52205-73-9

• 常用中文名：雌莫司汀磷酸钠
• 常用英文名：Estramustine phosphate sodium
• CAS号：52205-73-9
• 分子式：C₂₃H₃₀Cl₂NNa₂O₆P
• 分子量：564.347
• 相关类别： 原料药 抗肿瘤药 烷化剂类抗肿瘤药
• 发布时间：2018-09-02 19:27:26
• 更新时间：2024-01-08 14:37:03
• Estramustine磷酸钠盐是抗微管蛋白化疗试剂。

名称

• 中文名: 雌莫司汀磷酸钠
• 英文名: estramustine sodium phosphate
• 中文别名: 雌莫司丁磷酸钠
• 英文别名: EINECS 257-735-7; Estramustine phosphate disodium; Ro 21-8837/001; Estramustine sodium phosphate; iumphosphate; estracytsodium; Estracyt; carbamic acid, bis(2-chloroethyl)-, (17β)-17-(phosphonooxy)estra-1,3,5(10)-trien-3-yl ester, disodium salt; disodium (8R,9S,13S,14S,17S)-3-{[bis(2-chloroethyl)carbamoyl]oxy}-13-methyl-7,8,9,11,12,13,14,15,16,17-decahydro-6H-cyclopenta[a]phenanthren-17-yl phosphate; Disodium (17β)-3-{[bis(2-chloroethyl)carbamoyl]oxy}estra-1(10),2,4-trien-17-yl phosphate; Carbamic acid, N,N-bis(2-chloroethyl)-, (17β)-17-(phosphonooxy)estra-1(10),2,4-trien-3-yl ester, sodium salt (1:2); MFCD00866320; estramustinephosphatedisodium; estramustine phosphate; emcyt; Dinatrium-(8R,9S,13S,14S,17S)-3-{[bis(2-chlorethyl)carbamoyl]oxy}-13-methyl-7,8,9,11,12,13,14,15,16,17-decahydro-6H-cyclopenta[a]phenanthren-17-ylphosphat; Estramustine phosphate sodium; phosphate de (8R,9S,13S,14S,17S)-3-{[bis(2-chloroéthyl)carbamoyl]oxy}-13-méthyl-7,8,9,11,12,13,14,15,16,17-décahydro-6H-cyclopenta[a]phénanthrén-17-yle de disodium; Estramustine (phosphate sodium)

物化性质

• 密度: 1.253g/cm3
• 沸点: 565.8ºC at 760mmHg
• 分子式: C₂₃H₃₀Cl₂NNa₂O₆P
• 分子量: 564.347
• 闪点: 296ºC
• 精确质量: 563.098328
• PSA: 111.77000
• LogP: 6.17540
• 储存条件: room temp

生物活性

• 描述: Estramustine磷酸钠盐是抗微管蛋白化疗试剂。
• 相关类别:
  信号通路 >> 细胞周期/DNA损伤 >> 微管/微管蛋白
  信号通路 >> 细胞骨架 >> 微管/微管蛋白
  研究领域 >> 癌症
• 参考文献:

  [1]. Perry CM, et al. Estramustine phosphate sodium. A review of its pharmacodynamic and pharmacokinetic properties, and therapeutic efficacy in prostate cancer. Drugs Aging. 1995 Jul;7(1):49-74.

  [2]. Bergenheim AT, et al. Pharmacokinetics and pharmacodynamics of estramustine phosphate. Clin Pharmacokinet. 1998 Feb;34(2):163-72.

  [3]. Dene Simpson, et al. Estramustine Phosphate Sodium. American Journal of Cancer 2 (5):373–390.

