2-Methoxyestradiol (2-MeOE2)
(Synonyms: 二甲氧基雌二醇; 2-ME2; NSC-659853) 目录号 : GC15084
2-Methoxyestradiol (2-MeOE2/2-Me)是一种HIF-1α抑制剂。
Cas No.:362-07-2
Sample solution is provided at 25 µL, 10mM.
2-Methoxyestradiol (2-MeOE2/2-Me) is an HIF-1α inhibitor. It can inhibit the accumulation of HIF-1α nuclei and the transcription activity of HIF[1-3] .2-ME can trigger p53-induced apoptosis through 2 mechanisms: activation of P38 and NF-κB as well as activation of JNK and AP-1 which leads to phosphorylation of Bcl-2. It prevents mitosis of tumor cell by inhibiting tubulin assembly, destabilizing microtubules, and interfering with spindle mitosis. As an apoptosis inducer and an angiogenesis inhibitor with potential antineoplastic activity[4].
2-Methoxyestradiol (10 µg/mL;1-4days) treatment significantly inhibited the proliferation ability of B16 melanoma cells[5]. 2-Methoxyestradiol (0.03-33mM) abolished L-lactate-induced migration and proliferation of osteosarcoma cells[6].
2-Methoxyestradiol (30 mg/kg;i.p/p.o; 7days/3weeks) treatment prior to and post irradiation inhibited Radiation-induced skin injury (RISI) on the skin of C57/BL6 mice. 2-ME also reduced radiation-induced inflammation, skin thickness, and vascular fibrosis[7].
References:
[1]. Lakhani NJ, Sarkar MA, et,al. 2-Methoxyestradiol, a promising anticancer agent. Pharmacotherapy. 2003 Feb;23(2):165-72. doi: 10.1592/phco.23.2.165.32088. PMID: 12587805.
[2]. Ricker JL, Chen Z, et,al. 2-methoxyestradiol inhibits hypoxia-inducible factor 1alpha, tumor growth, and angiogenesis and augments paclitaxel efficacy in head and neck squamous cell carcinoma. Clin Cancer Res. 2004 Dec 15;10(24):8665-73. doi: 10.1158/1078-0432.CCR-04-1393. PMID: 15623651.
[3]. Tevaarwerk, A.J.; Holen, K.D.; et,al. Phase I trial of 2-Methoxyestradiol NanoCrystal dispersion in advanced solid malignancies. Clin. Cancer Res. 2009, 15, 1460-1465.
[4]. Fotsis T, Zhang Y, et,al. The endogenous oestrogen metabolite 2-methoxyoestradiol inhibits angiogenesis and suppresses tumour growth. Nature. 1994 Mar 17;368(6468):237-9. doi: 10.1038/368237a0. PMID: 7511798.
[5]. Hua W, Huang X, et,al. 2-methoxyestradiol inhibits melanoma cell growth by activating adaptive immunity. Immunopharmacol Immunotoxicol. 2022 Aug;44(4):541-547. doi: 10.1080/08923973.2022.2062380. Epub 2022 Apr 22. PMID: 35451929.
[6]. Gorska-Ponikowska M, Kuban-Jankowska A, et,al. 2-Methoxyestradiol Reverses the Pro-Carcinogenic Effect of L-Lactate in Osteosarcoma 143B Cells. Cancer Genomics Proteomics. 2017 Nov-Dec;14(6):483-493. doi: 10.21873/cgp.20058. PMID: 29109098; PMCID: PMC6070326.
[7]. Kim JH, Nam JK, et,al. 2-Methoxyestradiol Inhibits Radiation-Induced Skin Injuries. Int J Mol Sci. 2022 Apr 10;23(8):4171. doi: 10.3390/ijms23084171. PMID: 35456989; PMCID: PMC9032705.
2-Methoxyestradiol (2-MeOE2/2-Me)是一种HIF-1α抑制剂。它可以抑制HIF-1α核的聚集和HIF的转录活性[1-3]。2-Methoxyestradiol可通过激活P38和NF-κB以及激活JNK和AP-1导致Bcl-2磷酸化两种机制触发p53诱导的细胞凋亡。它通过抑制微管蛋白组装、破坏微管稳定和干扰纺锤体有丝分裂来阻止肿瘤细胞的有丝分裂。作为细胞凋亡诱导剂和血管生成抑制剂,具有潜在的抗肿瘤活性[4]。
2-Methoxyestradiol(10 µg/mL;1-4days)处理显著抑制B16黑色素瘤细胞的增殖能力[5]。2-Methoxyestradiol (0.03-33mM)可消除L-乳酸诱导的骨肉瘤细胞的迁移和增殖[6]。
2-Methoxyestradiol (30 mg/kg;i.p/p.o; 7days/3weeks)辐照前后对C57/BL6小鼠皮肤的辐射性皮肤损伤(RISI)有抑制作用。2-ME还能减少辐射引起的炎症、皮肤厚度和血管纤维化[7]。
| Cell experiment [1]: | |
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Cell lines |
B16 cells |
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Preparation Method |
B16 cells were plated in 96-well plates (1000 cells per well) and treated with 2-Methoxyestradiol (10 µg/mL) after cell adherence. CCK8 assay was performed at day 1, 2, 3, and 4 after treatment. |
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Reaction Conditions |
10 µg/mL;1-4days |
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Applications |
2-Methoxyestradiol treatment significantly inhibited the proliferation ability of B16 melanoma cells. |
| Animal experiment [2]: | |
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Animal models |
C57BL/6 mice |
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Preparation Method |
Mice skin were irradiated with 17 and 20 Gy using a 4-cm field. 2-Methoxyestradiol was injected into the irradiation group. |
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Dosage form |
30 mg/kg;i.p/p.o; 7days/3weeks |
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Applications |
2-Methoxyestradiol inhibits radiation-induced skin vascular injuries, perivascular collagen deposition, and upregulated HIF-1α expression. |
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References: [1]. Hua W, Huang X, et,al. 2-methoxyestradiol inhibits melanoma cell growth by activating adaptive immunity. Immunopharmacol Immunotoxicol. 2022 Aug;44(4):541-547. doi: 10.1080/08923973.2022.2062380. Epub 2022 Apr 22. PMID: 35451929. |
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| Cas No. | 362-07-2 | SDF | |
| 别名 | 二甲氧基雌二醇; 2-ME2; NSC-659853 | ||
| 化学名 | (8R,9S,13S,14S,17S)-2-methoxy-13-methyl-6,7,8,9,11,12,14,15,16,17-decahydrocyclopenta[a]phenanthrene-3,17-diol | ||
| Canonical SMILES | CC12CCC3C(C1CCC2O)CCC4=CC(=C(C=C34)OC)O | ||
| 分子式 | C19H26O3 | 分子量 | 302.41 |
| 溶解度 | ≥ 15.25 mg/mL in DMSO, ≥ 24.25 mg/mL in EtOH with ultrasonic | 储存条件 | Store at -20°C |
| General tips | 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 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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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 |
| 10 mM | 0.3307 mL | 1.6534 mL | 3.3068 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
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