雌莫司汀磷酸钠

中文名称:

雌莫司汀磷酸钠

中文同义词:

雌莫司汀磷酸钠;雌莫司汀磷酸钠, 抗微管蛋白化疗试剂;雌莫司丁磷酸钠

英文名称:

Estramustine sodium phosphate

英文同义词:

ESTRAMUSTINE PHOSPHATE SODIUM;-(dihydrogenphosphate),disodiumsalt;iumphosphate;Estra-1,3,5(10)-triene-3,17-diol (17beta)-, 3-[bis(2-chloroethyl)carbamate] 17-(dihydrogen phosphate), disodium salt;Estra-1,3,5(10)-triene-3,17-diol (17β)-, 3-[bis(2-chloroethyl)carbamate] 17-(dihydrogen phosphate), disodium salt;Estracyt;Estramustine phosphate disodium salt;NSC 89199

CAS号:

52205-73-9

分子式:

C23H33Cl2NNaO6P

分子量:

544.38

EINECS号:

257-735-7

相关类别:

医药原料药;医药、农药及染料中间体;Active Pharmaceutical Ingredients;Intermediates;Other APIs

Mol文件:

52205-73-9.mol

储存条件 

Inert atmosphere,2-8°C

溶解度 

H2O: soluble50mg/mL

CAS 数据库

52205-73-9(CAS DataBase Reference)

生物活性

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。

体外研究

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.

体内研究

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.

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.

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