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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Cited by 21 Publications

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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 MXXjfZRwfG:6aXPpeJkh[XO|YYm= MnrsglExOCEQvF2= MXvHTVUxRTBwN{Cg{txO MVu5NlQxOzR6
HCT-116 NHO5XXhkgXSxdH;4bYNqfHliYYPzZZk> M13ld54yODBizszN M3;P[2dKPTB;MD60O{DPxE1? M3HXZ|kzPDB|NEi=
SF-539 NUPpXIhw[3m2b4TvfIlkcXS7IHHzd4F6 MWj+NVAxKM7:TR?= NHLOfmNIUTVyPUCuN|Ih|ryP M1qyOlkzPDB|NEi=
UACC-62 M3nJR4N6fG:2b4jpZ4l1gSCjc4PhfS=> M3zpbZ4yODBizszN NHPn[ZNIUTVyPUCuN|Yh|ryP MmnkPVI1ODN2OB?=
OVCAR-3 NH:yS4ZkgXSxdH;4bYNqfHliYYPzZZk> NXfCXmh7hjFyMDFOwG0> MXPHTVUxRTBwMkGg{txO NVrN[Fh{QTJ2MEO0PC=>
SN12C Ml3KZ5l1d3SxeHnjbZR6KGG|c3H5 NHnMOFB,OTByIN88US=> MYDHTVUxRTBwOUWg{txO NFf2U5U6OjRyM{S4
DU-145 M2DLS4N6fG:2b4jpZ4l1gSCjc4PhfS=> M3z1bJ4yODBizszN MYrHTVUxRTFwODFOwG0> NILhVFU6OjRyM{S4
MDA-MB-435 MU\jfZRwfG:6aXPpeJkh[XO|YYm= NUDjZ|hXhjFyMDFOwG0> NX\JNotQT0l3ME2wMlA5KM7:TR?= MYW5NlQxOzR6
LNCaP NE\sU|JIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NWnLPGhrhjVyIN88US=> NW\IeIhNUUN3ME2wMlUh|ryP NXLrbFJ2OTZ4NUC5PFk>
DU145 NHXCNoRIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NGjjOYVIUTVyPUGuNlIh|ryP NV3FOotnOTd4OU[0NVk>
MDA-MB-23  MVfHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NFTseGJIUTVyPUCuPVQh|ryP M1;ZOVE4Pjl4NEG5
MCF7 M3XDbWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NXLwcno2T0l3ME2yMlM2KM7:TR?= MX:xO|Y6PjRzOR?=
U87-MG NH;rdIlIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M1z0TWlEPTB;OD61OEDPxE1? M{XkW|E6PzZ{MkS2
PC3 NGP0SZJIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MWTJR|UxRTJwNkWg{txO NIfFN3EyQTd4MkK0Oi=>
HUVEC MkfzS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NH;JdoZKSzVyPUCuPFQh|ryP NV7NfId[OTl5NkKyOFY>
U937 NF7Gb49Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MkjaTWM2OD1{LkmxJO69VQ>? M{\vdlIxOzN2NEKx
SK-OV-3 NUDXc4dVTnWwY4Tpc44h[XO|YYm= MmflZ4lz[3WvdnXueJMhWGeyLX3l[IlifGWmIHTyeYchemW|aYP0ZY5k\SC5aYToJGVEPTBib3[gPFY4KG6P MnrtNlA6PzN2OEi=
SK-OV-3 MDR-1-6/6 NVnzNldFTnWwY4Tpc44h[XO|YYm= M1y0T4NqemO3bY\lcpR{KFCpcD3t[YRq[XSnZDDkdpVoKHKnc3nzeIFv[2Vid3n0bEBGSzVyIH;mJFIzPjhibl2= NGDDWW4zODl5M{S4PC=>
HeLa NVzsZ3RUTnWwY4Tpc44h[XO|YYm= MlTGbY5pcWKrdIROtmlKUS22dXL1cIlvKG:wIHTyeYche2Wwc3n0bZZqfHl? MmfBNlA6PzN2OEi=
HUVEC MUHGeY5kfGmxbjDhd5NigQ>? NXrnTVZRe2ixd4OgZY51cWGwZ3nv[4VvcWNiYXP0bZZqfHl? NXPCTXZUOjF7Mki3PVQ>

... 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]
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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]
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  • 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]
- Collapse
  • 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(Data is from Selleck tests instead of citations):
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
in solvent
Synonyms NSC 659853

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID