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  3. 2-Methoxyestradiol

2-Methoxyestradiol  (Synonyms: 二甲氧基雌二醇; 2-ME2; NSC-659853)

目录号: HY-12033 纯度: 99.64%
COA 产品使用指南

2-Methoxyestradiol (2-ME2),具有口服活性的 17β-雌二醇 (E2) 的内源性代谢产物,是凋亡 (apoptosis) 诱导剂和血管生成 (angiogenesis) 抑制剂,具有有效的抗肿瘤活性。2-Methoxyestradiol 也可破坏微管 (microtubules) 的稳定。2-Methoxyestradiol 是一种有效的超氧化物歧化酶 (SOD) 抑制剂和活性氧生成剂,可诱导转化细胞系 HEK293、癌细胞系 U87 和 HeLa 的自噬 (autophagy)。

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2-Methoxyestradiol Chemical Structure

2-Methoxyestradiol Chemical Structure

CAS No. : 362-07-2

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Top Publications Citing Use of Products

    2-Methoxyestradiol purchased from MCE. Usage Cited in: Exp Ther Med. 2017 Aug;14(2):1825-1831.  [Abstract]

    HIF 1α regulates the protein levels of RGC 32 and epithelial mesenchymal transition associated genes induced by hypoxia. Proteins are extracted from cells after different treatments. Protein levels of HIF 1α, RGC 32, E cadherin, cytokeratins, N cadherin and vimentin are detected by western blotting. a, no treatment cells under normoxia; b, cells under hypoxia; c, cells are pretreated with HIF 1α inhibitor for 30 min, and then incubated under hypoxia; d, cells are transfected with negative contro

    2-Methoxyestradiol purchased from MCE. Usage Cited in: Cancer Lett. 2016 Nov 1;382(1):44-52.  [Abstract]

    Downregulation of VEGF and HIF-1α by FP08S2 is dependent on Erk inactivation. VEGF and HIF-1α expression at protein level is detected after 2-ME treatment by Western blotting. 18S rRNA is used as internal control in qPCR while GAPDH is used as loading control in Western blotting.

    2-Methoxyestradiol purchased from MCE. Usage Cited in: Cancer Biol Ther. 2016 Jun 2;17(6):625-34.  [Abstract]

    HL-60 and Kasumi-1 cells are treated with different concentration of 2ME2 (0.1, 0.5, 2.5, or 5μM) for 24 hours or diluent control, and intracelluar protein levels are examined by Western blot.
    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    2-Methoxyestradiol (2-ME2), an orally active endogenous metabolite of 17β-estradiol (E2), is an apoptosis inducer and an angiogenesis inhibitor with potent antineoplastic activity. 2-Methoxyestradiol also destablize microtubules. 2-Methoxyestradio, also a potent superoxide dismutase (SOD) inhibitor and a ROS-generating agent, induces autophagy in the transformed cell line HEK293 and the cancer cell lines U87 and HeLa[1][2][3][4][5][6].

    IC50 & Target

    Human Endogenous Metabolite

     

    体外研究
    (In Vitro)

    2-Methoxyestradiol (2-ME) (5-100 μM) 以浓度依赖性方式抑制纯化微管蛋白的组装,在 200 μM 2-Methoxyestradiol (2ME2) 时抑制最大 (60%)。在活的间期 MCF7 细胞中,有丝分裂停滞的 IC50 (1.2 μM),2-Methoxyestradiol 显著抑制平均微管生长速率、持续时间和长度以及整体动态性,这与其在体外的作用一致,并且没有任何可观察到的微管解聚。2-Methoxyestradiol 在许多活跃分裂的细胞类型中诱导 G2-M 停滞和细胞凋亡,同时保护静止细胞。2-Methoxyestradiol 在秋水仙碱位点或附近与微管蛋白结合,抑制微管组装,高浓度已显示可解聚细胞中的微管[1]
    2-Methoxyestradiol (2-ME) 降低缺氧培养细胞中的 HIF-1α 和 HIF-2α 核染色。2-Methoxyestradiol 是一种抗血管生成、抗增殖和促凋亡剂,可抑制 HIF-1α 蛋白水平及其转录活性。与 DMSO 处理的细胞 (分别为 66.2±7.2 和 101.2±2.3%;p=0.04) 相比,在 96 小时时,10 μM 2-Methoxyestradiol 处理的 A549 细胞的生长速率显著降低。与低 O2 浓度下的细胞相比,在常氧条件下用 10 μM 2-Methoxyestradiol 处理的细胞中观察到细胞凋亡显著增加 (5.8±0.2%;p=0.003)[2]

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

    体内研究
    (In Vivo)

    为了研究 2-Methoxyestradiol (2-ME2) 对葡萄膜炎发展的影响,将 C57BL/6 小鼠随机分为两组并用 IRBP 肽进行免疫。2ME2 组从第 0 天到第 13 天开始腹膜内注射 2-Methoxyestradiol (15 mg/kg),而对照组则给予载体。2-Methoxyestradiol (2ME2) 组疾病评分为0.30±0.30,显著低于对照组的2.09±0.28 (p<0.05),每组5只小鼠[3]
    用 2-Methoxyestradiol (60-600 mg/kg/d) 处理会导致肿瘤生长的剂量依赖性抑制。2-Methoxyestradiol 处理组中具有强哌莫硝唑阳性染色 (+++) 的细胞百分比显著降低 (60 mg/kg/d 为 36.0%,200 和 600 mg/kg/d 为 0%) 比较与车辆处理组 (86.5%)。这可能是由于 2-Methoxyestradiol 处理后以剂量依赖性方式显著抑制肿瘤生长[4]

