2-Methoxyestradiol (2-MeOE2) (Synonyms: 2Hydroxyestradiol 2methyl ether, 2ME2, NSC 659853, Panzem) |
| カタログ番号GC15084 |
2-メトキシエストラジオール(2-MeOE2/2-Me)2-Methoxyestradiol (2-MeOE2)はHIF-1αの阻害剤である。
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Cas No.: 362-07-2
Sample solution is provided at 25 µL, 10mM.
2-メトキシエストラジオール(2-MeOE2/2-Me)2-Methoxyestradiol (2-MeOE2)はHIF-1αの阻害剤である。HIF-1α核の蓄積とHIFの転写活性を阻害できる[1-3]。2-MEは二つのメカニズムを通じてp53誘発性アポトーシスを惹起できる。この二つのメカニズムは：P38とNF-κBの活性、そしてBcl-2のリン酸化を導くJNKとAP-1の活性化である。チューブリンアセンブリを阻害し、微小管を不安定させ、紡錘体の有糸分裂を干渉することで腫瘍細胞の有糸分裂を阻止する。2-メトキシエストラジオールはアポトーシスの誘導体であり、血管新生の阻害剤でもあり、潜在的な抗悪腫瘍活性を持っている[4]。
2-メトキシエストラジオール(10 µg/mL;1-4日間)の処理は、B16悪性黒色腫細胞の増殖能力を著しく阻害した[5]。2-メトキシエストラジオール(0.03-33mM)は骨肉腫細胞のL乳酸誘導性移動と増殖を廃止した[6]。
照射の前後に2-メトキシエストラジオール(30 mg/kg;i.p/p.o; 7日/3週間)を処理したところ、C57/BL6マウスの皮膚における放射線誘発性皮膚損傷(RISI)は阻害された。2-MEは放射線誘発性炎症、皮膚肥厚と心筋線維症をも減らした[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.
| 細胞実験[1]: | |
細胞株 | B16細胞 |
準備方法 | B16細胞を96ウェルプレート(ウェルごとに1000の細胞)に置き、細胞接着後に2-メトキシエストラジオール(10 µg/mL)で処理した。CCK8アッセイは処理後の1、2、3、4日目に実行した。 |
反応条件 | 10 µg/mL;1-4日目 |
アプリケーション | 2-メトキシエストラジオールの処理はB16悪性黒色腫細胞の増殖能力を著しく阻害した。 |
| 動物実験 [2]: | |
動物モデル | C57BL/6マウス |
準備方法 | 4cmのフィルドで、17と20Gyでマウスの皮膚を照射した。2-メトキシエストラジオールを照射グループに注射した。 |
投与形態 | 30 mg/kg;i.p/p.o; 7日/3週間 |
アプリケーション | 2-メトキシエストラジオールは放射線誘発の皮膚導管の損傷、血管周囲のコラーゲンの沈着を阻害し、HIF-1αの発見を上方制御した。 |
| 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. | |
| Cas No. | 362-07-2 | SDF | |
| 同義語 | 2Hydroxyestradiol 2methyl ether, 2ME2, NSC 659853, Panzem | ||
| Chemical 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 | ||
| Canonical SMILES | CC12CCC3C(C1CCC2O)CCC4=CC(=C(C=C34)OC)O | ||
| Formula | C19H26O3 | M.Wt | 302.41 |
| 溶解度 | ≥ 15.25 mg/mL in DMSO, ≥ 24.25 mg/mL in EtOH with ultrasonic | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 3.3068 mL | 16.5338 mL | 33.0677 mL |
| 5 mM | 661.4 μL | 3.3068 mL | 6.6135 mL |
| 10 mM | 330.7 μL | 1.6534 mL | 3.3068 mL |
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- Purity: >98.00%
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Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)
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