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52205-73-9

中文名称 雌莫司汀磷酸钠
英文名称 Estramustine sodium phosphate
CAS 52205-73-9
EINECS 编号 257-735-7
分子式 C23H30Cl2NNa2O6P
MDL 编号 MFCD00866320
分子量 564.35
MOL 文件 52205-73-9.mol
更新日期 2023/03/20 15:41:23
52205-73-9 结构式 52205-73-9 结构式

基本信息

中文别名
雌莫司汀磷酸钠
英文别名
(17-beta)-estra-1,3,5(10)-triene-3,17-diol 3-(bis(2-chloroethyl)carbamate) 17-(dihydrogenphosphate) disodium salt
ESTRAMUSTINE PHOSPHATE SODIUM
-(dihydrogenphosphate),disodiumsalt
3,5(10)-triene-3,17-diol(17-beta)-estra-3-(bis(2-chloroethyl)carbamate)17
emcyt
estra-1,3,5(10)-triene-3,17-beta-diol3-(bis(2-chloroethyl)carbamate)17-disod
estracytsodium
estramustinephosphatedisodium
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
Ro 21-8837/001
Estra-1,3,5(10)-trien-3,17-diol-(17beta)-, 3-(Bis(2-chlorethyl)carbamat) 17-(Dihydrogen-phosphat), Dinatriumsalz
(17-beta)-Estra-1,3,5(10)-triene-3,17-diol 3-(bis(2-chloroethyl)carbamate) 17-(dihydrogenphosphate) disodium salt
1,3,5(10)-Estratriene-3,17β-diol 3-[bis(2-chloroethyl)carbamate]17-[phosphoric acid disodium] salt
所属类别
原料药:烷化剂类抗肿瘤药

物理化学性质

储存条件Inert atmosphere,2-8°C
溶解度H2O中可溶50mg/mL
形态结晶固体
稳定性吸湿性,溶液不稳定

安全数据

危险性符号(GHS)
GHS08
警示词危险
危险性描述H361-H351
危险品标志Xi
危险类别码37
安全说明26
WGK Germany3
RTECS号KG7350000
海关编码29242990

知名试剂公司产品信息

常见问题列表

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.
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