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雌莫司汀磷酸钠
产品纠错
CAS号:52205-73-9 | 英文名称:Estramustine sodium phosphate
分子式 C23H33Cl2NNaO6P
分子量 544
EINECS号 257-735-7
MDL MFCD00866320
Smiles
InChIKey
乙二醇化学百科
基本信息
中文名称 雌莫司汀磷酸钠
英文名称 Estramustine sodium phosphate
CAS号 52205-73-9
分子式 C23H33Cl2NNaO6P
分子量 544.38
EINECS号 257-735-7
物化性质
溶解度 H2O中可溶50mg/mL
形态 结晶固体
颜色 白色至米白色
稳定性 吸湿性,溶液不稳定
安全信息
危险品标志 Xi
危险类别码 37
安全说明 26
WGK Germany 3
RTECS号 KG7350000
海关编码 29242990
生产及用途
Estramustine phosphate sodium (EMP, Emcyt, Estracyt)是一种具有独特双重作用模式的抗肿瘤药。Estramustine phosphate sodium的代谢产物estrone和estradiol具有抗促性腺激素的活性,导致睾丸激素水平降低。Estramustine(estramustine phosphate sodium去磷酸化作用产生的细胞毒性代谢产物)是一种具有抗微管作用的抗前列腺肿瘤药物。

Estramustine phosphate sodium (1 µg/mL) treatment suppressed PC3 cell growth.
Estramustine phosphate sodium (2 µg/mL) treatment significantly elevates phosphatidylserine eversion amount on PC3 cells. Estramustine phosphate sodium induces PC3 cell apoptosis.
Estramustine phosphate sodium (2 µg/mL) treatment decreases MiR-31 level. Estramustine phosphate odium induces s prostate cancer cell line PC3 apoptosis through reducing miR-31.
Estramustine phosphate sodium, a unique antitumour agent, is selectively taken up by prostate cells and exerts antineoplastic effects by interfering with microtubule of dynamics and by reducing plasma levels of testosterone.
Estrone and estradiol, products of the metabolism of Estramustine phosphate sodium, have shown antigonadotrophic activity resulting in reduced testosterone levels similar to those achieved after surgical castration.

Estramustine phosphate sodium (4-12 mg/kg; intraperitoneal injection; daily; for 2 weeks) inhibits PAC120 tumor growth 53% by day 35.

Animal Model: Swiss nu/nu (nude) male mice (5-week-old) bearing PAC120 tumors
Dosage: 4 mg/kg, 12 mg/kg
Administration: Intraperitoneal injection; daily; for 2 weeks
Result: Suppressed the development of skin lesions and resulted in a dissociation between DTH response and antibody production.
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