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Cat. No. M1992
2-Methoxyestradiol Structure


Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
10mM*1mL in DMSO USD 45  USD45 In stock
10mg USD 40  USD40 In stock
50mg USD 95  USD95 In stock
100mg USD 160  USD160 In stock
200mg USD 240  USD240 In stock
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Quality Control & Documentation
Biological Activity

2-methoxyestradiol (2-ME2), an endogenous metabolite of 17β -estradiol (E2) with oral activity, is an apoptosis inducer and angiogenesis inhibitor with effective antitumor activity. Methoxyestradiol can also destabilize microtubules. Methoxyestradiol is a potent inhibitor of superoxide dismutase (SOD) and reactive oxygen species (ROS) that can induce autophagy in transformed cell line HEK293, cancer cell line U87 and HeLa.

Product Citations
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).
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).
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)
Protocol (for reference only)
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
Chemical Information
Molecular Weight 302.41
Formula C19H26O3
CAS Number 362-07-2
Solubility (25°C) DMSO ≥ 60 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
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 Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.


[1] Stengel C, et al. Anticancer Res. The In Vitro and In Vivo Activity of the Microtubule Disruptor STX140 Is Mediated by Hif-1 Alpha and CAIX Expression.

[2] Fukui M, et al. Mol Carcinog. Mechanism of 2-methoxyestradiol-induced apoptosis and growth arrest in human breast cancer cells.

[3] Lakhani NJ, et al. Pharmacotherapy. 2-Methoxyestradiol, a promising anticancer agent.

[4] LaVallee TM, et al. Cancer Res. 2-methoxyestradiol up-regulates death receptor 5 and induces apoptosis through activation of the extrinsic pathway.

[5] LaVallee TM, et al. Cancer Res. 2-Methoxyestradiol inhibits proliferation and induces apoptosis independently of estrogen receptors alpha and beta.

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Abmole Inhibitor Catalog

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

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