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2-Methoxyestradiol (2-MeOE2) HIF inhibitor

Name: 2-Methoxyestradiol (2-MeOE2)
Brand: Selleck Chemicals
SKU: S1233
Availability: InStock
Rating: 5 (89 reviews)

Cat.No.S1233

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

Chemical Structure

Molecular Weight: 302.41

Jump to Mechanism of Action Cell Culture & Working Concentration Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: Purity: 99.99%

99.99

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Cell Culture, Treatment & Working Concentration

Cell Lines	Assay Type	Concentration	Activity Description
HOP-62	cytotoxicity assay	~100 μM	GI50=0.70 μM
HCT-116	cytotoxicity assay	~100 μM	GI50=0.47 μM
SF-539	cytotoxicity assay	~100 μM	GI50=0.32 μM
UACC-62	cytotoxicity assay	~100 μM	GI50=0.36 μM
OVCAR-3	cytotoxicity assay	~100 μM	GI50=0.21 μM
SN12C	cytotoxicity assay	~100 μM	GI50=0.95 μM
DU-145	cytotoxicity assay	~100 μM	GI50=1.8 μM
MDA-MB-435	cytotoxicity assay	~100 μM	GI50=0.08 μM
LNCaP	Growth inhibitory assay	~50 μM	IC50=0.5 μM
DU145	Growth inhibitory assay		GI50=1.22 μM
MDA-MB-23	Growth inhibitory assay		GI50=0.94 μM
MCF7	Growth inhibitory assay		GI50=2.35 μM
U87-MG	Growth inhibitory assay		IC50=8.54 μM
PC3	Growth inhibitory assay		IC50=2.65 μM
HUVEC	Growth inhibitory assay		IC50=0.84 μM
U937	Growth inhibitory assay		IC50=2.91 μM
SK-OV-3	Function assay		circumvents Pgp-mediated drug resistance with EC50 of 867 nM
SK-OV-3 MDR-1-6/6	Function assay		circumvents Pgp-mediated drug resistance with EC50 of 2268 nM
HeLa	Function assay		inhibitsβIII-tubulin on drug sensitivity
HUVEC	Function assay		shows antiangiogenic activity
Click to View More Cell Line Experimental Data

Chemical Information, Storage & Stability

Molecular Weight	302.41	Formula	C₁₉H₂₆O₃	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	362-07-2	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	NSC 659853, 2-ME2			Smiles	CC12CCC3C(C1CCC2O)CCC4=CC(=C(C=C34)OC)O

Solubility

In vitro
Batch:

DMSO : 60 mg/mL (198.4 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	10%DMSO 1 40%PEG300 2 5%TWEEN80 3 45%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	6.000mg/ml (19.84mM)	Taking the 1 mL working solution as an example, add 100 μL of 60 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 450 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC₅₀/Ki	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 (2-MeOE2) 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, it also inhibits cellular microtubule depolymerization in rat aortic smooth muscle A-10 cells with EC50 of 7.5 μM. ^[1] This compound inhibits proliferation of MCF-7 and BM cells with IC50 of 52 μM and 8 μM. ^[2] In MDA-MB-231 cells, it inhibits HIF-1-mediated transcriptional activation of target genes without affecting the transcription of HIF-1α itself. ^[3] A recent study shows that 2-MeOE2 (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, it ameliorates TGF-β3-induced Smad2/3 phosphorylation and nuclear translocation, and inhibits TGF-β3-induced activation of the PI3K/Akt/mTOR pathway. ^[4]
Kinase Assay	Microtubule depolymerizing activity
Kinase Assay	The effects of 2-Methoxyestradiol (2-MeOE2) 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 determine 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 are calculated from the log dose–response curves.
In vivo	In a 9L rat glioma (9L-V6R) rat model, 2-Methoxyestradiol (2-MeOE2) significantly decreases HIF-1 activity and inhibits tumor growth in a dose-dependent manner, with a 4-fold reduction at 60 mg/kg/day and a 23-fold reduction at 600 mg/kg/day, respectively. ^[5]
References	[1] https://pubmed.ncbi.nlm.nih.gov/12441194/ [2] https://pubmed.ncbi.nlm.nih.gov/12711011/ [3] https://pubmed.ncbi.nlm.nih.gov/12726862/ [4] https://pubmed.ncbi.nlm.nih.gov/22579131/ [5] https://pubmed.ncbi.nlm.nih.gov/17178898/ [6] https://pubmed.ncbi.nlm.nih.gov/21115915/ [7] https://pubmed.ncbi.nlm.nih.gov/25218350/

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