2-Methoxyestradiol (2-MeOE2)

Catalog No.S1233 Synonyms: NSC 659853

2-Methoxyestradiol (2-MeOE2) Chemical Structure

Molecular Weight(MW): 302.41

2-Methoxyestradiol (2-MeOE2) depolymerizes microtubules and blocks HIF-1α nuclear accumulation and HIF-transcriptional activity. Phase 2.

Size Price Stock Quantity  
In DMSO USD 70 In stock
USD 50 In stock
USD 170 In stock
USD 270 In stock
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2 Customer Reviews

  • Pancreatic cancer cell lines (CFPAC-1 and BxPC-3) were treated with siHIF-1 and 2-ME and then evaluate the expression HIF-1α, CRT and P-eIF2α by Western blotting experiment.

    Oncotarget, 2015, 6(4): 2250-62. 2-Methoxyestradiol (2-MeOE2) purchased from Selleck.

    The knockdown of Set7 by Set7-shRNA-2 in RCC4 cells increased GST expression, but this effect was not evident when HIF-2 activity was inhibited by addition of 2ME2 (50 ng/µl,18 h), as revealed by semi-quantitative real-time PCR assays.

    Nucleic Acids Res, 2015, 43(10): 5081-98 . 2-Methoxyestradiol (2-MeOE2) purchased from Selleck.

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Biological Activity

Description 2-Methoxyestradiol (2-MeOE2) depolymerizes microtubules and blocks HIF-1α nuclear accumulation and HIF-transcriptional activity. 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 NYeyPZlb[3m2b4TvfIlkcXS7IHHzd4F6 MnWyglExOCEQvF2= NYPqdXQ2T0l3ME2wMlcxKM7:TR?= MVS5NlQxOzR6
HCT-116 M2P0WYN6fG:2b4jpZ4l1gSCjc4PhfS=> MkDsglExOCEQvF2= NVXDdXhHT0l3ME2wMlQ4KM7:TR?= MkLxPVI1ODN2OB?=
SF-539 NGXCblZkgXSxdH;4bYNqfHliYYPzZZk> M1e5cp4yODBizszN NWrs[IFxT0l3ME2wMlMzKM7:TR?= NVjiOY5DQTJ2MEO0PC=>
UACC-62 MV\jfZRwfG:6aXPpeJkh[XO|YYm= Mlr2glExOCEQvF2= MX3HTVUxRTBwM{[g{txO Mo\3PVI1ODN2OB?=
OVCAR-3 Ml\3Z5l1d3SxeHnjbZR6KGG|c3H5 M1uwe54yODBizszN MoKxS2k2OD1yLkKxJO69VQ>? M4fKUVkzPDB|NEi=
SN12C NITPfHBkgXSxdH;4bYNqfHliYYPzZZk> M1LWfp4yODBizszN NX;EXoh5T0l3ME2wMlk2KM7:TR?= NYPBcnRtQTJ2MEO0PC=>
DU-145 Moe2Z5l1d3SxeHnjbZR6KGG|c3H5 NI\Hcml,OTByIN88US=> M1zPNGdKPTB;MT64JO69VQ>? MnmwPVI1ODN2OB?=
MDA-MB-435 M4S0d4N6fG:2b4jpZ4l1gSCjc4PhfS=> M1nvcZ4yODBizszN NELTPHdIUTVyPUCuNFgh|ryP M{fvRlkzPDB|NEi=
LNCaP M2fw[Gdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MnHpglUxKM7:TR?= MUnJR|UxRTBwNTFOwG0> MYqxOlY2ODl6OR?=
DU145 Ml;0S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M1fVT2dKPTB;MT6yNkDPxE1? NX7LT2ZNOTd4OU[0NVk>
MDA-MB-23  MVzHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M1nqZ2dKPTB;MD65OEDPxE1? NHvReJQyPzZ7NkSxPS=>
MCF7 MXzHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MnXMS2k2OD1{LkO1JO69VQ>? NIDITmUyPzZ7NkSxPS=>
U87-MG MUDHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NEC3[otKSzVyPUiuOVQh|ryP MUOxPVc3OjJ2Nh?=
PC3 MU\Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M3iwOGlEPTB;Mj62OUDPxE1? M4j1elE6PzZ{MkS2
HUVEC NGW3PYFIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M3nk[WlEPTB;MD64OEDPxE1? MkfaNVk4PjJ{NE[=
U937 MWPHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MnXBTWM2OD1{LkmxJO69VQ>? NVTZU2pCOjB|M{S0NlE>
SK-OV-3 MXXGeY5kfGmxbjDhd5NigQ>? M3ey[INqemO3bY\lcpR{KFCpcD3t[YRq[XSnZDDkdpVoKHKnc3nzeIFv[2Vid3n0bEBGSzVyIH;mJFg3PyCwTR?= MoLZNlA6PzN2OEi=
SK-OV-3 MDR-1-6/6 MUTGeY5kfGmxbjDhd5NigQ>? NX;Pd|dI[2m{Y4XteoVvfHNiUHfwMY1m\GmjdHXkJIRzfWdicnXzbZN1[W6lZTD3bZRpKEWFNUCgc4YhOjJ4ODDuUS=> NWe4[VRbOjB7N{O0PFg>
HeLa MXzGeY5kfGmxbjDhd5NigQ>? MX7pcohq[mm2c98yTWlKNXS3YoXsbY4hd25iZIL1[{B{\W6|aYTpeol1gQ>? M13WbVIxQTd|NEi4
HUVEC M{ftUmZ2dmO2aX;uJIF{e2G7 NFLiVFF{cG:5czDhcpRq[W6paX;n[Y5q[yCjY4Tpeol1gQ>? NX7Ucm1MOjF7Mki3PVQ>

... 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]

Protocol

Kinase Assay:[1]
+ Expand

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]
+ Expand
  • 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]
+ Expand
  • Animal Models: 9L-V6R cells are injected into the brains of Fischer 344 rats
  • Formulation: 2-Methoxyestradiol is dissolved in DMSO.
  • 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 <1 mg/mL
Ethanol <1 mg/mL
In vivo 2% DMSO+corn oil 5mg/mL

* 1 mg/ml means slightly soluble or insoluble.
* 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 powder
in solvent
Synonyms NSC 659853

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT00328497 Completed Carcinoid Tumor CASI Pharmaceuticals, Inc. May 2006 Phase 2
NCT00028821 Completed Refractory Multiple Myeloma|Stage III Multiple Myeloma|Unspecified Adult Solid Tumor, Protocol Specific National Cancer Institute (NCI) January 2002 Phase 1
NCT00030095 Completed Unspecified Adult Solid Tumor, Protocol Specific National Cancer Institute (NCI) September 2001 Phase 1
NCT00592579 Completed Relapsed Multiple Myeloma|Plateau Phase Multiple Myeloma CASI Pharmaceuticals, Inc. March 2001 Phase 2

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID