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2-甲氧基雌二醇

高效抗肿瘤和抗血管生成剂
规格或纯度: ≥98%
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货号 (SKU) 包装规格 是否现货 价格 数量
M125960-10mg
 10mg 现货 Stock Image
M125960-25mg
 25mg 现货 Stock Image
M125960-50mg
 50mg 现货 Stock Image
M125960-100mg
 100mg 现货 Stock Image
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基本描述

别名 2-甲氧基雌二醇 | 2-甲氧基-β-雌二醇
英文别名 2-MeOE2 | 2-Methoxyestradiol | 2-ME2 | NSC-659853 | 2-Methoxy-β-estradiol
规格或纯度 ≥98%
英文名称 2-Methoxyestradiol (2-MeOE2)
生化机理 2-methoxyestradiol (2ME2) is a natural metabolite of estrogen that is known to inhibit HIF-1 alpha with an IC50 of 0.71 ± 0.11 μM for the inhibition of BPAEC migration.2-Methoxyestradiol is an endogenous estrogen metabolite with low affinity for the estrogen receptor but which disrupts microtubule function. 2-Methoxyestradiol is formed by CYP450-mediated hydroxylation followed by catechol-O-methyltransferase (COMT) methylation of estradiol. 2-Methoxyestradiol is a derivative of an oestrogenic steroidal hormone and has demonstrated: potent inhibition of endothelial cell proliferation and migration and inhibition of bFGF and VEGF-induced corneal neovascularization in mice. In MDA-MB-231 cells, 2-Methoxyestradiol inhibits HIF mediated transcriptional activation of target genes without affecting the transcription of HIF-1α itself. 2-Methoxyestradiol has been shown to induce apoptosis throμgh activation of the p53 pathway throμgh either activation of p38 and NF-κ.Potent antioxidant. Inhibits angiogenesis in vivo with direct cytotoxic effects seen in vitro . Interacts with endothelial tubulin dynamics and increases the expression of death receptor 5 in endothelial cells. Induces apoptosis by p53 induction via activ
储存温度 -20°C储存
运输条件 超低温冰袋运输
备注 如果有可能，您尽量在使用的当天配置溶液，并在当天使用完它。但是，如果您需要预先配制储备溶液，我们建议您将溶液等份保存在-20°C的密封小瓶中。通常，它们最多可以使用一个月。在使用前和打开样品瓶之前，我们建议您让您的产品在室温下平衡至少1小时。需要更多关于溶解度，用法和处理的建议吗？请访问我们的常见问题（FAQ）页面以获取更多详细信息。
产品介绍

2-Methoxyestradiol (2-MeOE2)使微管解聚，且抑制HIF-1α核积累和HIF转录活性。Phase 2。A disruptor of microtubule function and HIF-1 inhibitor

最大吸收波长：286(EtOH) nm

2-Methoxyestradiol (2-MeOE2) depolymerizes microtubules and blocks HIF-1α nuclear accumulation and HIF-transcriptional activity. Phase 2.
A disruptor of microtubule function and HIF-1 inhibitor

名称和标识符

IUPAC Name (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
INCHI InChI=1S/C19H26O3/c1-19-8-7-12-13(15(19)5-6-18(19)21)4-3-11-9-16(20)17(22-2)10-14(11)12/h9-10,12-13,15,18,20-21H,3-8H2,1-2H3/t12-,13+,15-,18-,19-/m0/s1
InChi Key CQOQDQWUFQDJMK-SSTWWWIQSA-N
Canonical SMILES CC12CCC3C(C1CCC2O)CCC4=CC(=C(C=C34)OC)O
Isomeric SMILES C[C@]12CC[C@H]3[C@H]([C@@H]1CC[C@@H]2O)CCC4=CC(=C(C=C34)OC)O
WGK Germany 3
RTECS KG7537500
PubChem CID 66414
分子量 302.41

化学和物理性质

溶解性 Soluble in DMSO (10 mg/mL), ethanol (10 mg/mL), chloroform, ethanol (1 mg/ml), and 1:1DMF:PBS(pH7.2) (0.5 mg/ml). Insoluble in water.
比旋光度 107° (C=0.5,THF)
熔点 187 °C

安全和危险性（GHS）

象形图
ghs06

Toxic

ghs08

Health Hazard

ghs09

Environmental Hazard

ghs07

Harmful
信号词 Danger
危险声明 H315: Causes skin irritation
H319: Causes serious eye irritation
H335: May cause respiratory irritation
H301: Toxic if swallowed
H311: Toxic in contact with skin
H331: Toxic if inhaled
H400: Very toxic to aquatic life
H410: Very toxic to aquatic life with long lasting effects
H372: Causes damage to organs through prolonged or repeated exposure
H360: May damage fertility or the unborn child
H350: May cause cancer
H301+H311+H331: Toxic if swallowed, in contact with skin or if inhaled
预防措施声明 P261,P305+P351+P338,P273,P280,P302+P352,P321,P405,P501,P264,P260,P271,P270,P304+P340,P403+P233,P362+P364,P391,P330,P361+P364,P203,P264+P265,P301+P316,P318,P337+P317,P332+P317,P316,P319
WGK Germany 3
RTECS KG7537500
个人防护装备 Eyeshields, Faceshields, full-face particle respirator type N100 (US), Gloves, respirator cartridge type N100 (US), type P1 (EN143) respirator filter, type P3 (EN 143) respirator cartridges

质检证书(COA)

质检报告(COA)

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可替换产品

  1. 2-甲氧基雌二醇
    2-甲氧基雌二醇, 10mM in DMSO, 1ml

    ¥402.90

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参考文献

1. Pribluda VS, Gubish Jr ER, Lavallee TM, Treston A, Swartz GM, Green SJ.  (2000)  2-Methoxyestradiol: an endogenous antiangiogenic and antiproliferative drug candidate..  Cancer Metastasis Rev,  19  (1-2):  (173-9).  [PMID:11191057]
2. Lakhani NJ, Sarkar MA, Venitz J, Figg WD.  (2003)  2-Methoxyestradiol, a promising anticancer agent..  Pharmacotherapy,  23  (2):  (165-72).  [PMID:12587805]
3. Sidor C, D'Amato R, Miller KD.  (2005)  The potential and suitability of 2-methoxyestradiol in cancer therapy..  Clin Cancer Res,  11  (16):  (6094-5).  [PMID:16115955]
4. Dahut WL, Lakhani NJ, Gulley JL, Arlen PM, Kohn EC, Kotz H, McNally D, Parr A, Nguyen D, Yang SX et al..  (2006)  Phase I clinical trial of oral 2-methoxyestradiol, an antiangiogenic and apoptotic agent, in patients with solid tumors..  Cancer Biol Ther,  5  (1):  (22-7).  [PMID:16357512]
5. Koganti S, Snyder R, Thekkumkara T.  (2012)  Pharmacologic effects of 2-methoxyestradiol on angiotensin type 1 receptor down-regulation in rat liver epithelial and aortic smooth muscle cells..  Gend Med,  9  (2):  (76-93).  [PMID:22366193]
6. Thekkumkara T, Snyder R, Karamyan VT.  (2016)  Competitive Binding Assay for the G-Protein-Coupled Receptor 30 (GPR30) or G-Protein-Coupled Estrogen Receptor (GPER)..  Methods Mol Biol,  1366  (13):  (11-17).  [PMID:26585123]
7. Prossnitz ER, Arterburn JB.  (2015)  International Union of Basic and Clinical Pharmacology. XCVII. G Protein-Coupled Estrogen Receptor and Its Pharmacologic Modulators..  Pharmacol Rev,  67  (3):  (505-40).  [PMID:26023144]
8. Liu J et al..  (2019)  CCR7 Chemokine Receptor-Inducible lnc-Dpf3 Restrains Dendritic Cell Migration by Inhibiting HIF-1a-Mediated Glycolysis..  Immunity,  50  (3):  (600-615.e15).  [PMID:30824325]
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