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Flutamide

CAS号

13311-84-7

分子式

C11H11F3N2O3

主要靶点

Androgen Receptor

仅限科研使用

Cat No : CM01087

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Synonyms

SCH 13521|SCH13521|SCH-13521|氟他胺|Inhibitor|Androgen Receptor|AndrogenReceptor|Flutamide|inhibit



产品信息

CAS号 13311-84-7
分子式 C11H11F3N2O3
主要靶点 Androgen Receptor
主要通路 内分泌与激素
分子量 276.21
纯度 100%, 此纯度可做参考,具体纯度与批次有关系,可咨询客服
储存条件 Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
别名 SCH 13521|SCH13521|SCH-13521|氟他胺|Inhibitor|Androgen Receptor|AndrogenReceptor|Flutamide|inhibit

靶点活性

Androgen receptor:55 nM(Ki)

体内活性

Flutamide和亮丙瑞林联合使用可以用于治疗前列腺癌。Flutamide-OH是Flutamide的活性代谢物形式,直接结合大鼠垂体前叶雄性激素受体(Ki=55 nM)。Flutamide不影响小鼠乳腺癌Shionogi SC-l 15细胞在培养基中雄性激素敏感克隆的增殖,仅表现出抗雄激素作用,而没有雄激素作用。

体外活性

Flutamide使大鼠前列腺重量明显从319 mg降低到245 mg.联合使用Flutamide和黄体生成素释放激素激动剂引发副作用,使前列腺重量降低到101 mg,并且前列腺ODC活性明显下降.

溶解度

Ethanol:51 mg/mL (184.64 mM);DMSO:55 mg/mL (199.12 mM)

细胞实验

Effect of flutamide on the growth of an androgen-sensitive clone (SEM-l) of mouse mammary carcinoma Shionogi cells in culture. The cells are incubated up to 40 days in medium (MEM + 2% dextran-coated charcoal extracted fetal calf serum) containing the compounds at a concentration of 1 μM. Media are changed every second day.(Only for Reference)

参考文献

1.Simard J, et al. Mol Cell Endocrinol, 1986, 44(3), 261-270.
2.Luthy IA, et al. J Steroid Biochem, 1988, 31(5), 845-852.
3.Crawford ED, et al. N Engl J Med, 1989, 321(7), 419-424.
4.Marchetti B, et al. J Steroid Biochem, 1988, 29(6), 691-698.

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