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2-Methoxyestradiol (2-MeOE2) (Synonyms: 2Hydroxyestradiol 2methyl ether, 2ME2, NSC 659853, Panzem)

Catalog No.GC15084

2-Methoxyestradiol (2-MeOE2/2-Me) is a HIF-1α inhibitor that inhibits HIF-1α accumulation and HIF transcriptional activity. 2-Methoxyestradiol can trigger p53-induced apoptosis and has potential antitumor activity..

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2-Methoxyestradiol (2-MeOE2) Chemical Structure

Cas No.: 362-07-2

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10mM (in 1mL DMSO)
$35.00
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25mg
$37.00
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50mg
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100mg
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300mg
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Sample solution is provided at 25 µL, 10mM.

Product has been cited by 1 publications

Product Documents

Quality Control & SDS

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Protocol

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.
[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.

Background

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.

Chemical Properties

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.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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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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