Acolbifene (Synonyms: SCH 57068) |
カタログ番号GC18362 |
EM800 の活性代謝物であるアコルビフェン (EM-652) は、経口で活性な純粋な抗エストロゲンおよび選択的エストロゲン受容体アンタゴニストです。アコルビフェン (EM-652) は、エストラジオール (E2) によって誘導される ERα (IC50 = 2 nM) および ERβ (IC50 = 0.4 nM) の転写活性を阻害します。アコルビフェン (EM-652) は、強力で純粋な抗発がん特性を持っています。
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Cas No.: 182167-02-8
Sample solution is provided at 25 µL, 10mM.
Acolbifene is a selective estrogen receptor modulator (SERM). It inhibits transcriptional activity of estrogen receptor α (ERα) and ERβ induced by estradiol . 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). 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. Acolbifene (50 μg per day) inhibits tumor growth stimulated by estrone in a ZR-75-1 human breast cancer xenograft model in ovariectomized mice. It also inhibits E1-stimulated endometrial epithelium thickening in vivo in ovariectomized mice when administered at a dose of 50 μg per day.
References:
[1].Labrie, F., Labrie, C., Bélanger, A., et al. EM-652 (SCH 57068), a third generation SERM acting as pure antiestrogen in the mammary gland and endometrium J. Steroid Biochem. Mol. Biol. 69(1-6), 51-84 (1999).
[2]. Martel, C., Provencher, L., Li, X., et al. Binding characteristics of novel nonsteroidal antiestrogens to the rat uterine estrogen receptors J. Steroid Biochem. Mol. Biol. 64(3-4), 199-205 (1998).
[3]. Gutman, M., Couillard, S., Roy, J., et al. Comparison of the effects of EM-652 (SCH57068), tamoxifen, toremifene, droloxifene, idoxifene, GW-5638 and raloxifene on the growth of human ZR-75-1 breast tumors in nude mice Int. J. Cancer 99(2), 273-278 (2002).
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