Bazedoxifene acetate

Bazedoxifene acetate (TSE 424; WAY-TES 424), a novel selective estrogen receptor modulator (SERM), has been developed to have favorable effects on bone and the lipid profile while minimizing stimulation of uterine or breast tissues. (In Vitro):Bazedoxifene acetate is a small molecular GP130 inhibitor, which binds to GP130 D1 domain.Bazedoxifene acetate inhibits STAT3 phosphorylation induced by Il-6 and IL-11 in GP130/STAT3 pathway signaling.Bazedoxifene acetate (10 μM-20 μM; 2 hours) inhibits STAT3 Phosphorylation Induced by cytokines in human pancreatic cancer cells.Bazedoxifene acetate (5-20 μM; overnight) induces apoptosis in human pancreatic cancer cells.Bazedoxifene acetate inhibits STAT3 nuclear translocation induced by IL-6.Bazedoxifene acetate blocks the cells migration in pancreatic cancer cells by inhibition of GP130.(In Vivo):Bazedoxifene acetate (5 mg/kg; i.g.; daily, for 18 days) inhibits Capan-1 tumor growth in mouse model in vivo.