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

    Clinical Trial
    分子量

    302.41

    Formula

    C19H26O3

    CAS 号
    性状

    固体

    颜色

    White to off-white

    中文名称

    二甲氧基雌二醇;二甲氧雌二醇

    结构分类
    初始来源
    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 2 years
    -20°C 1 year
    溶解性数据
    In Vitro: 

    DMSO 中的溶解度 : 250 mg/mL (826.69 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)

    H2O 中的溶解度 : < 0.1 mg/mL (insoluble)

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 3.3068 mL 16.5338 mL 33.0677 mL
    5 mM 0.6614 mL 3.3068 mL 6.6135 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, 2 years; -20°C, 1 year。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

    • 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

    In Vivo:

    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    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.08 mg/mL (6.88 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。
    • 方案 二

      请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.08 mg/mL (6.88 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 900 μL 20% 的 SBE-β-CD 生理盐水水溶液 中,混合均匀。

      20% SBE-β-CD in Saline 的配制(4°C,储存一周):2 g SBE-β-CD(磺丁基醚 β-环糊精)粉末定容于 10 mL 的生理盐水中,完全溶解至澄清透明。
    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: 99.82%

    参考文献
    Kinase Assay
    [1]

    Microtubule protein (2.75 mg/mL) is assembled to steady-state [in 100 mM PIPES containing 1 mM EGTA and 1 mM MgSO4 (PEM100) and 1 mM GTP, 35°C for 45 minutes] containing 2-Methoxyestradiol (final drug concentrations of 1-500 μM). Final DMSO and ethanol concentrations are adjusted to 1% and 5%, respectively. Concentrations of 2-Methoxyestradiol ≤ 5 μM have no effect on microtubule polymer mass, and thus 20 to 500 μM 2-Methoxyestradiol is used for most of the experiments. Incubation with 2-Methoxyestradiol is carried out for 30 minutes, at which time microtubule depolymerization is maximal, and microtubules are centrifuged at 35°C for 30 minutes and the supernatant is removed from the pellets. Microtubule pellets are solubilized overnight in 0.2 M NaOH and the protein concentrations of supernatants and pellets are determined[1].

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

    Cell Assay
    [1]

    MCF7 breast carcinoma cells stably transfected with green fluorescent protein (GFP)-α-tubulin are cultured in DMEM supplemented with nonessential amino acids, 0.1% penicillin/streptomycin, 10% fetal bovine serum, and 0.4 mg/mL G418 at 37°C in 5% CO2. Transfection of MCF7 cells with GFP-α-tubulin is carried out. To evaluate mitotic indices, cells are plated at a concentration of 6×104/2 mL into six-well plates. After 48 hours, cells are incubated in the absence or presence of 2-Methoxyestradiol at concentrations ranging from 100 nM to 30 μM for 20 hours. To collect both floating and attached cells, medium is collected; attached cells are rinsed with Versene (137 mM NaCl, 2.7 mM KCl, 1.5 mM KH2PO4, 8.1 mM Na2HPO4, and 0.5 mM EDTA), detached by trypsinization, and added back to the medium. Cells are collected by centrifugation and fixed with 10% formalin for 30 minutes, permeabilized in ice-cold methanol for 10 minutes, and stained with 4′,6-diamidino-2-phenylindole to visualize nuclei. Results are the mean and SE of seven experiments in each of which 500 cells are counted for each concentration. The mitotic IC50 is the drug concentration that induced one half of the maximal mitotic accumulation[1].

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

    Animal Administration
    [3][4]

    Mice[3]
    6~8-week-old C57BL/6 mice are used. C57BL/6 mice are immunized subcutaneously 0.1 mL at tail and 0.05 mL at both thigh sites with IRBP antigen complex. 500 ng Pertussis toxin is injected concurrently. This day is settled as day 0. Then mice are divided into 4 groups, each group containing 5 mice. 15 mg/kg 2-Methoxyestradiol or vehicle is abdominal injected during 0-13 days, 0-6 days, and 7-13 days. At day 14 eyes or lymphoglandula is collected after euthanasia.
    Rats[4]
    Fischer 344 rats (average body weight=150 g, n=6 per group) are treated with an i.p. injection of the vehicle (60, 200, or 600 mg/kg/d of 2-Methoxyestradiol/Panzem) for nine consecutive days beginning on the 8th day after the initial tumor cell injection. The experiment is repeated a second time using three rats per group.

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

    参考文献

    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, 2 years; -20°C, 1 year。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

    可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 3.3068 mL 16.5338 mL 33.0677 mL 82.6692 mL
    5 mM 0.6614 mL 3.3068 mL 6.6135 mL 16.5338 mL
    10 mM 0.3307 mL 1.6534 mL 3.3068 mL 8.2669 mL
    15 mM 0.2205 mL 1.1023 mL 2.2045 mL 5.5113 mL
    20 mM 0.1653 mL 0.8267 mL 1.6534 mL 4.1335 mL
    25 mM 0.1323 mL 0.6614 mL 1.3227 mL 3.3068 mL
    30 mM 0.1102 mL 0.5511 mL 1.1023 mL 2.7556 mL
    40 mM 0.0827 mL 0.4133 mL 0.8267 mL 2.0667 mL
    50 mM 0.0661 mL 0.3307 mL 0.6614 mL 1.6534 mL
    60 mM 0.0551 mL 0.2756 mL 0.5511 mL 1.3778 mL
    80 mM 0.0413 mL 0.2067 mL 0.4133 mL 1.0334 mL
    100 mM 0.0331 mL 0.1653 mL 0.3307 mL 0.8267 mL
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