduction in cell viability incubated for 72 hrs
    		[PMID: 35348328]
    MV4-11 IC50
    > 20 μM
    Compound: 2; RVX-208
    Cytotoxicity against human MV4-11 cells assessed as decrease in cell viability after 24 hrs by MTT assay
    Cytotoxicity against human MV4-11 cells assessed as decrease in cell viability after 24 hrs by MTT assay
    		[PMID: 27266999]
    MV4-11 IC50
    4.48 μM
    Compound: 1; RVX-208
    Antiproliferative activity against human MV4-11 cells after 72 hrs by MTT assay
    Antiproliferative activity against human MV4-11 cells after 72 hrs by MTT assay
    		[PMID: 28765013]
    NALM-6 EC50
    > 5 μM
    Compound: 3; RVX-208
    Cytotoxicity against human NALM6 cells assessed as reduction in cell viability after 5 days by CellTiter-Glo assay
    Cytotoxicity against human NALM6 cells assessed as reduction in cell viability after 5 days by CellTiter-Glo assay
    		[PMID: 29170024]
    NB-4 EC50
    > 5 μM
    Compound: RVX-028
    Cytotoxicity against human NB-4 cells assessed as reduction in cell viability incubated for 72 hrs
    Cytotoxicity against human NB-4 cells assessed as reduction in cell viability incubated for 72 hrs
    		[PMID: 35348328]
    NRK-49F IC50
    42 μM
    Compound: RVX-208
    Antifibrotic activity against rat NRK-49F cells assessed as reduction in cell growth measured after 48 hrs by MTT assay
    Antifibrotic activity against rat NRK-49F cells assessed as reduction in cell growth measured after 48 hrs by MTT assay
    		[PMID: 30926312]
    OCI-AML2 IC50
    8.31 μM
    Compound: 1; RVX-208
    Antiproliferative activity against human OCI-AML2 cells after 72 hrs by MTT assay
    Antiproliferative activity against human OCI-AML2 cells after 72 hrs by MTT assay
    		[PMID: 28765013]
    OCI-AML-3 IC50
    7.17 μM
    Compound: 1; RVX-208
    Antiproliferative activity against human OCI-AML3 cells after 72 hrs by MTT assay
    Antiproliferative activity against human OCI-AML3 cells after 72 hrs by MTT assay
    		[PMID: 28765013]
    SW-620 IC50
    > 10 μM
    Compound: RVX-208
    Antiproliferative activity against human SW620 cells assessed as reduction in cell viability measured after 24 to 48 hrs by MTT assay
    Antiproliferative activity against human SW620 cells assessed as reduction in cell viability measured after 24 to 48 hrs by MTT assay
    		[PMID: 32153186]
    U-937 IC50
    > 20 μM
    Compound: 2; RVX-208
    Cytotoxicity against human U937 cells assessed as decrease in cell viability after 24 hrs by MTT assay
    Cytotoxicity against human U937 cells assessed as decrease in cell viability after 24 hrs by MTT assay
    		[PMID: 27266999]
    體外研究
    (In Vitro)

    Apabetalone (RVX-208) competes with binding of an acetylated histone peptide to tandem BD1 BD2 protein constructs of the four BET proteins, with IC50s between 0.5 and 1.8 μM. Apabetalone increases the production of ApoA-I in hepatocytes in vitro, which results in increased high density lipoprotein cholesterol (HDL-C). Apabetalone selectively binds to bromodomains of the BET (Bromodomain and Extra Terminal) family, competing for a site bound by the endogenous ligand, acetylated lysine, and that this accounts for its pharmacological activity. Apabetalone increases Apolipoprotein A-I (ApoA-I) production through an epigenetic mechanism and suggests that BET inhibition may be a promising new approach to the treatment of atherosclerosis. Apabetalone increases ApoA-I expression in liver cells[2].

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

    In the atherosclerosis prophylactic treatment study design, mice are fed a Western diet concurrent with the treatment with 150 mg/kg/dose b.i.d. for 12 weeks. Mice are sacrificed at 12 weeks after treatment. There is a progressive increase in body weight in both the vehicle treated as well as the Apabetalone (RVX-208) treated groups. However, there is only an increase of 4 g (from 24 g to 28 g) body weight after 12 weeks on Western diet in the Apabetalone treated group whereas this increase is found to be 9 g (25 g-34 g) in the vehicle treated group. The significant decrease in body weight gain in Apabetalone treated mice is not due to decreased feed consumption, suggesting a positive attribute of the molecule. Plasma lipid measurements are done at 6 weeks and 12 weeks of treatment with either the vehicle or Apabetalone. Compared to the vehicle control animals, Apabetalone treated mice show significant increase (~200%) in the levels of HDL-C at 6 weeks of treatment, which is sustained until end of the study (12 weeks)[3].

