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Background: 2-Methoxyestradiol is currently in clinical trials as a therapeutic against breast and ovarian cancer. 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
CAS Number: 362-07-2
Description: 2-Methoxyestradiol (2-MeOE2), an endogenous metabolite of 17β-estradiol (E2), is an inhibitor of microtubule assembly that inhibits the polymerization of tubulin and interferes with mitotic spindle dynamics leading to the blockage of mitosis of human cancer cells which lack estrogen receptors in metaphase. 2-MeOE2 is also an inhibitor of tumor growth and angiogenesis. Study results have shown that 2-MeOE2 induces mammalian cell transformation and genotoxicity in Syrian hamster embryo (SHE) fibroblasts through concentration-dependent inhibition of cell growth. Moreover, 2-MeOE2 has demonstrated anti-proliferative activity against estrogen-responsive breast cancer cell line MCF-7 and subsequent inhibition of the growth of tumors subcutaneously inoculated in mice.
Purity: 98% purity by HPLC
Solubility: Soluble in DMSO ~20 mg/ml
Storage Stability: Store at or below -20°C. Solid form is stable at least 12 months from date of receipt, when stored as directed. Do not store aqueous solutions for more than one day.
Biosafety Level: Not applicable (BSL-1)
References: 1. Tsutsui, T., et al. Carcinogensis 2000; 21(4): 735-740.
2. Attalla, H., et al. Biochem. Biophys. Res. Commun. 1996; 228: 467-473.