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MCE 国际站:Exemestane
中文名:依西美坦
CAS:107868-30-4
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:Exemestane (FCE 24304) 是一种选择性、不可逆和具有口服活性的甾体芳香酶抑制剂,对的IC50分别为 30 nM 和 40 nM >人胎盘l和大鼠卵巢芳香化酶,分别。依西美坦可用于激素依赖性乳腺癌研究[1][2]。 IC50 和目标:IC50:30 nM(人胎盘芳香酶)和 40 nM(大鼠卵巢芳香酶)[1]
体外:依西美坦(EXE;1-1000 nM;72 小时;hFOB,Saos-2 细胞<)处理显着增加细胞数量[2]。依西美坦(0.1- μM;72小时)增加 hFOB 和 Saos-2 细胞中的碱性磷酸酶活性,并诱导 hFOB 细胞中 MYBL2、OSTM1、HOXD11、ADCYAP1R1 和磷脂酰肌醇蛋白聚糖 2 的表达[2]。依西美坦竞争性抑制和时间依赖性地灭活人胎盘芳香酶,Ki 为 4.3 nM。依西美坦取代大鼠前列腺雄激素受体中的 [3H]5α-二氢睾酮,IC50 为 0.9 μM[1]。
体内:依西美坦(EXE;20-100 mg/kg;肌肉注射;每周一次;持续 16 周)治疗显着增加腰椎和股骨 BMD、股骨弯曲强度、第五腰椎抗压强度和骨小梁体积。依西美坦显着降低卵巢切除术引起的血清吡啶啉和血清骨钙素的增加。依西美坦显着降低血清胆固醇和低密度脂蛋白胆固醇[3]。依西美坦(20 毫克/千克/天皮下注射)诱导 26% 的完全 (CR) 和 18% 的部分 ( PR) 大鼠体内 7,12-二甲基苯并蒽 (DMBA) 诱导的乳腺肿瘤肿瘤消退[4]。
热销产品:Acifran | D-Serine | Baricitinib (phosphate) | Butylated hydroxytoluene | Rebamipide | Panitumumab (anti-EGFR) | Gypenoside XLVI | Trifarotene | CJJ300 | Tolbutamide
研究领域:Metabolic Enzyme/Protease
作用靶点:Cytochrome P450
Trending products:Recombinant Proteins | Bioactive Screening Libraries | Natural Products | Fluorescent Dye | PROTAC | Isotope-Labeled Compounds | Oligonucleotides
参考文献:[1]. Di Salle, E., et al., Novel aromatase and 5 alpha-reductase inhibitors. J Steroid Biochem Mol Biol, 1994. 49(4-6): p. 289-94.
[2]. Miki, Y, et al. Effects of aromatase inhibitors on human osteoblast and osteoblast-like cells: a possible androgenic bone protective effects induced by exemestane. Bone. 2004 Sep 1;10(17):5717-23.
[3]. Goss, P.E., et al., Effects of the steroidal aromatase inhibitor exemestane and the nonsteroidal aromatase inhibitor letrozole on bone and lipid metabolism in ovariectomized rats. Clin Cancer Res, 2004. 10(17): p. 5717-23.
[4]. Zaccheo, T., D. Giudici, and E. Di Salle, Inhibitory effect of combined treatment with the aromatase inhibitor exemestane and tamoxifen on DMBA-induced mammary tumors in rats. J Steroid Biochem Mol Biol, 1993. 44(4-6): p. 677-80.
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