2-Methoxyestradiol (2-MeOE2) (Synonyms: 2Hydroxyestradiol 2methyl ether, 2ME2, NSC 659853, Panzem) |
| Catalog No.GC15084 |
2-Methoxyestradiol (2-MeOE2)은 HIF-1α 억제제이다.
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Cas No.: 362-07-2
Sample solution is provided at 25 µL, 10mM.
2-Methoxyestradiol (2-MeOE2)은 HIF-1α 억제제이다. 그것의 축적를 억제 할 수 있는HIF-1αHIF의 전사 활동을 통해2-ME는 두 가지 메커니즘을 통해 p53 유도의 조직소멸을 유발할 수 있다: P38와 NF-κB의 활성화뿐만 아니라JNK와 AP-1의 활성화, 이는 Bcl-2의인산화를 유도한다. 이를 통해 종양 세포의 유전을 방해하고 마이크로튭의 안정성을 흐트러뜨리고 스핀들 유전을 방해하여 종양 세포의 유전을 방지한다. 조직소멸 유도제와 혈관 생성 억제제로써 잠재적인 항종양 활동을 가지고 있다[4].
2-Methoxyestradiol (10 µg/mL; 1-4일) 처리로 B16 흑색종 세포의 증식 능력이 현저히 억제되었다[5]. 2-Methoxyestradiol (0.03-33mM)은 L-젖산 유도된 골육종 세포의 이동과 증식을 없앴다[6].
방사선 조사 전후에 2-Methoxyestradiol (30 mg/kg; 복강 주사/경구; 7일/3주) 처리는 C57/BL6 쥐의 피부에서 방사선 유도 피부 손상(RISI)을 억제했다. 2-Methoxyestradiol은 또한 방사선 유도 염증, 피부 두께 및 혈관 섬유증을 줄였다[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.
| 세포 실험 [1]: | |
세포 라인 | B16세포 |
제조 방법 | B16 세포가 96웰 판에 재배되었습니다(각 구멍에 1000개의 세포). 세포가 서식한 후2-Methoxyestradiol (10 µg/mL)으로 처리되었습니다. 처리 후 1일, 2일, 3일, 4일에 CCK8 검사를 실시했습니다. |
반응 조건 | 10 µg/mL;1-4일 |
응용 분야 | 2-Methoxyestradiol 처리는 B16 흑색종 세포의 증식능력을 유의적으로 억제했습니다. |
| 동물 실험 [2]: | |
동물 모형 | C57BL/6 쥐 |
제조 방법 | 쥐의 피부는 4cm의 조사 영역으로 17 및 20 Gy의 방사선을 받았습니다. 조사 그룹의 쥐에게 2-Methoxyestradiol을 주입했습니다. |
제형 | 30 mg/kg;i.p/p.o; 7일/3주 |
응용 분야 | 2-Methoxyestradiol은 방사선 유도 피부 혈관 손상을 억제하고 혈관 주변 콜라겐 축적 및 HIF-1α 표현 상승을 억제합니다. |
참고문헌: [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.[2]. 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. | |
| Cas No. | 362-07-2 | SDF | |
| Synonyms | 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 |
| Solubility | ≥ 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. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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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 |
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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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