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 NXfk[Ip[[3m2b4TvfIlkcXS7IHHzd4F6 MnjjglExOCEQvF2= NFXBVJdIUTVyPUCuO|Ah|ryP M37yNlkzPDB|NEi=
HCT-116 M{\yWYN6fG:2b4jpZ4l1gSCjc4PhfS=> MX\+NVAxKM7:TR?= NW\De3F[T0l3ME2wMlQ4KM7:TR?= MVO5NlQxOzR6
SF-539 NI\oWpdkgXSxdH;4bYNqfHliYYPzZZk> NYLpPYhVhjFyMDFOwG0> MYTHTVUxRTBwM{Kg{txO M3jqUFkzPDB|NEi=
UACC-62 NWHEO4RC[3m2b4TvfIlkcXS7IHHzd4F6 M2C1bJ4yODBizszN M2X0[mdKPTB;MD6zOkDPxE1? NFfxdZQ6OjRyM{S4
OVCAR-3 MUjjfZRwfG:6aXPpeJkh[XO|YYm= MkjOglExOCEQvF2= MUfHTVUxRTBwMkGg{txO NFXpVGI6OjRyM{S4
SN12C NUPjeG1N[3m2b4TvfIlkcXS7IHHzd4F6 MVj+NVAxKM7:TR?= NX\YV3FCT0l3ME2wMlk2KM7:TR?= MV25NlQxOzR6
DU-145 NUP4T4wx[3m2b4TvfIlkcXS7IHHzd4F6 MnjmglExOCEQvF2= M165c2dKPTB;MT64JO69VQ>? NXHl[|FKQTJ2MEO0PC=>
MDA-MB-435 MWPjfZRwfG:6aXPpeJkh[XO|YYm= M3nENp4yODBizszN MonWS2k2OD1yLkC4JO69VQ>? MnTGPVI1ODN2OB?=
LNCaP MXXHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NH3hbHF,PTBizszN MoixTWM2OD1yLkWg{txO Mo\wNVY3PTB7OEm=
DU145 MWLHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MYjHTVUxRTFwMkKg{txO MXqxO|Y6PjRzOR?=
MDA-MB-23  M{jlZWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NF31R5hIUTVyPUCuPVQh|ryP M2PqSVE4Pjl4NEG5
MCF7 M3fSfGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M3HITmdKPTB;Mj6zOUDPxE1? M1fQXlE4Pjl4NEG5
U87-MG NVvsd3ZoT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NETiXpRKSzVyPUiuOVQh|ryP M{jNOFE6PzZ{MkS2
PC3 NISyZ3RIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NFvP[GdKSzVyPUKuOlUh|ryP M3LPfVE6PzZ{MkS2
HUVEC NIPnRlBIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MmD1TWM2OD1yLki0JO69VQ>? NFu1TVkyQTd4MkK0Oi=>
U937 NHLkXllIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MWrJR|UxRTJwOUGg{txO MoryNlA{OzR2MkG=
SK-OV-3 NV;MV5liTnWwY4Tpc44h[XO|YYm= NUntdpcz[2m{Y4XteoVvfHNiUHfwMY1m\GmjdHXkJIRzfWdicnXzbZN1[W6lZTD3bZRpKEWFNUCgc4YhQDZ5IH7N MlPKNlA6PzN2OEi=
SK-OV-3 MDR-1-6/6 MWPGeY5kfGmxbjDhd5NigQ>? MlH0Z4lz[3WvdnXueJMhWGeyLX3l[IlifGWmIHTyeYchemW|aYP0ZY5k\SC5aYToJGVEPTBib3[gNlI3QCCwTR?= MkXFNlA6PzN2OEi=
HeLa MYLGeY5kfGmxbjDhd5NigQ>? NFjYc|lqdmirYnn0d:6zUUmLLYT1ZpVtcW5ib36g[JJ2\yC|ZX7zbZRqfmm2eR?= MWeyNFk4OzR6OB?=
HUVEC MoS5SpVv[3Srb36gZZN{[Xl? MmTyd4hwf3NiYX70bYFv\2mxZ3XubYMh[WO2aY\peJk> MkDFNlE6Ojh5OUS=

... 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 slightly soluble or insoluble
Ethanol slightly soluble or insoluble
In vivo Add solvents individually and in order:
2% DMSO+corn oil
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
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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HIF Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID