2-Methoxyestradiol (2ME2) is a drug that prevents the formation of new blood vessels that tumors need in order to grow (angiogenesis). It is derived from estrogen, although it binds poorly to known estrogen receptors, and belongs to the family of drugs called angiogenesis inhibitors. It has undergone Phase 1 clinical trials against breast cancers. Preclinical models also suggest that 2ME2 could also be effective against inflammatory diseases such as rheumatoid arthritis. The CAS name for 2ME2 is (17 bêta)-2-methoxyestra-1, 3, 5(10)-triene-3, 17-diol. It also acts as a vasodilator.
2-Methoxy 17β-Estradiol is a natural metabolite of 17β-Estradiol which is devoid of estrogenic activity. Inhibits cell proliferation and angiogenesis. 2-Methoxy 17β-Estradiol binds to the colchicine binding site of tubulin, and has been suggested to function as a natural regulator of microtubule assembly and function.
