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    2-Methoxyestradiol (2MeOE2, NSC659853, 2ME2)
    2-Methoxyestradiol (2MeOE2, NSC659853, 2ME2)

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V0294
    CAS #: 362-07-2Purity ≥98%

    Description: 2-Methoxyestradiol (2-MeOE2, NSC-659853, 2-ME2; 2-ME), an endogenous/natural metabolite of estradiol [17β-estradiol (E2)], is a potent inhibitor of tubulin with potential anticancer activity. It also acts as a blocker of HIF-1α nuclear accumulation and HIF-transcriptional activity, an inhibitor of angiogenesis as well as an inducer of apoptosis. As an inhibitor of microtubule assembly, it inhibits the polymerization of tubulin and interferes with mitotic spindle dynamics which leads to the blockage of mitosis of human cancer cells.

    References:  Steroids. 2002;67(13-14):1079-89; Carcinogenesis. 2000;21(4):735-40; Cancer Res. 2006;66(24):11991-7.

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    -20℃ for 3 years in powder form

    -80℃ for 2 years in solvent

    Solubility (In vitro)

    DMSO: 60 mg/mL (198.4 mM)

    Water: <1 mg/mL

    Ethanol: <1 mg/mL

    Solubility (In vivo)

    2% DMSO+corn oil: 5mg/mL


    NSC 659853; NSC-659853; NSC659853; 2-ME; 2-Methoxy Estradiol. 2-methoxyestradiol; US brand name: Panzem. Abbreviation: 2-ME2.

    Chemical Name: (8R,9S,13S,14S,17S)-2-methoxy-13-methyl-7,8,9,11,12,13,14,15,16,17-decahydro-6H-cyclopenta[a]phenanthrene-3,17-diol

    SMILES Code: OC1=C(OC)C=C2[[email protected]@]3([H])CC[[email protected]]4(C)[[email protected]@H](O)CC[[email protected]@]4([H])[[email protected]]3([H])CCC2=C1

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    In Vitro

    In vitro activity: 2-Methoxyestradiol exhibits the inhibitory activity of cellular proliferation in a breast carcinoma cell line MDA-MB-435 and an ovarian carcinoma cell line SK-OV-3 with IC50 of 1.38 μM and 1.79 μM, respectively. Furthermore, 2-Methoxyestradiol also inhibits cellular microtubule depolymerization in rat aortic smooth muscle A-10 cells with EC50 of 7.5 μM. 2-Methoxyestradiol inhibits proliferation of MCF-7 and BM cells with IC50 of 52 μM and 8 μM. In MDA-MB-231 cells, 2-Methoxyestradiol inhibits HIF-1-mediated transcriptional activation of target genes without affecting the transcription of HIF-1α itself. A recent study shows that 2-Methoxyestradiol (0.5 μM), blocks TGF-β3-induced expression of collagen (Col) type I(αI), Col III(αI), plasminogen activator inhibitor (PAI) 1, connective tissue growth factor (CTGF), and α-smooth muscle actin (α-SMA). Moreover, 2-Methoxyestradiol ameliorates TGF-β3-induced Smad2/3 phosphorylation and nuclear translocation, and inhibits TGF-β3-induced activation of the PI3K/Akt/mTOR pathway


    Kinase Assay: 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 Assay: 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.

    In Vivo

    In a 9L rat glioma (9L-V6R) rat model, 2-Methoxyestradiol significantly decreases HIF-1 activity and inhibits the tumor growth in a dose-dependent manner by 4-fold reduction for 60 mg/kg/day, and 23-fold reduction for 600 mg/kg/day, respectively.

    Animal model

    9L-V6R cells are injected into the brains of Fischer 344 rats

    Formulation & Dosage

    Dissolved in DMSO;<600mg/kg; i.p. injection


    Steroids. 2002 Dec;67(13-14):1079-89; Carcinogenesis. 2000 Apr;21(4):735-40; Cancer Res. 2006 Dec 15;66(24):11991-7.

    These protocols are for reference only. InvivoChem does not independently validate these methods.

    2-Methoxyestradiol (2-MeOE2)

    Treatment of 9L rat glioma cells with 2-methoxyestradiol (2ME2) at different oxygen concentration. Cancer Res. 2006 Dec 15;66(24):11991-7.

    2-Methoxyestradiol (2-MeOE2)

    A, a representative Gd-DTPA enhanced T1-weighted MRI image from each treatment group: left, before treatment; right, after treatment. B, summary of the tumor volume from the six rats in each group; all 24 rats before and after 2-methoxyestradiol treatment were measured by noninvasive post-contrast T1-weighted MRI. C, top left, acrylic brain matrices used to slice the rat brain into a 2-mm thickness from the tip of the frontal lobe of cerebrum (Start) to match with the MRI data that were scanned in the same orientation (End; bottom left). Cancer Res. 2006 Dec 15;66(24):11991-7.

    2-Methoxyestradiol (2-MeOE2)

    BLIs of HIF-1 activity are shown from three representative rats of each group at the end of 2-methoxyestradiol treatment. Right, scale of light intensity. Cancer Res. 2006 Dec 15;66(24):11991-7.


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