Powder: -20°C for 3 years | In solvent: -80°C for 1 year
2-Methoxyestradiol (2-ME2) 是一种口服生物可利用的雌二醇代谢物,具有抗肿瘤活性。它通过减少内皮细胞增殖和诱导内皮细胞凋亡来抑制血管生成,也可破坏微管的稳定。它可诱导半胱天冬酶活化,导致细胞周期停滞在 G2 期、DNA 断裂和细胞凋亡。
产品描述 | 2-Methoxyestradiol (2-ME2) is an orally bioavailable estradiol metabolite with potential antineoplastic activity. 2-Methoxyestradiol inhibits angiogenesis by reducing endothelial cell proliferation and inducing endothelial cell apoptosis. This agent also inhibits tumor cell growth by binding to tubulin, resulting in antimitotic activity, and by inducing caspase activation, resulting in cell cycle arrest in the G2 phase, DNA fragmentation, and apoptosis. |
体外活性 | 2-Methoxyestradiol(60 mg/kg/day)可使肿瘤降低4倍,若剂量提高10倍则使之降低23倍.2-Methoxyestradiol对9L大鼠胶质瘤模型(9L-V6R)疗效呈剂量依赖性,使HIF-1活性显著降低,且抑制肿瘤生长. |
体内活性 | 2-Methoxyestradiol(0.5 μM)对TGF-β3诱导胶原(Col)I型(αI)、Col III(αI)、结缔组织生长因子、纤溶酶原激活物抑制剂和α-平滑肌肌动蛋白表达具有阻断作用。 作用于MDA-MB-231细胞时,2-Methoxyestradiol对HIF-1调节的靶基因转录激活有抑制作用,对HIF-1α自身转录无影响。作用于乳腺癌细胞系 MDA-MB-435(IC50:1.38 μM)和卵巢癌细胞系SK-OV-3(IC50:1.79 μM)时,2-Methoxyestradiol抑制细胞增殖。此外, 作用于大鼠主动脉平滑肌A-10细胞时,2-Methoxyestradio可抑制细胞微管解聚(EC50:7.5 μM)。其还减轻TGF-β3诱导的Smad2/3磷酸化和核易位,且对TGF-β3诱导的PI3K/Akt/mTOR通路激活具有抑制作用。2-Methoxyestradiol对MCF-7(IC50:52 μM)和BM(IC50:8 μM)细胞增殖有抑制作用。 |
激酶实验 | Microtubule depolymerizing activity: The effects of 2-Methoxyestradiol on cellular microtubule depolymerization are determined by indirect immunofluorescence techniques in rat aortic smooth muscle A-10 cells. Microtubules are visualized using a β-tubulin antibody. Three viewers determines the percent microtubule loss for each treatment concentration. The data are averaged and plotted as percent microtubule loss versus drug concentration and the EC50s for microtubule depolymerization calculated from the log dose–response curves. |
细胞实验 | The sulforhodamine B (SRB) assay is used to evaluate the antiproliferative activity of 2-Methoxyestradiol in the MDA-MB-435 and SK-OV-3 cell lines. Cells a plated into 96-well plates and allowed to grow and attach for 24 hours followed by addition of 2-Methoxyestradiol or vehicle controls. The cells are incubated with drugs for 48 hours and then the cellular protein is fixed, stained, and concentration determined by absorbance at 560 nm. Log dose–response curves are constructed for each experiment and the IC50 for inhibition of proliferation determined.(Only for Reference) |
别名 | 2-甲氧雌二醇, 二甲氧基雌二醇, NSC-659853, 2-MeOE2, 2-ME2 |
分子量 | 302.41 |
分子式 | C19H26O3 |
CAS No. | 362-07-2 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 15.1 mg/mL (50 mM)
可选溶剂 | 浓度 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 | |
20 mM | 0.1653 mL | 0.8267 mL | 1.6534 mL | 4.1335 mL | |
50 mM | 0.0661 mL | 0.3307 mL | 0.6614 mL | 1.6534 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
2-Methoxyestradiol 362-07-2 Angiogenesis Apoptosis Autophagy Chromatin/Epigenetic Cytoskeletal Signaling Immunology/Inflammation Metabolism NF-Κb Reactive Oxygen Species Microtubule Associated Endogenous Metabolite HIF 2-甲氧雌二醇 二甲氧基雌二醇 NSC-659853 2-MeOE2 2Methoxyestradiol NSC 659853 Microtubule/Tubulin Inhibitor 2 Methoxyestradiol NSC659853 inhibit 2-ME2 inhibitor