1. Epigenetics
  2. Histone Methyltransferase
  3. EZM 2302

EZM 2302是共激活因子相关的精氨酸甲基转移酶1 (CARM1) 制剂, IC50值为6 nM。

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EZM 2302 Chemical Structure

EZM 2302 Chemical Structure

CAS No. : 1628830-21-6

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥2092
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1 mg ¥740
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5 mg ¥1625
In-stock
10 mg ¥2450
In-stock
25 mg ¥4100
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50 mg ¥5850
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100 mg ¥8150
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200 mg   询价  
500 mg   询价  

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Customer Review

    EZM 2302 purchased from MCE. Usage Cited in: Aging (Albany NY). 2020 Jun 2;12(11):10578-10593.  [Abstract]

    The Western blot results show that EZM2302 (10 nM) inhibits the enzymatic activity of CARM1 and CARM2, leading to significantly reduced H3R17me2a and H3R26me2a levels.
    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    EZM 2302 is an inhibitor of coactivator-associated arginine methyltransferase 1 (CARM1) with an IC50 of 6 nM.

    IC50 & Target

    IC50: 6 nM (CARM1)[1]

    体外研究
    (In Vitro)

    EZM 2302 binds to CARM1 and is a selective inhibitor of CARM1 activity (IC50=6 nM) with broad selectivity against other histone methyltransferases. Treatment of MM cell lines with EZM 2302 leads to inhibition of PABP1 and SMB methylation and cell stasis with IC50 values in the nanomolar range (9, 31 nM, respectively). EZM 2302 inhibits the in vitro proliferation of multiple hematopoietic cell lines, with day 14 IC50 values of less than 100 nM in 9 of 15 cell lines[1].

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

    体内研究
    (In Vivo)

    EZM 2302 is stable in human hepatocytes (CL<3 mL/min/kg), and moderately binds to human, mouse and rat plasma proteins with a mean fraction unbound of 0.66, 0.46 and 0.74, respectively. In mouse and rat, the plasma clearance (CL) is 43 and 91 mL/min/kg, respectively. EZM 2302 shows dose-dependent exposure and tumor growth inhibition (TGI) after 21 days in the RPMI-8226 xenograft model. Tumors in all EZM 2302 dose groups measured on day 21 show significant decreases in tumor growth compared to vehicle[1].

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

    分子量

    585.09

    Formula

    C29H37ClN6O5

    CAS 号
    性状

    固体

    颜色

    White to off-white

    运输条件

    Room temperature in continental US; may vary elsewhere.

    储存方式
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 1 year
    -20°C 6 months
    溶解性数据
    细胞实验: 

    DMSO 中的溶解度 : 100 mg/mL (170.91 mM; 超声助溶; 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 1.7091 mL 8.5457 mL 17.0914 mL
    5 mM 0.3418 mL 1.7091 mL 3.4183 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: 10% DMSO    90% Corn Oil

      Solubility: ≥ 2.5 mg/mL (4.27 mM); 澄清溶液

      此方案可获得 ≥ 2.5 mg/mL(饱和度未知)的澄清溶液,此方案实验周期在半个月以上的动物实验酌情使用。

      1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

    • 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 (3.56 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。

      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

    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: 99.59%

    参考文献
    Cell Assay
    [1]

    Cultured cells in linear/log phase growth are split to a seeding density of 2e5 cells/mL in 2–20mLs of media, depending on the yield required at the end of the growth period. EZM 2302 is diluted in DMSO and added to each culture vessel with a final DMSO concentration of 0.2%. Cells are allowed to grow for 96 hours. At the conclusion of each treatment period, cells are harvested by centrifugation (5 minutes, 1200 rpm), and cell pellets are rinsed once with PBS before being frozen on dry ice pending further processing[1].

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

    Animal Administration
    [1]

    Rats[1]

    Male Sprague-Dawley rats (n=3) are treated with a single dose of EZM2302 at 2 mg/kg by intravenous (i.v.) injection and 10 mg/kg by oral gavage administration (p.o.; mouse only), formulated in 5% dextrose in water, pH 3.5. An additional group of rats, cannulated in both the jugular and portal veins are dosed by oral gavage (10 mg/kg, in 0.5% methylcellulose in water). Approximately 110 μL of blood is taken from the animals by retro-orbital bleeding (mouse), tail vein (rat i.v.) or both jugular and portal vein sampling (rat p.o.) at pre-specified time intervals. The 2 h samples are split for parallel determination of blood and plasma concentration[1].

    Mice[1]

    RPMI-8226 cells are inoculated at 5×106 cells/mouse and treatment began when the mean tumor sizes reach 120 mm3 (28 days post-inoculation). CB-17 SCID Mice are assigned into groups using a randomized block design. EZM2302 or vehicle (0.5% methylcellulose in water) is administered orally BID at a dose volume of 37.5, 75, 150, or 300 mg/kg for 21 days. Body weights are measured twice a week for the duration of the study. Tumor size is measured twice weekly in two dimensions using a caliper, and the volume is expressed in cubic millimeters. Animals are euthanized 3 hours post-final dose, with blood and tissues collected for analysis[1].

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

    参考文献

    EZM 2302 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 1.7091 mL 8.5457 mL 17.0914 mL 42.7285 mL
    5 mM 0.3418 mL 1.7091 mL 3.4183 mL 8.5457 mL
    10 mM 0.1709 mL 0.8546 mL 1.7091 mL 4.2728 mL
    15 mM 0.1139 mL 0.5697 mL 1.1394 mL 2.8486 mL
    20 mM 0.0855 mL 0.4273 mL 0.8546 mL 2.1364 mL
    25 mM 0.0684 mL 0.3418 mL 0.6837 mL 1.7091 mL
    30 mM 0.0570 mL 0.2849 mL 0.5697 mL 1.4243 mL
    40 mM 0.0427 mL 0.2136 mL 0.4273 mL 1.0682 mL
    50 mM 0.0342 mL 0.1709 mL 0.3418 mL 0.8546 mL
    60 mM 0.0285 mL 0.1424 mL 0.2849 mL 0.7121 mL
    80 mM 0.0214 mL 0.1068 mL 0.2136 mL 0.5341 mL
    100 mM 0.0171 mL 0.0855 mL 0.1709 mL 0.4273 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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    产品名称:
    EZM 2302
    目录号:
    HY-111109
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