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2-Methoxyestradiol

Catalog No. T2220 CAS 362-07-2

Synonyms: NSC-659853, 2-MeOE2, 2-ME2

2-Methoxyestradiol (2-ME2) is an orally bioavailable estradiol metabolite with potential antineoplastic activity. 2-Methoxyestradiol inhibits angiogenesis by reducing endothelial cell proliferation and inducing endothelial cell apoptosis. This agent also inhibits tumor cell growth by binding to tubulin, resulting in antimitotic activity, and by inducing caspase activation, resulting in cell cycle arrest in the G2 phase, DNA fragmentation, and apoptosis.

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2-Methoxyestradiol, CAS 362-07-2

Pack Size	Availability	Price/USD
50 mg	In stock	$ 50.00
100 mg	In stock	$ 58.00
1 mL * 10 mM (in DMSO)	In stock	$ 30.00

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Purity: 99.95%

Purity: 99.84%

Purity: 98%

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Description	2-Methoxyestradiol (2-ME2) is an orally bioavailable estradiol metabolite with potential antineoplastic activity. 2-Methoxyestradiol inhibits angiogenesis by reducing endothelial cell proliferation and inducing endothelial cell apoptosis. This agent also inhibits tumor cell growth by binding to tubulin, resulting in antimitotic activity, and by inducing caspase activation, resulting in cell cycle arrest in the G2 phase, DNA fragmentation, and apoptosis.
In vitro	2-Methoxyestradiol (60 mg/kg/day) can reduce tumor size by fourfold, and increasing the dose tenfold further reduces it by 23 times. This compound demonstrates dose-dependent therapeutic efficacy in the 9L rat glioma model (9L-V6R), significantly decreasing HIF-1 activity and inhibiting tumor growth.
In vivo	2-Methoxyestradiol (0.5 μM) inhibits the TGF-β3-induced expression of Type I collagen (Col I) (αI), Col III (αI), connective tissue growth factor, plasminogen activator inhibitor, and α-smooth muscle actin. In MDA-MB-231 cells, it suppresses the transcriptional activation of HIF-1-regulated target genes without affecting HIF-1α transcription itself. It inhibits cell proliferation in breast cancer cell line MDA-MB-435 (IC50: 1.38 μM) and ovarian cancer cell line SK-OV-3 (IC50: 1.79 μM). Furthermore, in rat aortic smooth muscle A-10 cells, 2-Methoxyestradiol prevents microtubule disassembly (EC50: 7.5 μM) and mitigates TGF-β3-induced Smad2/3 phosphorylation and nuclear translocation, as well as inhibiting the activation of the TGF-β3-induced PI3K/Akt/mTOR pathway. Additionally, it suppresses cell proliferation in MCF-7 (IC50: 52 μM) and BM (IC50: 8 μM) cells.
Kinase Assay	Microtubule depolymerizing activity: The effects of 2-Methoxyestradiol on cellular microtubule depolymerization are determined by indirect immunofluorescence techniques in rat aortic smooth muscle A-10 cells. Microtubules are visualized using a β-tubulin antibody. Three viewers determines the percent microtubule loss for each treatment concentration. The data are averaged and plotted as percent microtubule loss versus drug concentration and the EC50s for microtubule depolymerization calculated from the log dose–response curves.
Cell Research	The sulforhodamine B (SRB) assay is used to evaluate the antiproliferative activity of 2-Methoxyestradiol in the MDA-MB-435 and SK-OV-3 cell lines. Cells a plated into 96-well plates and allowed to grow and attach for 24 hours followed by addition of 2-Methoxyestradiol or vehicle controls. The cells are incubated with drugs for 48 hours and then the cellular protein is fixed, stained, and concentration determined by absorbance at 560 nm. Log dose–response curves are constructed for each experiment and the IC50 for inhibition of proliferation determined.(Only for Reference)

Synonyms	NSC-659853, 2-MeOE2, 2-ME2
Molecular Weight	302.41
Formula	C19H26O3
CAS No.	362-07-2

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 15.1 mg/mL (50 mM)

References and Literature

1. Rao PN, et al. Steroids. 2002, 67(13-14), 1079-1089. 2. Seeger H, et al. J Steroid Biochem Mol Biol. 2003, 84(2-3), 255-257. 3. Mabjeesh NJ, et al. Cancer Cell. 2003, 3(4), 363-375. 4. Salama SA, et al. Fertil Steril. 2012. 5. Kang SH, et al. Cancer Res. 2006, 66(24),111991-11997. 6. Aquino-Gálvez A, et al. Effects of 2-methoxyestradiol on apoptosis and HIF-1α and HIF-2α expression in lung cancer cells under normoxia and hypoxia. Oncol Rep. 2016 Jan;35(1):577-83. 7. Xu L, et al. 2-Methoxyestradiol Alleviates Experimental Autoimmune Uveitis by Inhibiting Lymphocytes Proliferation and T Cell Differentiation. Biomed Res Int. 2016;2016:7948345.

Citations

1. Chen X C, Tang G X, Luo W H, et al. Monitoring and Modulating mtDNA G-Quadruplex Dynamics Reveal Its Close Relationship to Cell Glycolysis. Journal of the American Chemical Society. 2021 2. Guo Y, Tian J, Guo Y, et al.Oncogenic KRAS effector USP13 promotes metastasis in non-small cell lung cancer through deubiquitinating β-catenin.Cell Reports.2023, 42(12).

Related compound libraries

This product is contained In the following compound libraries：

Drug Repurposing Compound Library Human Endogenous Metabolite Library Inhibitor Library Microtubule-Targeted Compound Library Anti-Cancer Active Compound Library Anti-Cancer Clinical Compound Library Anti-Cancer Drug Library Bioactive Compounds Library Max Pyroptosis Compound Library Glycometabolism Compound Library

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Keywords

2-Methoxyestradiol 362-07-2 Angiogenesis Apoptosis Autophagy Chromatin/Epigenetic Cytoskeletal Signaling Immunology/Inflammation Metabolism NF-Κb Reactive Oxygen Species Microtubule Associated HIF Endogenous Metabolite NSC-659853 2-MeOE2 2Methoxyestradiol NSC 659853 Microtubule/Tubulin Inhibitor 2 Methoxyestradiol NSC659853 inhibit 2-ME2 inhibitor

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