2-Methoxyestradiol is a metabolite of estradiol that exhibits anti-angiogenic, vasodilatory, antihypertensive, anti-fibrotic, anticancer chemotherapeutic and chemopreventive activities. 2-Methoxyestradiol also displays antimitotic activity, binding the colchicine site of tubulin and stabilizing microtubule polymerization. This compound decreases tumor growth, VEGF expression, and angiogenesis in animal models of hepatocellular carcinoma and prevents initial development of tumors in animal models of prostate cancer. In hypertensive rates, 2-methoxyestradiol decreases mean arterial blood pressure. Additionally, this compound inhibits TGF-β3-induced fibrosis in vitro, decreasing expression of collagen, PAI-1, CTGF, and α-SMA and preventing phosphorylation of Smad2/3.