Flutamide | 氟他胺

MCE 国际站：Flutamide

中文名：氟他胺

CAS：13311-84-7

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：Flutamide 是一种抗雄激素药物，其活性代谢物与雄激素受体结合，Ki 值为 55 nM，主要用于治疗前列腺癌。靶标：体外雄激素受体：氟他胺 (Eulexin) 是一种抗雄激素药物。 Flutamide-OH 是氟他胺的活性代谢物，直接结合大鼠垂体前叶雄激素受体，Ki 值为 55 nM [1]。 lutamide不影响培养的雄激素敏感克隆小鼠乳腺癌盐野义SC-l 15细胞的增殖，仅显示抗雄激素作用，而无雄激素作用[2]。当与亮丙瑞林一起使用时，氟他胺可治疗前列腺癌 [3]。体内：氟他胺可使大鼠腹侧前列腺重量从 319 毫克显着降低至 245 毫克。氟他胺和 LHRH 激动剂的组合会产生累加效应，使前列腺重量减少至 101 mg，并显着降低前列腺 ODC 活性 [4]。

体外：Flutamide 的活性代谢物是 Flutamide-OH。 两者均直接结合大鼠垂体前叶雄激素受体(Ki=55 nM)[1]。Flutamide 不影响培养的小鼠乳腺癌Shionogi SC-l 15细胞的雄激素敏感克隆的增殖，仅显示抗雄激素作用，但不显示雄激素作用[2]。Flutamide 与 Leuprolides 一起使用可抑制前列腺癌[3]。Flutamide 对 PC3 和 LNCap 具有细胞毒活性 (IC50s 分别为 20 μM 和 12 μM)。Flutamide (10 μM, 5 μM; 48 h) 诱导 PC3 和 LNCap 细胞凋亡，减少细胞迁移和定植[4]。Flutamide 还下调细胞中 KLK2 和 EMT 通路基因的表达[4]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内：Flutamide 导致大鼠腹侧前列腺重量从 319 mg 显着减少至 245 mg。Flutamide 和 LHRH 激动剂的组合可产生叠加效应，前列腺重量降至 101 mg，前列腺 ODC 活性显着下降[5]。Flutamide (12.5-50 mg/kg；皮下注射；每天一次，连续 3 天) 缓解热应激小鼠的中暑[6]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. Clinical Trial

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研究领域：Vitamin D Related/Nuclear Receptor

作用靶点：Androgen Receptor

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参考文献：[1]. Simard J, et al. Characteristics of interaction of the antiandrogen flutamide with the androgen receptor in various target tissues. Mol Cell Endocrinol. 1986 Mar;44(3):261-70.

[2]. Luthy IA, et al. Androgenic activity of synthetic progestins and spironolactone in androgen-sensitive mouse mammary carcinoma (Shionogi) cells in culture. J Steroid Biochem. 1988 Nov;31(5):845-52.

[3]. Crawford ED, et al. A controlled trial of leuprolide with and without flutamide in prostatic carcinoma. N Engl J Med. 1989 Aug 17;321(7):419-24.

[4]. Rahimnia R, et al. The effect of Ganoderma lucidum polysaccharide extract on sensitizing prostate cancer cells to flutamide and docetaxel: an in vitro study. Sci Rep. 2023 Nov 2;13(1):18940.

[5]. Lin CY, et al. Flutamide, an androgen receptor antagonist, improves heatstroke outcomes in mice. Eur J Pharmacol. 2012 Aug 5;688(1-3):62-7.

[6]. Marchetti B, et al. Characteristics of flutamide action on prostatic and testicular functions in the rat. J Steroid Biochem. 1988 Jun;29(6):691-8.