Description
A SERM; inhibits E2-induced transcriptional activity of ERα and ERβ (IC50s = 2 and 0.4 nM, respectively); binds to ERs in cytosol from human breast cancer and non-cancerous uterine cells (Kis = 0.047 and 0.042 nM, respectively); binds 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); 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); inhibits E1-stimulated tumor growth in a ZR-75-1 human breast cancer xenograft model in ovariectomized mice (50 μg per day); inhibits E1-stimulated endometrial epithelium thickening in vivo in ovariectomized mice (50 μg per day)
Formal name: (2S)-3-(4-hydroxyphenyl)-4-methyl-2-[4-[2-(1-piperidinyl)ethoxy]phenyl]-2H-1-benzopyran-7-ol
Synonyms: SCH 57068
Molecular weight: 457.6
CAS: 182167-02-8
Purity: ≥98%
Formulation: A solid
Product Type|Biochemicals|Receptor Pharmacology||Research Area|Cancer||Research Area|Endocrinology & Metabolism|Hormones & Receptors|Estrogens & Progestins||Research Area|Endocrinology & Metabolism|Reproductive Biology
