2-methoxyestradiol - CAS 362-07-2
Catalog number:
Not Intended for Therapeutic Use. For research use only.
HIF/HIF Prolyl-Hydroxylase
2-methoxyestradiol, also known as 2-ME, is an orally bioavailable estradiol metabolite with potential antineoplastic activity. 2-Methoxyestradiol inhibits angiogenesis by reducing endothelial cell proliferation and inducing endothelial cell apoptosis. This agent also inhibits tumor cell growth by binding to tubulin, resulting in antimitotic activity, and by inducing caspase activation, resulting in cell cycle arrest in the G2 phase, DNA fragmentation, and apoptosis.
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white solid powder
2-ME; 2-Methoxy Estradiol. US brand name: Panzem. Abbreviation: 2ME2. Chemical structure name: (17beta)-2-Methoxyestra-1,3,5(10)-triene-3,17-diol.
Current Developer:
EntreMed, Inc.
1.Recent Advances in chemistry and pharmacology of 2-methoxyestradiol: An anticancer investigational drug.
Kumar BS1, Raghuvanshi DS1, Hasanain M2, Alam S1, Sarkar J2, Mitra K2, Khan F1, Negi AS3. Steroids. 2016 Mar 26. pii: S0039-128X(16)30001-0. doi: 10.1016/j.steroids.2016.03.017. [Epub ahead of print]
2-Methoxyestradiol (2ME2), an estrogen hormone metabolite is a potential cancer chemotherapeutic agent. Presently, it is an investigational drug under various phases of clinical trials alone or in combination therapy. Its anticancer activity has been attributed to its antitubulin, antiangiogenic, pro-apoptotic and ROS induction properties. This anticancer drug candidate has been explored extensively in last twenty years for its detailed chemistry and pharmacology. Present review is an update of its chemistry and biological activity. It also extends an assessment of potential of 2ME2 and its analogues as possible anticancer drug in future.
2.Nitro-oxidative Stress Is Involved in Anticancer Activity of 17β-Estradiol Derivative in Neuroblastoma Cells.
Gorska M1, Kuban-Jankowska A2, Milczarek R3, Wozniak M2. Anticancer Res. 2016 Apr;36(4):1693-8.
Neuroblastoma is one of the most common childhood malignancies and the primary cause of death from pediatric cancer. Derivatives of 17β-estradiol, 2-methoxyestradiol, as well as selective estrogen receptor modulators, such as fulvestrant, are novel potentially active anticancer agents. In particular, 2-methoxyestradiol is effective in treatment of numerous malignancies, including breast and prostate cancer, Ewing sarcoma, and osteosarcoma. Herein, we treated neuroblastoma SH-SY5Y cells with physiologically and pharmacologically relevant concentrations of 2-methoxyestradiol. We used flow cytometry in order to determine cell viability, cell death, level of nitric oxide and mitochondrial membrane potential. We demonstrated that at pharmacologically relevant concentrations, 2-methoxyestradiol results in induction of apoptosis of neuroblastoma SH-SY5Y cells via nitric oxide generation and reduction of mitochondrial membrane potential. Based on the obtained data, we propose that 2-methoxyestradiol may be a natural modulator of cancer cell death and survival through nitro-oxidative stress-dependent mechanisms.
3.[Effect of 2-methoxyestradiol combined with quercetin on prostate cancer in vitro].
Song LM1, Wang GD, Wang HP, Xing NZ. Zhonghua Yi Xue Za Zhi. 2016 Jan 12;96(2):95-9. doi: 10.3760/cma.j.issn.0376-2491.2016.02.004.
OBJECTIVE: To detect the effects of quercetin (Que) combined with 2-methoxyestradiol (2-ME) on the proliferation of androgen-dependent LNCaP human prostate cancer cells line and androgen-independent PC-3 human prostate cancer cells line, and to evaluate the antitumor effects of different combos of the two drugs.
4.Oxidative pathways in response to polyunsaturated aldehydes in the marine diatom Skeletonema marinoi (Bacillariophyceae).
Gallina AA1, Palumbo A1, Casotti R1. J Phycol. 2016 Apr 8. doi: 10.1111/jpy.12421. [Epub ahead of print]
Polyunsaturated aldehydes (PUA) have recently been shown to induce reactive oxygen species (ROS) and possibly reactive nitrogen species (RNS, e.g. peroxynitrite) in the diatom Skeletonema marinoi (S. marinoi), which produces high amounts of PUA. We now are attempting to acquire better understanding of which reactive molecular species are involved in the oxidative response of S. marinoi to PUA. We used flow cytometry, the dye Dihydrorhodamine 123 (DHR) as the main indicator of ROS (but which is also known to partially detect RNS), and different scavengers and inhibitors of both NO synthesis and superoxide dismutase activity (SOD). Both the scavengers Tempol (for ROS) and Uric Acid (UA, for peroxynitrite) induced a lower DHR-derived green fluorescence in S. marinoi cells exposed to the PUA, suggesting that both reactive species were produced. When PUA-exposed S. marinoi cells were treated with the NO scavenger 2-4-carboxyphenyl-4,4,5,5-tetramethylimidazoline-1-oxyl-3-oxide (cPTIO), an opposite response was observed, with an increase in DHR-derived green fluorescence.
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CAS 362-07-2 2-methoxyestradiol

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