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国际站:Letrozole
中文名:来曲唑
CAS:112809-51-5
品牌:MedChemExpress (MCE)
存储条件:Powder: -20°C, 3 years; 4°C, 2 years.In solvent: -80°C, 6 months; -20°C, 1 month.
生物活性:Letrozole (CGS 20267) 是一种有效、选择性、可逆和具有口服活性的芳香酶非甾体抑制剂,IC50 为 11.5 nM . Letrozole选择性抑制雌激素的生物合成,可用于乳腺癌的研究[1][2][3]。 IC50 和目标:IC50:11.5 nM(芳香酶)
体外:Letrozole (0.1-100 nM; 24-96 h) 以剂量和时间依赖性方式显着抑制 MCF-7 上皮性乳腺癌细胞的生长[2]。Letrozole ( 10 nM) 显着抑制 4-androstene-3,17-dione 或睾酮对 MCF-7 细胞增殖的刺激作用[2]。Letrozole (10 nM; 24-48 h ) 抑制 MCF-7 细胞中分泌的金属蛋白酶(MMP-2 和 MMP-9)的水平[2]。
体内:Letrozole (3-300 μg/kg; 每天口服一次,持续 6 周) 对大鼠具有抗肿瘤作用[3]。
参考文献:[1]. Bhatnagar AS, et, al. Highly selective inhibition of estrogen biosynthesis by CGS 20267, a new non-steroidal aromatase inhibitor. J Steroid Biochem Mol Biol. 1990 Dec 20;37(6):1021-7.[2]. Mitropoulou TN, et, al. Letrozole as a potent inhibitor of cell proliferation and expression of metalloproteinases (MMP-2 and MMP-9) by human epithelial breast cancer cells. Int J Cancer. 2003 Mar 20;104(2):155-60.[3]. Schieweck K, et, al. Anti-tumor and endocrine effects of non-steroidal aromatase inhibitors on estrogen-dependent rat mammary tumors. J Steroid Biochem Mol Biol. 1993 Mar;44(4-6):633-6.
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