毒性和生态

CHEMICAL IDENTIFICATION RTECS NUMBER : KG7350000 CHEMICAL NAME : Estra-1,3,5(10)-triene-3,17-diol (17-beta)-, 3-(bis(2-chloroethyl)carbamate) 17-(dihydrogen phosphate), disodium salt CAS REGISTRY NUMBER : 52205-73-9 LAST UPDATED : 199707 DATA ITEMS CITED : 20 MOLECULAR FORMULA : C23-H32-Cl2-N-O6-P.2Na MOLECULAR WEIGHT : 566.41 WISWESSER LINE NOTATION : L E5 B666TTT&J E1 FOPWO OOVN2G2G &-NA- 2 HEALTH HAZARD DATA ACUTE TOXICITY DATA TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 5400 mg/kg TOXIC EFFECTS : Gastrointestinal - hypermotility, diarrhea Kidney, Ureter, Bladder - hematuria REFERENCE : OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 20,1141,1980 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Subcutaneous SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 9 gm/kg TOXIC EFFECTS : Skin and Appendages - dermatitis, other (after systemic exposure) Skin and Appendages - hair REFERENCE : OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 20,1141,1980 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intravenous SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 208 mg/kg TOXIC EFFECTS : Lungs, Thorax, or Respiration - respiratory depression REFERENCE : OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 20,1141,1980 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : >12 gm/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 20,1141,1980 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Subcutaneous SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 5200 mg/kg TOXIC EFFECTS : Skin and Appendages - dermatitis, other (after systemic exposure) Skin and Appendages - hair REFERENCE : OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 20,1141,1980 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intravenous SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 380 mg/kg TOXIC EFFECTS : Lungs, Thorax, or Respiration - respiratory depression REFERENCE : OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 20,1141,1980 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Mammal - dog DOSE/DURATION : >3 gm/kg TOXIC EFFECTS : Gastrointestinal - changes in structure or function of salivary glands Gastrointestinal - hypermotility, diarrhea Kidney, Ureter, Bladder - hematuria REFERENCE : OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 20,1141,1980 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Rodent - rabbit DOSE/DURATION : 5655 mg/kg TOXIC EFFECTS : Gastrointestinal - hypermotility, diarrhea Kidney, Ureter, Bladder - hematuria REFERENCE : OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 20,1141,1980 ** OTHER MULTIPLE DOSE TOXICITY DATA ** TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 3500 mg/kg/5W-C TOXIC EFFECTS : Liver - changes in liver weight Endocrine - other changes Blood - changes in serum composition (e.g. TP, bilirubin, cholesterol) REFERENCE : OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 21,211,1981 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 3640 mg/kg/26W-C TOXIC EFFECTS : Kidney, Ureter, Bladder - other changes in urine composition Endocrine - other changes Blood - changes in serum composition (e.g. TP, bilirubin, cholesterol) REFERENCE : OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 21,549,1981 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Mammal - dog DOSE/DURATION : 320 mg/kg/32D-I TOXIC EFFECTS : Blood - hemorrhage Blood - normocytic anemia Related to Chronic Data - changes in uterine weight REFERENCE : OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 20,1161,1980 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Primate - monkey DOSE/DURATION : 1274 mg/kg/13W-I TOXIC EFFECTS : Endocrine - other changes Blood - changes in serum composition (e.g. TP, bilirubin, cholesterol) Related to Chronic Data - changes in uterine weight REFERENCE : OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 20,757,1980 ** REPRODUCTIVE DATA ** TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral DOSE : 30 mg/kg SEX/DURATION : male 60 day(s) pre-mating TOXIC EFFECTS : Reproductive - Paternal Effects - testes, epididymis, sperm duct REFERENCE : OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 20,1211,1980 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral DOSE : 5500 ug/kg SEX/DURATION : female 7-17 day(s) after conception TOXIC EFFECTS : Reproductive - Effects on Newborn - behavioral Reproductive - Effects on Newborn - physical REFERENCE : OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 20,1219,1980 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral DOSE : 22 mg/kg SEX/DURATION : female 7-17 day(s) after conception TOXIC EFFECTS : Reproductive - Fertility - post-implantation mortality (e.g. dead and/or resorbed implants per total number of implants) Reproductive - Effects on Newborn - growth statistics (e.g.%, reduced weight gain) REFERENCE : OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 20,1219,1980 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral DOSE : 44 mg/kg SEX/DURATION : female 7-17 day(s) after conception TOXIC EFFECTS : Reproductive - Fertility - litter size (e.g. # fetuses per litter; measured before birth) Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus) Reproductive - Effects on Newborn - live birth index (measured after birth) REFERENCE : OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 20,1219,1980 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral DOSE : 650 ug/kg SEX/DURATION : female 6-18 day(s) after conception TOXIC EFFECTS : Reproductive - Fertility - litter size (e.g. # fetuses per litter; measured before birth) REFERENCE : OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 21,41,1981 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral DOSE : 2600 ug/kg SEX/DURATION : female 6-15 day(s) after conception TOXIC EFFECTS : Reproductive - Fertility - post-implantation mortality (e.g. dead and/or resorbed implants per total number of implants) REFERENCE : OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 21,41,1981 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral DOSE : 1300 ug/kg SEX/DURATION : female 6-15 day(s) after conception TOXIC EFFECTS : Reproductive - Fertility - other measures of fertility REFERENCE : OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 21,41,1981 *** NIOSH STANDARDS DEVELOPMENT AND SURVEILLANCE DATA *** NIOSH OCCUPATIONAL EXPOSURE SURVEY DATA : NOES - National Occupational Exposure Survey (1983) NOES Hazard Code - X5435 No. of Facilities: 9 (estimated) No. of Industries: 1 No. of Occupations: 1 No. of Employees: 63 (estimated) No. of Female Employees: 9 (estimated)

安全

• 个人防护装备: dust mask type N95 (US);Eyeshields;Gloves
• 危害码 (欧洲): Xi
• 风险声明 (欧洲): 37
• 安全声明 (欧洲): 26
• 危险品运输编码: NONH for all modes of transport
• RTECS号: KG7350000