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2-Methoxyestradiol

Catalog No. T2220 CAS 362-07-2

Synonyms: 2-MeOE2, 2-ME2, NSC-659853, 2-甲氧雌二醇, 二甲氧基雌二醇

2-Methoxyestradiol 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

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Purity: 98%

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Storage & Solubility Information

Description	2-Methoxyestradiol 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.
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	2-MeOE2, 2-ME2, NSC-659853, 2-甲氧雌二醇, 二甲氧基雌二醇
Molecular Weight	302.41
Formula	C19H26O3
CAS No.	362-07-2

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

DMSO: 15.1 mg/mL (50 mM)

( < 1 mg/ml refers to the product slightly soluble or insoluble )

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

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Compound Library Preclinical Compound Library Autophagy Compound Library HIF-1 Signaling Pathway Compound Library Glycometabolism Compound Library Anti-Cancer Metabolism Compound Library Human Endogenous Metabolite Library Glutamine Metabolism Compound Library Anti-Pancreatic Cancer Compound Library Inhibitor Library

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Keywords

2-Methoxyestradiol 362-07-2 NF-Kb信号通路表观遗传代谢凋亡免疫与炎症细胞骨架血管生成自噬 Apoptosis Autophagy Endogenous Metabolite HIF Microtubule Associated Reactive Oxygen Species NSC 659853 NSC659853 NSC-659853 2Methoxyestradiol 2-MeOE2 Microtubule/Tubulin Inhibitor 2 Methoxyestradiol 2-ME2 inhibit inhibitor

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