2-Methoxyestradiol (2-MeOE2)

Catalog No.S1233

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

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2-Methoxyestradiol (2-MeOE2) Chemical Structure

2-Methoxyestradiol (2-MeOE2) Chemical Structure
Molecular Weight: 302.41

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Product Description

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 LinesAssay TypeConcentrationIncubation TimeFormulationActivity DescriptionPMID
HOP-62MWPjfZRwfG:6aXPpeJkh[XO|YYm=MVL+NVAxKM7:TR?=MlHiS2k2OD1yLkewJO69VQ>?M4PBXFkzPDB|NEi=
HCT-116NGjqc4RkgXSxdH;4bYNqfHliYYPzZZk>NH\Me5Z,OTByIN88US=>NYf4blY4T0l3ME2wMlQ4KM7:TR?=MnXXPVI1ODN2OB?=
SF-539MlOwZ5l1d3SxeHnjbZR6KGG|c3H5NFjs[2Z,OTByIN88US=>NXTpeWw1T0l3ME2wMlMzKM7:TR?=NWHmOHZkQTJ2MEO0PC=>
UACC-62NV2z[VNl[3m2b4TvfIlkcXS7IHHzd4F6Ml6zglExOCEQvF2=NXuze45UT0l3ME2wMlM3KM7:TR?=NFHVVG86OjRyM{S4
OVCAR-3MonKZ5l1d3SxeHnjbZR6KGG|c3H5NWrSd3hxhjFyMDFOwG0>NID5XpJIUTVyPUCuNlEh|ryPMn\EPVI1ODN2OB?=
SN12CM3TyXIN6fG:2b4jpZ4l1gSCjc4PhfS=>MV\+NVAxKM7:TR?=M2DBS2dKPTB;MD65OUDPxE1?NY\jXlhZQTJ2MEO0PC=>
DU-145MX3jfZRwfG:6aXPpeJkh[XO|YYm=NHWxcXJ,OTByIN88US=>NUL4R4NQT0l3ME2xMlgh|ryPMVG5NlQxOzR6
MDA-MB-435NH:0N|FkgXSxdH;4bYNqfHliYYPzZZk>NVj6WWJXhjFyMDFOwG0>NGfjUIdIUTVyPUCuNFgh|ryPMl7IPVI1ODN2OB?=
LNCaPMVfHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>?MoXPglUxKM7:TR?=NUPFeZNGUUN3ME2wMlUh|ryPM4\vVFE3PjVyOUi5
DU145MXzHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>?NGPhNI9IUTVyPUGuNlIh|ryPNX\KNmF{OTd4OU[0NVk>
MDA-MB-23 NUHjdHVFT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm=M3HsTmdKPTB;MD65OEDPxE1?NGHaXHoyPzZ7NkSxPS=>
MCF7MmPaS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl?M2jYN2dKPTB;Mj6zOUDPxE1?M2jOcVE4Pjl4NEG5
U87-MGMYnHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>?MkfHTWM2OD16LkW0JO69VQ>?NGDE[XQyQTd4MkK0Oi=>
PC3MXHHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>?MXLJR|UxRTJwNkWg{txOMXyxPVc3OjJ2Nh?=
HUVECNUDweGY4T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm=NEHaUmJKSzVyPUCuPFQh|ryPM3[xXVE6PzZ{MkS2
U937NYXmTHpZT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm=NWLWe2NvUUN3ME2yMlkyKM7:TR?=M1y3XFIxOzN2NEKx
SK-OV-3Ml\zSpVv[3Srb36gZZN{[Xl?M{\UTYNqemO3bY\lcpR{KFCpcD3t[YRq[XSnZDDkdpVoKHKnc3nzeIFv[2Vid3n0bEBGSzVyIH;mJFg3PyCwTR?=MU[yNFk4OzR6OB?=
SK-OV-3 MDR-1-6/6MmjaSpVv[3Srb36gZZN{[Xl?MojHZ4lz[3WvdnXueJMhWGeyLX3l[IlifGWmIHTyeYchemW|aYP0ZY5k\SC5aYToJGVEPTBib3[gNlI3QCCwTR?=M4TXUVIxQTd|NEi4
HeLaNWrRXo5QTnWwY4Tpc44h[XO|YYm=MWPpcohq[mm2c98yTWlKNXS3YoXsbY4hd25iZIL1[{B{\W6|aYTpeol1gQ>?Mmq5NlA6PzN2OEi=
HUVECNHnVZWlHfW6ldHnvckBie3OjeR?=NIXZUpN{cG:5czDhcpRq[W6paX;n[Y5q[yCjY4Tpeol1gQ>?NWDC[IE1OjF7Mki3PVQ>

... 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]
Features

Protocol(Only for Reference)

Kinase Assay: [1]

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 Assay: [1]

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.

Animal Study: [5]

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.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)0.020.151.80.40.0810
Body Surface Area (m2)0.0070.0250.150.050.020.5
Km factor36128520
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

References

[1] Rao PN, et al. Steroids. 2002, 67(13-14), 1079-1089.

[2] Seeger H, et al. J Steroid Biochem Mol Biol. 2003, 84(2-3), 255-257.

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Clinical Trial Information( data from http://clinicaltrials.gov, updated on 2016-07-30)

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

Chemical Information

Download 2-Methoxyestradiol (2-MeOE2) SDF
Molecular Weight (MW) 302.41
Formula

C19H26O3

CAS No. 362-07-2
Storage 3 years -20℃powder
6 months-80℃in solvent
Synonyms NSC 659853
Solubility (25°C) * In vitro DMSO 60 mg/mL (198.4 mM)
Water <1 mg/mL (<1 mM)
Ethanol <1 mg/mL (<1 mM)
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 Name (8R,9S,13S,14S,17S)-2-methoxy-13-methyl-7,8,9,11,12,13,14,15,16,17-decahydro-6H-cyclopenta[a]phenanthrene-3,17-diol

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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