2. Cell Cycle/DNA Damage Epigenetics Autophagy Apoptosis
  3. HDAC Autophagy Apoptosis
  4. Entinostat

Entinostat  (Synonyms: 恩替诺特; MS-275; SNDX-275)

目录号: HY-12163 纯度: 99.82%
COA 产品使用指南

摩尔计算器

Entinostat 选择性，可口服的 HDAC class I 抑制剂，抑制 HDAC1，HDAC2 和 HDAC3 的 IC50 分别为 243 nM，453 nM 和 248 nM。

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Entinostat Chemical Structure

Entinostat Chemical Structure

CAS No. : 209783-80-2

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Customer Review

Other Forms of Entinostat:

Entinostat 相关抗体

Top Publications Citing Use of Products

MCE 顾客使用本产品发表的 51 篇科研文献

Proliferation Assay
WB

    Entinostat purchased from MCE. Usage Cited in: PLoS One. 2018 Jul 6;13(7):e0200015.  [Abstract]

    Western blot analysis of AcH3 and H3 in HCC827 whole cell lysate. Cells are treated with Entinostat (Ent) for 4 days in vitro. Band densities are determined with a Luminescent Image Analyzer LAS-3000, and AcH3 densities are normalized by H3.

    Entinostat purchased from MCE. Usage Cited in: Carcinogenesis. 2015 Feb;36(2):192-201.  [Abstract]

    Entinostat shows a mild inhibitory effect on cell growth.

    查看 HDAC 亚型特异性产品:

    查看所有亚型
    HDAC HDAC1 HDAC2 HDAC3 HDAC4 HDAC5 HDAC6 HDAC7 HDAC8 HDAC9 HDAC10 HDAC11 HD1 HD2

    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    Entinostat is an oral and selective class I HDAC inhibitor, with IC50s of 243 nM, 453 nM, and 248 nM for HDAC1, HDAC2, and HDAC3, respectively.

    IC50 & Target[1]

    HDAC1

    243 nM (IC50)

    HDAC3

    248 nM (IC50)

    HDAC2

    453 nM (IC50)

    体外研究
    (In Vitro)

    Binding affinity of Entinostat (MS-275) against HDAC1 and HDAC2 is 282 nM and 156 nM, respectively[1]. Effects of the HDAC inhibitor Entinostat (MS-275) have been examined in human leukemia and lymphoma cells (U937, HL-60, K562, and Jurkat) as well as in primary acute myelogenous leukemia blasts in relation to differentiation and apoptosis. MS-275 displays dose-dependent effects in each of the cell lines. When administered at a low concentration (e.g., 1 μM), MS-275 exhibits potent antiproliferative activity, inducing p21CIP1/WAF1-mediated growth arrest and expression of differentiation markers (CD11b) in U937 cells. Entinostat (MS-275) potently induces cell death, triggering apoptosis in ~70% of cells at 48 h[2].

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

    Entinostat 相关抗体:
    体内研究
    (In Vivo)

    Entinostat (MS-27-275) at 49 mg/kg shows marked antitumor effects against KB-3-1, 4-1St, and St-4 tumor lines, and a moderate effect against Capan-1 tumor. Entinostat at 24.5 mg/kg and 12.3 mg/kg also shows significant effects against these tumors. In addition, oral administration of Entinostat apparently increases the level of histone acetylation in HT-29 tumor xenografts 4-24 h after the administration[3]. MS-275 administration (3.5 mg/kg i.p.) to Experimental autoimmune neuritis (EAN) rats once daily from the appearance of first neurological signs greatly reduces the severity and duration of EAN and attenuated local accumulation of macrophages, T cells and B cells, anddemyelination of sciatic nerves. In addition, MS-275 treatment increases proportion of infiltrated Foxp3+ cells and anti-inflammatory M2 macrophages in sciatic nerves of EAN rats[4].

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

    376.41

    Formula

    C21H20N4O3
    CAS 号
    性状

    固体

    颜色

    White to light yellow

    中文名称

    恩替诺特
    运输条件

    Room temperature in continental US; may vary elsewhere.
    储存方式
    Powder -20°C 3 years
    In solvent -80°C 1 year
    -20°C 6 months
    溶解性数据
    细胞实验： 

    DMSO 中的溶解度 : 50 mg/mL (132.83 mM; 超声助溶 (<60°C); 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 2.6567 mL 13.2834 mL 26.5668 mL
    5 mM 0.5313 mL 2.6567 mL 5.3134 mL
    查看完整储备液配制表

    * 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；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
    储备液的保存方式和期限：-80°C, 1 year; -20°C, 6 months。-80°C储存时，请在1年内使用， -20°C储存时，请在6个月内使用。

    • 摩尔计算器

    • 稀释计算器

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

    质量
    =
    浓度
    ×
    体积
    ×
    分子量 *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    浓度 (start)

    C1

    ×
    体积 (start)

    V1

    =
    浓度 (final)

    C2

    ×
    体积 (final)

    V2

    动物实验：

    请根据您的 实验动物和给药方式 选择适当的溶解方案。

    以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：
    ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
    以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

    • 方案 一

      请依序添加每种溶剂： 5% DMSO    40% PEG300    5% Tween-80    50% Saline

      Solubility: ≥ 2.5 mg/mL (6.64 mM); 澄清溶液

    • 方案 二

      请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.08 mg/mL (5.53 mM); 澄清溶液

      此方案可获得 ≥ 2.08 mg/mL（饱和度未知）的澄清溶液。

      以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水 定容至 1 mL。

      生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。
    动物溶解方案计算器
    请输入动物实验的基本信息：

    给药剂量

    mg/kg

    动物的平均体重

    g

    每只动物的给药体积

    μL

    动物数量

    只
    由于实验过程有损耗，建议您多配一只动物的量
    请输入您的动物体内配方组成：
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    如果您的动物是免疫缺陷鼠或者体弱鼠，建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
    方案所需 助溶剂 包括：DMSO， ，均可在 MCE 网站选购。 ，Tween 80，均可在 MCE 网站选购。
    计算结果
    工作液所需浓度 : mg/mL
    储备液配制方法 : mg 药物溶于 μL  DMSO（母液浓度为 mg/mL）。
    您所需的储备液浓度超过该产品的实测溶解度，以下方案仅供参考，如有需要，请与 MCE 中国技术支持联系。
    动物实验体内工作液的配制方法 : 取 μL DMSO 储备液，加入 μL 。 μL ，混合均匀至澄清，再加 μL Tween 80，混合均匀至澄清，再加 μL 生理盐水。
    连续给药周期超过半月以上，请谨慎选择该方案。
    请确保第一步储备液溶解至澄清状态，从左到右依次添加助溶剂。您可采用超声加热 （超声清洗仪，建议频次 20-40 kHz），涡旋吹打等方式辅助溶解。
    纯度 & 产品资料

    纯度: 99.82%

    COA (190 KB) LCMS (92 KB) 元素分析报告 (206 KB)

    产品使用指南 (1538 KB)
    参考文献
    Kinase Assay
    [1]

    Biochemical assays of HDAC activity are carried out by Nanosyn in a reaction volume of 10 μL in 384-well microplates. A standard enzymatic reaction contains 5 μL of 2× HDAC inhibitor (e.g., Entinostat), 4 μL of 2.5× enzyme, and 1 μL of 10× substrate in assay buffer (100 mM HEPES, pH 7.5, 25 mM KCl, 0.1% BSA, 0.01% Triton X-100, 1% DMSO). Final concentration of all HDACs in the enzymatic assays is between 0.5 and 5 nM. A final substrate concentration of 1 μM FAM-RHKK(Ac)-NH2 or FAM-RHKK(trifluoroacetyl)-NH2 is used in all assays and found to be below the determined Km,app for each enzyme[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Cell Assay
    [1]

    SH-SY5Y cells are maintained under normal culture conditions in a humidified incubator at 37°C with 5% CO2 and are split twice weekly. Cells are plated in black 384-well plates at 2500 cells/well in 20-μL volume of DMEM/F-12 culture media supplemented with 10% FBS and permitted to adhere overnight. The following day, HDAC inhibitors (e.g., Entinostat) are serially diluted in 100% DMSO, and this series is subsequently cross-diluted into culture media. 5 μL of compound (e.g., Entinostat) diluted in media is added to the appropriate well of the cell plate to afford the indicated final concentration of inhibitor (e.g., Entinostat) with a final 0.1% DMSO. Treated cells are incubated under normal tissue culture conditions for 6, 24, 48, 72, or 96 h prior to quantitation of cellular ATP levels as measured using CellTiter-Glo reagents. Similarly, after 6 h of incubation with HDAC inhibitors (e.g., Entinostat), media from separate cell plates are aspirated, and cells are washed once with media containing no inhibitors. 25 μL of media supplemented with 10% FBS and 0.1% DMSO (no inhibitors) is added back to the cells, and cellular ATP levels are determined using CellTiter-Glo after 24, 48, 72, or 96 h of incubation. Luminescence is measured at each time point using an Envision Instrument with a 0.1 s count time[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [3][4]

    Mice[3]
    A2780 cells (9×106) are suspended in PBS and are injected subcutaneously into the flank of nude mouse. For the other tumor lines, KB-3-1, HCT-15, 4-1St, Calu-3, St-4, Capan-1, and HT-29, tumors are passaged several times before starting in vivo antitumor testing, and a tumor lump (2-3 mm in diameter) is transplanted subcutaneously into the flank of a nude mouse by using a trocar needle. Treatment (four or five mice in each experimental group) with the drugs is started after the tumors are confirmed to have grown in the body (tumor size, 20-100 mm3). Entinostat is administered orally once daily 5 days per week for 4 weeks. Tumor length and width are monitored twice weekly, and tumor volume is calculated.
    Rats[4]
    Male Lewis rats (8-10 weeks, 170-200 g) are housed under a 12-h light/dark cycle with free access to food and water. For therapeutic treatment, EAN rats receive i.p. injection of MS-275 (3.5 mg/kg) daily from day 10 to day 14 (six rats/group). For injection, MS-275 is suspended in phosphate buffered saline (PBS) and the same volume (1 mL) of PBS is given to control rats.

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

    Entinostat 相关分类

    完整储备液配制表

    * 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；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
    储备液的保存方式和期限：-80°C, 1 year; -20°C, 6 months。-80°C储存时，请在1年内使用， -20°C储存时，请在6个月内使用。

    可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.6567 mL 13.2834 mL 26.5668 mL 66.4169 mL
    5 mM 0.5313 mL 2.6567 mL 5.3134 mL 13.2834 mL
    10 mM 0.2657 mL 1.3283 mL 2.6567 mL 6.6417 mL
    15 mM 0.1771 mL 0.8856 mL 1.7711 mL 4.4278 mL
    20 mM 0.1328 mL 0.6642 mL 1.3283 mL 3.3208 mL
    25 mM 0.1063 mL 0.5313 mL 1.0627 mL 2.6567 mL
    30 mM 0.0886 mL 0.4428 mL 0.8856 mL 2.2139 mL
    40 mM 0.0664 mL 0.3321 mL 0.6642 mL 1.6604 mL
    50 mM 0.0531 mL 0.2657 mL 0.5313 mL 1.3283 mL
    60 mM 0.0443 mL 0.2214 mL 0.4428 mL 1.1069 mL
    80 mM 0.0332 mL 0.1660 mL 0.3321 mL 0.8302 mL
    100 mM 0.0266 mL 0.1328 mL 0.2657 mL 0.6642 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.

    Keywords:

    Entinostat209783-80-2MS-275 SNDX-275恩替诺特MS275MS 275SNDX275SNDX 275SNDX-275HDACAutophagyApoptosisHistone deacetylasesInhibitorinhibitorinhibit

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