Description
2-Methoxyestradiol (2ME2) is a naturally occurring metabolite of 17beta-estradiol with antiproliferative, antiangiogenic, and proapoptotic activity, and is considered to have potential clinical benefit in the treatment of cancer.
Storage
2 years at -20 centigrade
Targets
hypoxia-inducible factor-1
Molecular Formula
C19H2603
Chemical Name
(8R,9S,13S,14S,17S)-2-methoxy-13-methyl-7,8,9,11,12,13,14,15,16,17-decahydro-6H-cyclopenta[a]phenanthrene-3,17-diol
Solubility
DMSO 61 mg/mL Water
In vitro
2-Methoxyestradiol (2ME2) is a naturally occurring metabolite of 17beta-estradiol with antiproliferative, antiangiogenic, and proapoptotic activity, and is considered to have potential clinical benefit in the treatment of cancer. 2-Methoxyestradiol (2ME2) can inhibit HCT116 and MCF7 with GI50 of 0.8 nM and 0.9 nM. 2ME2 does not interact with the estrogen receptors. Its major target is believed to be the cellular microtubule skeleton. 2ME2 has been shown to inhibit the polymerization of tubulin in vitro, thus disrupting normal microtubule function. However, at therapeutic doses in vivo, the drug is likely to act by impairing microtubule dynamics. Given that rapid microtubule dynamics are essential for the correct assembly and function of the mitotic spindle, 2ME2 activates the spindle assembly checkpoint and causes metaphase arrest, and as a consequence, inhibition of cell proliferation and induction of cellular apoptosis.
In vivo
2-ME2 is an antiproliferative and anticancer agent for in vivo studies against Barrett esophageal adenocarcinoma (BEAC) and inhibiting the growth of BEAC xenografts.
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