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

    370.40

    Formula

    C20H22N2O5
    CAS 號
    性狀

    固體

    顏色

    White to yellow

    中文名稱

    阿帕他隆
    運輸條件

    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 1 year
    -20°C 6 months
    溶解性數(shù)據(jù)
    細(xì)胞實驗： 

    DMSO 中的溶解度 : ≥ 33 mg/mL (89.09 mM; 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)

    * "≥" means soluble, but saturation unknown.

    配制儲備液
    濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg
    1 mM 2.6998 mL 13.4989 mL 26.9978 mL
    5 mM 0.5400 mL 2.6998 mL 5.3996 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, 1 year; -20°C, 6 months。-80°C儲存時，請在1年內(nèi)使用， -20°C儲存時，請在6個月內(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

    動物實驗：

    請根據(jù)您的 實驗動物和給藥方式 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： 10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.5 mg/mL (6.75 mM); 澄清溶液

      此方案可獲得 ≥ 2.5 mg/mL（飽和度未知）的澄清溶液。

      以 1 mL 工作液為例，取 100 μL 25.0 mg/mL 的澄清 DMSO 儲備液加到 400 μL PEG300 中，混合均勻；再向上述體系中加入 50 μL Tween-80，混合均勻；然后再繼續(xù)加入 450 μL 生理鹽水 定容至 1 mL。

      生理鹽水的配制：將 0.9 g 氯化鈉，溶解于 ddH?O 并定容至 100 mL，可以得到澄清透明的生理鹽水溶液。
    • 方案 二

      請依序添加每種溶劑： 10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.5 mg/mL (6.75 mM); 澄清溶液

      此方案可獲得 ≥ 2.5 mg/mL（飽和度未知）的澄清溶液。

      以 1 mL 工作液為例，取 100 μL 25.0 mg/mL 的澄清 DMSO 儲備液加到 900 μL 20% 的 SBE-β-CD 生理鹽水水溶液 中，混合均勻。

      2 g SBE-β-CD（磺丁基醚 β-環(huán)糊精）粉末定容于 10 mL 的生理鹽水中，完全溶解至澄清透明。

    以下溶解方案，請直接配制工作液。建議現(xiàn)用現(xiàn)配，在短期內(nèi)盡快用完。 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： 50% PEG300    50% Saline

      Solubility: 15.15 mg/mL (40.90 mM); 懸濁液; 超聲助溶

    動物溶解方案計算器
    請輸入動物實驗的基本信息：

    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: 99.47%

    參考文獻(xiàn)
    Cell Assay
    [2]

    Huh7 cells are plated at 23,000/well in a 96 well plate in DMEM+10% FBS before allowing to grow overnight. Cells are treated with compounds for 48 h in 0.1% DMSO with or without 5 μM Actinomycin D. U937 cells are differentiated for 3 days in 60 ng/mL PMA, 32,000 cells/well in 96-well format. Cells are then treated with compound in 0.1% DMSO in RPMI media+10% FBS, and after 1 h, lipopolysaccharide is added to the cells at 1 μg/mL for 3 hours[2].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [3]

    Mice[3]
    Seven to eight week old male ApoE-/- mice are used. Based on the body weight and lipid values, mice are divided into 2 groups (n=12): group 1, vehicle; and group 2, test agent, Apabetalone. Mice are then switched to Western diet (0.15% cholesterol and 42% calories from fat) and concurrently treated orally by gavage with either vehicle or the test agent, Apabetalone (150 mg/kg/dose b.i.d) for 12 weeks. After 6 week of treatment, an interim blood draw is done to monitor serum lipid levels. After 12 weeks of treatment mice are sacrificed to measure blood lipid parameters, aortic lesion, and liver and aortic RNA. Eight mice are used for enface (aortic plaque) analysis, 4 mice for tissue collection for mRNA and all 12 mice used for aortic sinus lesion area measurement.

    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, 1 year; -20°C, 6 months。-80°C儲存時，請在1年內(nèi)使用， -20°C儲存時，請在6個月內(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 2.6998 mL 13.4989 mL 26.9978 mL 67.4946 mL
    5 mM 0.5400 mL 2.6998 mL 5.3996 mL 13.4989 mL
    10 mM 0.2700 mL 1.3499 mL 2.6998 mL 6.7495 mL
    15 mM 0.1800 mL 0.8999 mL 1.7999 mL 4.4996 mL
    20 mM 0.1350 mL 0.6749 mL 1.3499 mL 3.3747 mL
    25 mM 0.1080 mL 0.5400 mL 1.0799 mL 2.6998 mL
    30 mM 0.0900 mL 0.4500 mL 0.8999 mL 2.2498 mL
    40 mM 0.0675 mL 0.3375 mL 0.6749 mL 1.6874 mL
    50 mM 0.0540 mL 0.2700 mL 0.5400 mL 1.3499 mL
    60 mM 0.0450 mL 0.2250 mL 0.4500 mL 1.1249 mL
    80 mM 0.0337 mL 0.1687 mL 0.3375 mL 0.8437 mL
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    產(chǎn)品名稱：
    Apabetalone
    目錄號：
    HY-16652
    需求量：