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2-Methoxyestradiol (2-MeOE2)

Name: 2-Methoxyestradiol (2-MeOE2)
Brand: Selleck Chemicals
SKU: S1233
Rating: 5 (65 reviews)

Catalog No.S1233 Synonyms: NSC 659853, 2-ME2

For research use only.

2-Methoxyestradiol (2-MeOE2, NSC 659853, 2-ME2) depolymerizes microtubules and blocks HIF-1α nuclear accumulation and HIF-transcriptional activity. 2-Methoxyestradiol induces both autophagy and apoptosis in various carcinogenic cell lines. Phase 2.

2-Methoxyestradiol (2-MeOE2) Chemical Structure

CAS No. 362-07-2

Selleck's 2-Methoxyestradiol (2-MeOE2) has been cited by 65 publications

Purity & Quality Control

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HIF Signaling Pathway Map

Biological Activity

Description

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	MkPqZ5l1d3SxeHnjbZR6KGG\|c3H5	NWfj[4NnhjFyMDFOwG0>	MY\HTVUxRTBwN{Cg{txO	MX[5NlQxOzR6
HCT-116	MV\jfZRwfG:6aXPpeJkh[XO\|YYm=	Mn33glExOCEQvF2=	NV70clNmT0l3ME2wMlQ4KM7:TR?=	M2[yUlkzPDB\|NEi=
SF-539	NVfJXJJG[3m2b4TvfIlkcXS7IHHzd4F6	NXfUbGtZhjFyMDFOwG0>	NHfMdHhIUTVyPUCuN\|Ih\|ryP	M3;rbFkzPDB\|NEi=
UACC-62	MkC0Z5l1d3SxeHnjbZR6KGG\|c3H5	NV:2U2tphjFyMDFOwG0>	MonyS2k2OD1yLkO2JO69VQ>?	MUC5NlQxOzR6
OVCAR-3	NHL0OZlkgXSxdH;4bYNqfHliYYPzZZk>	NV;Cc\|luhjFyMDFOwG0>	M3\NUGdKPTB;MD6yNUDPxE1?	M3e4c\|kzPDB\|NEi=
SN12C	MXjjfZRwfG:6aXPpeJkh[XO\|YYm=	MWD+NVAxKM7:TR?=	NIDVcXFIUTVyPUCuPVUh\|ryP	MkC0PVI1ODN2OB?=
DU-145	MYLjfZRwfG:6aXPpeJkh[XO\|YYm=	MWD+NVAxKM7:TR?=	M3\uUGdKPTB;MT64JO69VQ>?	NV\xemhOQTJ2MEO0PC=>
MDA-MB-435	M1W0doN6fG:2b4jpZ4l1gSCjc4PhfS=>	MYn+NVAxKM7:TR?=	NHHscHNIUTVyPUCuNFgh\|ryP	NGO1Upk6OjRyM{S4
LNCaP	M1jLV2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7	Ml3GglUxKM7:TR?=	MVvJR\|UxRTBwNTFOwG0>	MmTGNVY3PTB7OEm=
DU145	MXPHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>?		MkT5S2k2OD1zLkKyJO69VQ>?	MlG4NVc3QTZ2MUm=
MDA-MB-23	MV\Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>?		NH3GU4hIUTVyPUCuPVQh\|ryP	Mkf0NVc3QTZ2MUm=
MCF7	MVHHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>?		NXzIb5ZnT0l3ME2yMlM2KM7:TR?=	NVPCSYxHOTd4OU[0NVk>
U87-MG	MX7Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>?		NWnVcpNEUUN3ME24MlU1KM7:TR?=	NHHjO\|kyQTd4MkK0Oi=>
PC3	M3yySWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7		Ml3uTWM2OD1{Lk[1JO69VQ>?	M4mxR\|E6PzZ{MkS2
HUVEC	NX7G[IxGT3Kxd4ToJIlvcGmkaYTvdpkh[XO\|YYm=		NYjTWGhkUUN3ME2wMlg1KM7:TR?=	MoTHNVk4PjJ{NE[=
U937	MYTHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>?		NGPzdVZKSzVyPUKuPVEh\|ryP	MWiyNFM{PDR{MR?=
SK-OV-3	MWDGeY5kfGmxbjDhd5NigQ>?		MorKZ4lz[3WvdnXueJMhWGeyLX3l[IlifGWmIHTyeYchemW\|aYP0ZY5k\SC5aYToJGVEPTBib3[gPFY4KG6P	MYGyNFk4OzR6OB?=
SK-OV-3 MDR-1-6/6	M1TV[mZ2dmO2aX;uJIF{e2G7		NEjyVIxkcXKldX32[Y51eyCSZ4CtcYVlcWG2ZXSg[JJ2\yC{ZYPpd5RidmOnIIfpeIghTUN3MDDv[kAzOjZ6IH7N	MXiyNFk4OzR6OB?=
HeLa	M4HWcWZ2dmO2aX;uJIF{e2G7		MVPpcohq[mm2c98yTWlKNXS3YoXsbY4hd25iZIL1[{B{\W6\|aYTpeol1gQ>?	MYmyNFk4OzR6OB?=
HUVEC	MU\GeY5kfGmxbjDhd5NigQ>?		M4LU[ZNpd3e\|IHHueIlidmerb3flcolkKGGldHn2bZR6	Mn3FNlE6Ojh5OUS=

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 (from 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 Research:^[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 Research:^[5]	Animal Models: 9L-V6R cells are injected into the brains of Fischer 344 rats Dosages: ≤600 mg/kg Administration: Administered via i.p.

References

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Solubility (25°C)

In vitro


In vivo	Add solvents to the product individually and in order (Data is from Selleck tests instead of citations): 2%DMSO+30%PEG300+5%Tween 80+ddH2O For best results, use promptly after mixing. Click to purchase: PEG300 Tween 80	5mg/mL

Chemical Information

Molecular Weight	302.41
Formula	C₁₉H₂₆O₃
CAS No.	362-07-2
Storage	3 years	-20°C	powder
Storage	2 years	-80°C	in solvent
Smiles	CC12CCC3C(C1CCC2O)CCC4=CC(=C(C=C34)OC)O

Download 2-Methoxyestradiol (2-MeOE2) SDF

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