2-Methoxyestradiol (2-MeOE2) (Synonyms: 2Hydroxyestradiol 2methyl ether, 2ME2, NSC 659853, Panzem) |
رقم الكتالوجGC15084 |
2-Methoxyestradiol (2-MeOE2/2-Me) is an HIF-1α inhibitor.
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-MeOE2/2-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.
Cell experiment [1]: | |
Cell lines |
B16 cells |
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. |
Reaction Conditions |
10 µg/mL;1-4days |
Applications |
2-Methoxyestradiol treatment significantly inhibited the proliferation ability of B16 melanoma cells. |
Animal experiment [2]: | |
Animal models |
C57BL/6 mice |
Preparation Method |
Mice skin were irradiated with 17 and 20 Gy using a 4-cm field. 2-Methoxyestradiol was injected into the irradiation group. |
Dosage form |
30 mg/kg;i.p/p.o; 7days/3weeks |
Applications |
2-Methoxyestradiol inhibits radiation-induced skin vascular injuries, perivascular collagen deposition, and upregulated HIF-1α expression. |
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 | |
المرادفات | 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 |
الذوبان | ≥ 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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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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3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5
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