Bazedoxifene-d4 is intended for use as an internal standard for the quantification of bazedoxifene by GC- or LC-MS. Bazedoxifene is a third generation selective estrogen receptor modulator (SERM). It is an indole-based ER ligand that binds to both ERα (IC50 = 26 nM) and ERβ (IC50 = 99 nM).1 Bazedoxifene antagonizes 17β-estradiol-dependent MCF-7 and T47D breast cancer cell proliferation in vitro as well as hormone-independent growth of MCF-7:5C cells that are resistant to long-term estrogen deprivation (80% reduction with 10 nM).2 It has been shown to arrest cell cycling by downregulating cyclin D1 and ERα.
1.Komm, B.S., Kharode, Y.P., Bodine, P.V.N., et al.Bazedoxifene acetate: A selective estrogen receptor modulator with improved selectivityEndocrinology146(9)3999-4008(2005) 2.Lewis-Wambi, J.S., Kim, H., Curpan, R., et al.The selective estrogen receptor modulator bazedoxifene inhibits hormone-independent breast cancer cell growth and down-regulates estrogen receptor α and cyclin D1Mol. Pharmacol.80(4)610-620(2011)