2-Methoxyestradiol (2-MeOE2)

Catalog No.S1233 Synonyms: NSC 659853, 2-ME2

For research use only.

2-Methoxyestradiol (2-MeOE2, NSC 659853, 2-ME2) 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.

2-Methoxyestradiol (2-MeOE2) Chemical Structure

CAS No. 362-07-2

Selleck's 2-Methoxyestradiol (2-MeOE2) has been cited by 57 publications

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Biological Activity

Description 2-Methoxyestradiol (2-MeOE2, NSC 659853, 2-ME2) 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.
Targets
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
HOP-62 MYDjfZRwfG:6aXPpeJkh[XO|YYm= MlfQglExOCEQvF2= MX3HTVUxRTBwN{Cg{txO NGr3Wo06OjRyM{S4
HCT-116 MnXEZ5l1d3SxeHnjbZR6KGG|c3H5 NHvjU2Z,OTByIN88US=> NY[zS3I3T0l3ME2wMlQ4KM7:TR?= MlG0PVI1ODN2OB?=
SF-539 NFjuXmtkgXSxdH;4bYNqfHliYYPzZZk> MlHLglExOCEQvF2= Mnn4S2k2OD1yLkOyJO69VQ>? Mn;5PVI1ODN2OB?=
UACC-62 MX7jfZRwfG:6aXPpeJkh[XO|YYm= M1nBd54yODBizszN NH7DWGVIUTVyPUCuN|Yh|ryP NYH0T41KQTJ2MEO0PC=>
OVCAR-3 MX;jfZRwfG:6aXPpeJkh[XO|YYm= MVX+NVAxKM7:TR?= NXvJeHlJT0l3ME2wMlIyKM7:TR?= MUG5NlQxOzR6
SN12C MoPiZ5l1d3SxeHnjbZR6KGG|c3H5 M{DlNp4yODBizszN NEL3O|RIUTVyPUCuPVUh|ryP MoHyPVI1ODN2OB?=
DU-145 M{nQe4N6fG:2b4jpZ4l1gSCjc4PhfS=> NV\PZ5pkhjFyMDFOwG0> NVjtPW5oT0l3ME2xMlgh|ryP NY\obXB4QTJ2MEO0PC=>
MDA-MB-435 M2\xOIN6fG:2b4jpZ4l1gSCjc4PhfS=> M{XGNp4yODBizszN NFjDTWRIUTVyPUCuNFgh|ryP NHO3Nno6OjRyM{S4
LNCaP NW\aXmdqT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MnrrglUxKM7:TR?= NGe1W2JKSzVyPUCuOUDPxE1? MWmxOlY2ODl6OR?=
DU145 M3H6Rmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NGGz[XhIUTVyPUGuNlIh|ryP M2XHVVE4Pjl4NEG5
MDA-MB-23  NF\z[5BIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MkjlS2k2OD1yLkm0JO69VQ>? M1v5OlE4Pjl4NEG5
MCF7 NU\QV4xTT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NFXNOoZIUTVyPUKuN|Uh|ryP MkPxNVc3QTZ2MUm=
U87-MG MlXRS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NF76VY5KSzVyPUiuOVQh|ryP M1myOVE6PzZ{MkS2
PC3 MYfHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M4nTTmlEPTB;Mj62OUDPxE1? M{\oVVE6PzZ{MkS2
HUVEC NFnMfYJIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M2XyRWlEPTB;MD64OEDPxE1? MXuxPVc3OjJ2Nh?=
U937 NGr0eHFIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MkHQTWM2OD1{LkmxJO69VQ>? NUTORZByOjB|M{S0NlE>
SK-OV-3 MoPMSpVv[3Srb36gZZN{[Xl? M2fiU4NqemO3bY\lcpR{KFCpcD3t[YRq[XSnZDDkdpVoKHKnc3nzeIFv[2Vid3n0bEBGSzVyIH;mJFg3PyCwTR?= NFfhTGczODl5M{S4PC=>
SK-OV-3 MDR-1-6/6 NYmySFl3TnWwY4Tpc44h[XO|YYm= Mn;PZ4lz[3WvdnXueJMhWGeyLX3l[IlifGWmIHTyeYchemW|aYP0ZY5k\SC5aYToJGVEPTBib3[gNlI3QCCwTR?= MVqyNFk4OzR6OB?=
HeLa NGnqTJJHfW6ldHnvckBie3OjeR?= MXnpcohq[mm2c98yTWlKNXS3YoXsbY4hd25iZIL1[{B{\W6|aYTpeol1gQ>? MknvNlA6PzN2OEi=
HUVEC NE[wbVhHfW6ldHnvckBie3OjeR?= NVXvXpFbe2ixd4OgZY51cWGwZ3nv[4VvcWNiYXP0bZZqfHl? NE[2d3AzOTl{OEe5OC=>
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]

Protocol (from reference)

Kinase Assay:[1]
  • 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]
  • 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]
  • 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.

5mg/mL

* 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
Formula

C19H26O3

CAS No. 362-07-2
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC12CCC3C(C1CCC2O)CCC4=CC(=C(C=C34)OC)O

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