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.

Purity & Quality Control

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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 NITaSmxkgXSxdH;4bYNqfHliYYPzZZk> NUTtW5RGhjFyMDFOwG0> NVm4UIw4T0l3ME2wMlcxKM7:TR?= M3HtelkzPDB|NEi=
HCT-116 NV7HTZd1[3m2b4TvfIlkcXS7IHHzd4F6 M2iycJ4yODBizszN NXrGUYxwT0l3ME2wMlQ4KM7:TR?= NH\mS3A6OjRyM{S4
SF-539 NXHwR2E2[3m2b4TvfIlkcXS7IHHzd4F6 M1n2Wp4yODBizszN M3vlVmdKPTB;MD6zNkDPxE1? MUe5NlQxOzR6
UACC-62 MoW1Z5l1d3SxeHnjbZR6KGG|c3H5 MWr+NVAxKM7:TR?= MYPHTVUxRTBwM{[g{txO MXy5NlQxOzR6
OVCAR-3 NVu3SXpW[3m2b4TvfIlkcXS7IHHzd4F6 MUj+NVAxKM7:TR?= NHnVb|JIUTVyPUCuNlEh|ryP MXO5NlQxOzR6
SN12C M1H1eoN6fG:2b4jpZ4l1gSCjc4PhfS=> MUH+NVAxKM7:TR?= NEX2VlNIUTVyPUCuPVUh|ryP MYe5NlQxOzR6
DU-145 NX3qflFN[3m2b4TvfIlkcXS7IHHzd4F6 M13kT54yODBizszN MnTCS2k2OD1zLkig{txO MnTlPVI1ODN2OB?=
MDA-MB-435 MV;jfZRwfG:6aXPpeJkh[XO|YYm= MYT+NVAxKM7:TR?= NYnlXlc1T0l3ME2wMlA5KM7:TR?= NY[yfIN5QTJ2MEO0PC=>
LNCaP M1nRRWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MV3+OVAh|ryP NYTLVHBXUUN3ME2wMlUh|ryP MnG3NVY3PTB7OEm=
DU145 MlrjS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MU\HTVUxRTFwMkKg{txO NYHDdmw4OTd4OU[0NVk>
MDA-MB-23  NInwRZRIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NWPEPWlkT0l3ME2wMlk1KM7:TR?= MYCxO|Y6PjRzOR?=
MCF7 MXLHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NULvVoZFT0l3ME2yMlM2KM7:TR?= NEXy[WwyPzZ7NkSxPS=>
U87-MG MWnHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NVT4O4o6UUN3ME24MlU1KM7:TR?= MYCxPVc3OjJ2Nh?=
PC3 NEDTXm1Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M{LtTWlEPTB;Mj62OUDPxE1? M1Hze|E6PzZ{MkS2
HUVEC MnrSS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? Ml3NTWM2OD1yLki0JO69VQ>? MWqxPVc3OjJ2Nh?=
U937 MVHHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? Mk\STWM2OD1{LkmxJO69VQ>? NHv5[JozODN|NESyNS=>
SK-OV-3 Ml6zSpVv[3Srb36gZZN{[Xl? MYrjbZJkfW24ZX70d{BR\3BvbXXkbYF1\WRiZIL1[{Bz\XOrc4ThcoNmKHerdHigSWM2OCCxZjC4Olchdk1? NUjLc4ZNOjB7N{O0PFg>
SK-OV-3 MDR-1-6/6 MUjGeY5kfGmxbjDhd5NigQ>? NITaN|NkcXKldX32[Y51eyCSZ4CtcYVlcWG2ZXSg[JJ2\yC{ZYPpd5RidmOnIIfpeIghTUN3MDDv[kAzOjZ6IH7N MXSyNFk4OzR6OB?=
HeLa M4HHSmZ2dmO2aX;uJIF{e2G7 MnPYbY5pcWKrdIROtmlKUS22dXL1cIlvKG:wIHTyeYche2Wwc3n0bZZqfHl? NUjHOFRNOjB7N{O0PFg>
HUVEC MXzGeY5kfGmxbjDhd5NigQ>? Mk\hd4hwf3NiYX70bYFv\2mxZ3XubYMh[WO2aY\peJk> M{S3bVIyQTJ6N{m0

... 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 Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order:
2% DMSO+corn oil
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 powder
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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HIF Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID