Formulation: A solid
Formal Name: (2S)-3-(4-hydroxyphenyl)-4-methyl-2-[4-[2-(1-piperidinyl)ethoxy]phenyl]-2H-1-benzopyran-7-ol
Purity: ≥98%
Formula Markup: C29H31NO4
Formula Weight: 457,6
Shelf life (days): 1460
CAS Number: 182167-02-8
Notes: Acolbifene is a selective estrogen receptor modulator (SERM). It inhibits transcriptional activity of estrogen receptor α (ERα) and ERβ induced by estradiol (E2; Item No. 10006315; IC50s = 2 and 0.4 nM, respectively).{38866} It binds to ERs in cytosol from human breast cancer and non-cancerous uterine cells (Kis = 0.047 and 0.042 nM, respectively) and to ERs in cytosol from rat uterine cells (IC50 = 0.44 nM) but not to progesterone or androgen receptors in cytosol from rat uterine and ventral prostate cells (IC50s = 22,500 and >10,000 nM, respectively).{38866,38867} Acolbifene inhibits E2-stimulated proliferation of T47D, ZR-75-1, and MCF-7 breast cancer cells (IC50s = 0.146, 0.75, and 0.321 nM, respectively) but not basal proliferation.{38866} Acolbifene (50 μg per day) inhibits tumor growth stimulated by estrone (E1; Item No. 10006485) in a ZR-75-1 human breast cancer xenograft model in ovariectomized mice.{38868} It also inhibits E1-stimulated endometrial epithelium thickening in vivo in ovariectomized mice when administered at a dose of 50 μg per day.
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