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2-Methoxyestradiol

Cat. No. M1992
2-Methoxyestradiol Structure
Synonym:

2ME2

Size Price Availability Quantity
50mg USD 110 In stock
100mg USD 200 In stock
200mg USD 250 In stock
1g USD 520 In stock
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Quality Control
Biological Activity

2-Methoxyestradiol is a tubulin polymerization inhibitor and also decreases HIF-1 activity. 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. 2-Methoxyestradiol induces p53-induced apoptosis via two pathways: activation of p38 and NF-κB; and activation of JNK and AP-1 leading to Bcl-2 phosphorylation. 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. 2-Methoxyestradiol also upregulates death receptor 5 and binds to tubulin, inhibiting its assembly. Preclinical models also suggest that 2ME2 could also be effective against inflammatory diseases such as rheumatoid arthritis. Several studies have been conducted showing 2ME2 is a microtubule-inhibitor and effective against prostate cancer in rodents.

Protocol
Cell Experiment
Cell lines MCF-7 and MDA-MB-231 cells
Preparation method Cell culture and cell treatment.
MCF-7 estrogen receptor-positive (ER+ve) human breast cancer cells, MDA-MB-231 ER-negative (ER−ve) human breast cancer cells were obtained from the American Type Culture Collection (LGC Promochem, Teddington, UK). Cells were routinely cultured in RPMI-1640 medium supplemented with 10% (v/v) fetal calf serum, 1% L-glutamine (200 mM), 1% non-essential amino acids (100 ×) and 1% bicarbonate (7.5%) from Sigma and maintained in a humidified incubator under 5% CO2 atmosphere at 37°C. For experiments using hypoxic conditions, cells were incubated under 1% O2 and 5% CO2 atmosphere at 37°C.
Concentrations 0.5 μM
Incubation time 18 h
Animal Experiment
Animal models mice bearing MCF-7 and MDA-MB-231 xenografts model
Formulation 10% tetrahydrofuran: 90% propylene glycol
Dosages 40 or 75 mg/kg
Administration orally daily for 28 days
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
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.

Chemical Information
Molecular Weight 302.41
Formula C19H26O3
CAS Number 362-07-2
Purity 100.00%
Solubility DMSO 60 mg/mL
Storage at -20°C
Customer Product Validations & Biological Datas
Source Sci Rep (2016). Figure 5. 2-methoxyestradiol (2-ME) was purchased from Abmole
Method CHIP assay and Immunohistochemistry staining
Cell Lines in vivo experiment
Concentrations 25mg/kg daily
Incubation Time 30 days
Results Administration of 2-ME and digoxin significantly decreased AngII- mediated HIF-1α, VEGF, MMP-2 and MMP-9 overexpression in the homogenates of the whole aortas, as shown in Fig. 5A. 2-ME and digoxin decreased the AngII induced HIF-1α levels accumulation and elastin degradation in the aorta (Fig. 5B).
Rating
Source Sci Rep (2016). Figure 4. 2-methoxyestradiol (2-ME) was purchased from Abmole
Method in vivo experiment
Cell Lines
Concentrations 25mg/kg daily
Incubation Time 30 days
Results Both non-selective HIF-1α inhibitors 2-ME (25 mg/kg/day, s.c.) and digoxin (1.25 mg/kg/day, i.p.) significantly improved the survival rates (log rank test, n= 20 in each group, p < 0.05, Fig. 4B); decreased the incidences of AAA (0% vs. 84% vs. 35%, vs. 40%, p < 0.01, Fig. 4C), the severities of AAA, in terms of less type III and type IV lesions (43% vs. 15%, vs. 15%, p < 0.05, Fig. 4D) and the external diameters of the aorta (0.67 ± 0.11 mm vs. 1.68.± 0.77 vs. 0.96± 0.30 vs. 1.10± 0.53 mm, p< 0.05, Fig. 4E).
Rating
Source Sci Rep (2016). Figure 3. 2-methoxyestradiol (2-ME) was purchased from Abmole
Method CHIP assay
Cell Lines HAECs
Concentrations 6 μM
Incubation Time 30 min
Results We found that both 2-ME and digoxin attenuated AngII and oxPAPC induced up-regulation of MMP-2 and MMP-9 (n = 5, Fig. 3)
Rating
Product Citations
References

The In Vitro and In Vivo Activity of the Microtubule Disruptor STX140 Is Mediated by Hif-1 Alpha and CAIX Expression.
Stengel C, et al. Anticancer Res. 2015 Oct;35(10):5249-61. PMID: 26408684.

Mechanism of 2-methoxyestradiol-induced apoptosis and growth arrest in human breast cancer cells.
Fukui M, et al. Mol Carcinog. 2009 Jan;48(1):66-78. PMID: 18521846.

2-Methoxyestradiol, a promising anticancer agent.
Lakhani NJ, et al. Pharmacotherapy. 2003 Feb;23(2):165-72. PMID: 12587805.

2-methoxyestradiol up-regulates death receptor 5 and induces apoptosis through activation of the extrinsic pathway.
LaVallee TM, et al. Cancer Res. 2003 Jan 15;63(2):468-75. PMID: 12543804.

2-Methoxyestradiol inhibits proliferation and induces apoptosis independently of estrogen receptors alpha and beta.
LaVallee TM, et al. Cancer Res. 2002 Jul 1;62(13):3691-7. PMID: 12097276.

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Keywords: 2-Methoxyestradiol, 2ME2 supplier, HIF, inhibitors

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