2-Methoxyestradiol (2-MeOE2)

For research use only.

Catalog No.S1233 Synonyms: NSC 659853

32 publications

2-Methoxyestradiol (2-MeOE2) Chemical Structure

CAS No. 362-07-2

2-Methoxyestradiol (2-MeOE2, NSC 659853) depolymerizes microtubules and blocks HIF-1α nuclear accumulation and HIF-transcriptional activity. 2-Methoxyestradiol induces both autophagy and apoptosis in various carcinogenic cell lines. Phase 2.

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Selleck's 2-Methoxyestradiol (2-MeOE2) has been cited by 32 publications

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Biological Activity

Description 2-Methoxyestradiol (2-MeOE2, NSC 659853) depolymerizes microtubules and blocks HIF-1α nuclear accumulation and HIF-transcriptional activity. 2-Methoxyestradiol induces both autophagy and apoptosis in various carcinogenic cell lines. Phase 2.
HIF-2α [1]
(Rat aortic smooth muscle A-10 cells)
Microtubule Associated [1]
(Cell-free assay)
HIF-1α [3]
(MDA-MB-231 cells)
In vitro

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. [1] 2-Methoxyestradiol inhibits proliferation of MCF-7 and BM cells with IC50 of 52 μM and 8 μM. [2] In MDA-MB-231 cells, 2-Methoxyestradiol inhibits HIF-1-mediated transcriptional activation of target genes without affecting the transcription of HIF-1α itself. [3] 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. [4]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HCT-116 NE\2VVdkgXSxdH;4bYNqfHliYYPzZZk> MWL+NVAxKM7:TR?= NWW2fYkyT0l3ME2wMlQ4KM7:TR?= NGjvcGs6OjRyM{S4
SF-539 Ml;SZ5l1d3SxeHnjbZR6KGG|c3H5 M3j2eZ4yODBizszN NWWyNVRtT0l3ME2wMlMzKM7:TR?= M4rnUlkzPDB|NEi=
UACC-62 M2HEe4N6fG:2b4jpZ4l1gSCjc4PhfS=> M376cp4yODBizszN MnHsS2k2OD1yLkO2JO69VQ>? M1v2TlkzPDB|NEi=
OVCAR-3 MUHjfZRwfG:6aXPpeJkh[XO|YYm= M3qwbZ4yODBizszN MnzCS2k2OD1yLkKxJO69VQ>? M3zZRVkzPDB|NEi=
DU-145 MnjOZ5l1d3SxeHnjbZR6KGG|c3H5 NHXMNoJ,OTByIN88US=> MlKzS2k2OD1zLkig{txO M4[3O|kzPDB|NEi=
MDA-MB-435 MoC0Z5l1d3SxeHnjbZR6KGG|c3H5 NUjYeIJlhjFyMDFOwG0> Mn7rS2k2OD1yLkC4JO69VQ>? NEDLRnk6OjRyM{S4
LNCaP NUfwTIg1T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M3ywd542OCEQvF2= MVjJR|UxRTBwNTFOwG0> NX\XbohNOTZ4NUC5PFk>
DU145 NHPS[lZIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M{DxWWdKPTB;MT6yNkDPxE1? M{X2fFE4Pjl4NEG5
MDA-MB-23  NEPyWIJIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M33Fb2dKPTB;MD65OEDPxE1? NEKwfpkyPzZ7NkSxPS=>
MCF7 MlLvS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MVPHTVUxRTJwM{Wg{txO M17NOFE4Pjl4NEG5
U87-MG MlT2S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NHXHfYxKSzVyPUiuOVQh|ryP NGjEV3AyQTd4MkK0Oi=>
PC3 MoPtS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M4LZb2lEPTB;Mj62OUDPxE1? NVOwXXpUOTl5NkKyOFY>
HUVEC M{X5eWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NWm2N48xUUN3ME2wMlg1KM7:TR?= MXqxPVc3OjJ2Nh?=
U937 M3zMWWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M2TJOWlEPTB;Mj65NUDPxE1? MXeyNFM{PDR{MR?=
SK-OV-3 NU\6c4RWTnWwY4Tpc44h[XO|YYm= M2LFfYNqemO3bY\lcpR{KFCpcD3t[YRq[XSnZDDkdpVoKHKnc3nzeIFv[2Vid3n0bEBGSzVyIH;mJFg3PyCwTR?= NFfWSpkzODl5M{S4PC=>
SK-OV-3 MDR-1-6/6 MUfGeY5kfGmxbjDhd5NigQ>? M{fGUoNqemO3bY\lcpR{KFCpcD3t[YRq[XSnZDDkdpVoKHKnc3nzeIFv[2Vid3n0bEBGSzVyIH;mJFIzPjhibl2= M1raUlIxQTd|NEi4
HeLa M3rLT2Z2dmO2aX;uJIF{e2G7 NYjudJZKcW6qaXLpeJPPukmLST30eYJ2dGmwIH;uJIRzfWdic3Xud4l1cX[rdIm= M{\zeVIxQTd|NEi4
HUVEC NFXJ[ZJHfW6ldHnvckBie3OjeR?= NGf3b3h{cG:5czDhcpRq[W6paX;n[Y5q[yCjY4Tpeol1gQ>? NGLBbmQzOTl{OEe5OC=>

... Click to View More Cell Line Experimental Data

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. [5]


Kinase Assay:[1]
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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:[1]
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  • Cell lines: MDA-MB-435 and SK-OV-3
  • Concentrations: 0-20 μM
  • Incubation Time: 48 hours
  • Method: 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)
Animal Research:[5]
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  • Animal Models: 9L-V6R cells are injected into the brains of Fischer 344 rats
  • Dosages: ≤600 mg/kg
  • Administration: Administered via i.p.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 60 mg/mL (198.4 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
2%DMSO+30%PEG300+5%Tween 80+ddH2O
For best results, use promptly after mixing.

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 302.41


CAS No. 362-07-2
Storage powder
in solvent
Synonyms NSC 659853
Smiles CC12CCC3C(C1CCC2O)CCC4=CC(=C(C=C34)OC)O

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID