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

Free Overnight Delivery on orders over $ 500
Next day delivery by 10:00 a.m. Order now.

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

Choose Selective HIF Inhibitors

Click to view more

Notes:

2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

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 Mnv5Z5l1d3SxeHnjbZR6KGG|c3H5 M4rGPZ4yODBizszN NWHoOIdoT0l3ME2wMlcxKM7:TR?= MmHlPVI1ODN2OB?=
HCT-116 MVPjfZRwfG:6aXPpeJkh[XO|YYm= NWLVOo1FhjFyMDFOwG0> MVfHTVUxRTBwNEeg{txO M3\ZdlkzPDB|NEi=
SF-539 Mm\2Z5l1d3SxeHnjbZR6KGG|c3H5 M4LrSZ4yODBizszN NHfYenJIUTVyPUCuN|Ih|ryP M1zSWlkzPDB|NEi=
UACC-62 NVTuUXd4[3m2b4TvfIlkcXS7IHHzd4F6 MkX4glExOCEQvF2= M{HmVmdKPTB;MD6zOkDPxE1? NV\NZXhHQTJ2MEO0PC=>
OVCAR-3 M{DVdYN6fG:2b4jpZ4l1gSCjc4PhfS=> Ml3hglExOCEQvF2= MmG3S2k2OD1yLkKxJO69VQ>? MlPMPVI1ODN2OB?=
SN12C M4D4TYN6fG:2b4jpZ4l1gSCjc4PhfS=> M2P1WZ4yODBizszN NHTxbXpIUTVyPUCuPVUh|ryP M33Y[lkzPDB|NEi=
DU-145 MoHzZ5l1d3SxeHnjbZR6KGG|c3H5 NVGwSXNVhjFyMDFOwG0> NFHVeHJIUTVyPUGuPEDPxE1? MkfYPVI1ODN2OB?=
MDA-MB-435 MknBZ5l1d3SxeHnjbZR6KGG|c3H5 NXfNUldihjFyMDFOwG0> NIKwUJZIUTVyPUCuNFgh|ryP MUe5NlQxOzR6
LNCaP MoPrS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M2G4XZ42OCEQvF2= M2Lm[mlEPTB;MD61JO69VQ>? MUSxOlY2ODl6OR?=
DU145 MX3Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M3mwV2dKPTB;MT6yNkDPxE1? MXuxO|Y6PjRzOR?=
MDA-MB-23  MUnHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M33FVGdKPTB;MD65OEDPxE1? NXHZbXo3OTd4OU[0NVk>
MCF7 NE\hVJVIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= Mn\tS2k2OD1{LkO1JO69VQ>? MlLCNVc3QTZ2MUm=
U87-MG MUHHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MVTJR|UxRThwNUSg{txO NXezPFBXOTl5NkKyOFY>
PC3 NVXsV3dXT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M17UcmlEPTB;Mj62OUDPxE1? NXuxWJg6OTl5NkKyOFY>
HUVEC M4XP[2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NGG1bYhKSzVyPUCuPFQh|ryP Mkj5NVk4PjJ{NE[=
U937 MWfHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MkPyTWM2OD1{LkmxJO69VQ>? NHzuVHIzODN|NESyNS=>
SK-OV-3 NFjQXJpHfW6ldHnvckBie3OjeR?= M3\MSINqemO3bY\lcpR{KFCpcD3t[YRq[XSnZDDkdpVoKHKnc3nzeIFv[2Vid3n0bEBGSzVyIH;mJFg3PyCwTR?= MU[yNFk4OzR6OB?=
SK-OV-3 MDR-1-6/6 MlW4SpVv[3Srb36gZZN{[Xl? M{PlOoNqemO3bY\lcpR{KFCpcD3t[YRq[XSnZDDkdpVoKHKnc3nzeIFv[2Vid3n0bEBGSzVyIH;mJFIzPjhibl2= M3r2clIxQTd|NEi4
HeLa Mnr1SpVv[3Srb36gZZN{[Xl? MYHpcohq[mm2c98yTWlKNXS3YoXsbY4hd25iZIL1[{B{\W6|aYTpeol1gQ>? NWK5TGpQOjB7N{O0PFg>
HUVEC MXHGeY5kfGmxbjDhd5NigQ>? M37HXpNpd3e|IHHueIlidmerb3flcolkKGGldHn2bZR6 MlmxNlE6Ojh5OUS=

... 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
+ 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
+ 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
+ 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

Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

  • Mass
    Concentration
    Volume
    Molecular Weight

*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

  • C1
    V1
    C2
    V2

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Mass Concentration Volume Molecular Weight

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

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

  • * Indicates a Required Field

HIF Signaling Pathway Map

Related HIF Products

Tags: buy 2-Methoxyestradiol (2-MeOE2) | 2-Methoxyestradiol (2-MeOE2) supplier | purchase 2-Methoxyestradiol (2-MeOE2) | 2-Methoxyestradiol (2-MeOE2) cost | 2-Methoxyestradiol (2-MeOE2) manufacturer | order 2-Methoxyestradiol (2-MeOE2) | 2-Methoxyestradiol (2-MeOE2) distributor
×
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID