2-Methoxyestradiol (2-MeOE2) (Synonyms: 2Hydroxyestradiol 2methyl ether, 2ME2, NSC 659853, Panzem) |
| Catalog No.GC15084 |
2-Methoxyestradiol (2-MeOE2) es un inhibidor de HIF-1α.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 362-07-2
Sample solution is provided at 25 µL, 10mM.
2-Methoxyestradiol (2-MeOE2) es un inhibidor de HIF-1α. Puede inhibir la acumulación de núcleos HIF-1α y la actividad de trascripción de HIF[1-3] .2-ME puede desencadenar la apoptosis inducida por p53 a través de 2 mechanisms: activación de P38 y NF-κB, así como la activación de JNK y AP-1 que conduce a la fosforilación de Bcl-2. Previene la mitosis de las células tumores al inhibir el ensamblaje de tubulina, desestabilizar los microtúbulos e interferir con la mitosis del huso. Como inductor de la apoptosis y un inhibidor de la angiogénesis con potencial actividad antineoplásica[4].
El tratamiento con 2-Methoxyestradiol (10 µg/mL;1-4 días) inhibió significativamente la capacidad de proliferación de las células de melanoma B16[5]. 2-Methoxyestradiol (0.03-33mM) abolió la migración inducida por L-lactate y la proliferación de células de osteosarcoma[6].
El tratamiento con 2-Methoxyestradiol (30 mg/kg;i.p/p.o; 7días/3 semanas) antes y después de la irradiación inhibió la lesión cutánea inducida por radiación (RISI) en la piel de ratones C57/BL6 . 2-ME también redujo la inflamación inducida por la radiación, el grosor de la piel y la fibrosis vascular[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.
| Experimentos celulares [1]: | |
Líneas celulares | Células B16 |
Método de preparación | Las células de B16 se platearon en placas de 96 pozos (1000 células por pozo) y se trataron con 2-Methoxyestradiol (10 µg/mL) después de la adherencia celular. El ensayo CCK8 se realizó en los días 1, 2, 3, y 4 después del tratamiento. |
Condiciones de reacción | 10 µg/mL;1-4 días |
Áreas de aplicación | El tratamiento con 2-Methoxyestradiol inhibió significativamente la capacidad de proliferación de las células de melanoma B16. |
| Experimentos con animales [2]: | |
Modelos animales | C57BL/6 ratones |
Método de preparación | La piel de los ratones se irradiaron con 17 y 20 Gy usando un campo de 4-cm. Se inyectó 2-Methoxyestradiol en el grupo de irradiación. |
Forma de dosificación | 30 mg/kg;i.p/p.o; 7 días/3 semanas |
Áreas de aplicación | 2-Methoxyestradiol inhibe las lesiones vasculares de la piel inducidas por la radiación, la deposición de colágeno perivascular y la expresión regulada ascendente de HIF-1α. |
| 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 | |
| Sinónimos | 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 | |||
|
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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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Quality Control & SDS
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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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