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2-Methoxyestradiol [362-07-2]

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Katalog-Nummer NB-64-11474-1mL

Size : 1mLx10mM(inDMSO)

Marke : Neo Biotech

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2-Methoxyestradiol

(Synonyms: NSC-659853, 2-MeOE2, 2-ME2) Copy Product Info

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

Catalog No. T2220 Copy Product Info

Purity: 99.95%

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.

Cas No. 362-07-2

For research use only—not for human use. No sales to individuals. Use as intended only.

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Purity:99.95%

Color:White

Product Introduction

Bioactivity

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.
Synonyms	NSC-659853, 2-MeOE2, 2-ME2
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)

Chemical Properties

Molecular Weight	302.41
Formula	C₁₉H₂₆O₃
Cas No.	362-07-2
Smiles	03[C@@]12CC[C@H](O)[C@@]1(C)CC[C@]1(03)c3cc(OC)c(O)cc3CC[C@@]2103
Relative Density.	1.178 g/cm3 (Predicted)

Storage & Solubility Information

Storage

Store under nitrogen Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 45 mg/mL (148.8 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (6.61 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	3.3068 mL	16.5338 mL	33.0677 mL	165.3384 mL
5 mM	0.6614 mL	3.3068 mL	6.6135 mL	33.0677 mL
10 mM	0.3307 mL	1.6534 mL	3.3068 mL	16.5338 mL
20 mM	0.1653 mL	0.8267 mL	1.6534 mL	8.2669 mL
50 mM	0.0661 mL	0.3307 mL	0.6614 mL	3.3068 mL
100 mM	0.0331 mL	0.1653 mL	0.3307 mL	1.6534 mL

Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density.

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, and a total of 10 animals are to be administered, using a formulation of 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO stock solution to 400 µL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 µL Tween 80 and mix well until fully clarified.

3) Add 450 µL Saline,PBS or ddH₂O and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

Keywords

ReactiveOxygenSpeciesReactive Oxygen SpeciesNSC659853NSC 659853MicrotubuleAssociatedMicrotubule/TubulinMicrotubule depolymerizationMicrotubule AssociatedInhibitorinhibitHIF-2αHIF-1αEndogenousMetaboliteEndogenous MetaboliteAutophagyApoptosis2-Methoxyestradiol2Methoxyestradiol2 Methoxyestradiol

Related Tags: 2-Methoxyestradiol chemical structure | 2-Methoxyestradiol in vivo | 2-Methoxyestradiol in vitro | 2-Methoxyestradiol formula | 2-Methoxyestradiol molecular weight