59917-39-4

• 常用中文名：硫酸长春地辛
• 常用英文名：Vindesine sulfate
• CAS号：59917-39-4
• 分子式：C₄₃H₅₇N₅O₁₁S
• 分子量：852.00
• 相关类别： 原料药 抗肿瘤药 天然来源类抗肿瘤药
• 发布时间：2018-03-18 08:00:00
• 更新时间：2024-01-02 23:38:22
• 硫酸长春地辛是一种有效的微管蛋白抑制剂,Ki为0.110µM。硫酸长春地辛在体外具有抗增殖作用。硫酸长春地辛在体内具有抗肿瘤作用[1]。

名称

• 中文名: 硫酸长春地辛
• 英文名: vindesine sulfate
• 英文别名: 2H-3,7-Methanoazacycloundecino[5,4-b]indole-9-carboxylic acid, 9-[(2β,3β,4β,5α,12β,19α)-3-(aminocarbonyl)-6,7-didehydro-3,4-dihydroxy-16-methoxy-1-methylaspidospermidin-15-yl]-5-et hyl-1,4,5,6,7,8,9,10-octahydro-5-hydroxy-, methyl ester, (5S,7S,9S)-, sulfate (1:1) (salt); methyl (5S,7S,9S)-9-[(2β,3β,4β,5α,12β,19α)-3-carbamoyl-3,4-dihydroxy-16-methoxy-1-methyl-6,7-didehydroaspidospermidin-15-yl]-5-ethyl-5-hydroxy-1,4,5,6,7,8,9,10-octahydro-2H-3,7-methanoazacycloundecino[5,4-b]indole-9-carboxylate sulfate (1:1); Vindesine Sulfate Salt; 2H-3,7-methanoazacycloundecino[5,4-b]indole-9-carboxylic acid, 9-[(2β,3β,4β,5α,12β,19α)-3-(aminocarbonyl)-6,7-didehydro-3,4-dihydroxy-16-methoxy-1-methylaspidospermidin-15-yl]-5-ethyl-1,4,5,6,7,8,9,10-octahydro-5-hydroxy-, methyl ester, (5S,7S,9S)-, sulfate (1:1) (salt); Vindesine sulphate; Methyl (13S,15S,17S)-13-[(2β,3β,4β,5α,12β,19α)-3-carbamoyl-3,4-dihydroxy-16-methoxy-1-methyl-6,7-didehydroaspidospermidin-15-yl]-17-ethyl-17-hydroxy-1,11-diazatetracyclo[13.3.1.0.0]nonadeca-4(12),5,7,9-tetraene-13-carboxylate sulfate (1:1)

物化性质

• 密度: 1.41 g/cm3
• 熔点: >250ºC
• 分子式: C₄₃H₅₇N₅O₁₁S
• 分子量: 852.00
• 精确质量: 851.377502
• PSA: 247.80000
• LogP: 3.80150
• 外观性状: 非晶形的固体
• 储存条件: 2-8°C
• 水溶解性: deionized water: ≥50mg/mL

生物活性

• 描述: 硫酸长春地辛是一种有效的微管蛋白抑制剂,Ki为0.110µM。硫酸长春地辛在体外具有抗增殖作用。硫酸长春地辛在体内具有抗肿瘤作用[1]。
• 相关类别:
  研究领域 >> 癌症
  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
• 体外研究: 硫酸长春地辛抑制L细胞生长,在40 nM处显示约25%的抑制作用【1】。
• 参考文献:

  [1]. Jordan MA, et al. Comparison of the effects of vinblastine, vincristine, vindesine, and vinepidine on microtubule dynamics and cell proliferation in vitro. Cancer Res. 1985 Jun;45(6):2741-7.

毒性和生态

CHEMICAL IDENTIFICATION RTECS NUMBER : YY8090000 CAS REGISTRY NUMBER : 59917-39-4 LAST UPDATED : 199706 DATA ITEMS CITED : 11 MOLECULAR FORMULA : C43-H55-N5-O7.H2-O4-S MOLECULAR WEIGHT : 852.11 HEALTH HAZARD DATA ACUTE TOXICITY DATA TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intraperitoneal SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 1050 ug/kg TOXIC EFFECTS : Behavioral - ataxia Gastrointestinal - hypermotility, diarrhea Kidney, Ureter, Bladder - urine volume increased TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Subcutaneous SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 1790 ug/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intravenous SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 1920 ug/kg TOXIC EFFECTS : Gastrointestinal - hypermotility, diarrhea Kidney, Ureter, Bladder - urine volume increased Blood - normocytic anemia TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intraperitoneal SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 3500 ug/kg TOXIC EFFECTS : Behavioral - ataxia Gastrointestinal - hypermotility, diarrhea Kidney, Ureter, Bladder - urine volume increased TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Subcutaneous SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 6800 ug/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intravenous SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 6300 ug/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Intravenous SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 1250 ug/kg/33D-I TOXIC EFFECTS : Endocrine - other changes Blood - changes in bone marrow (not otherwise specified) Biochemical - Enzyme inhibition, induction, or change in blood or tissue levels - transaminases TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Intravenous DOSE : 1250 ug/kg SEX/DURATION : male 10 day(s) pre-mating TOXIC EFFECTS : Reproductive - Paternal Effects - testes, epididymis, sperm duct Reproductive - Paternal Effects - prostate, seminal vesicle, Cowper's gland, accessory glands TYPE OF TEST : Micronucleus test MUTATION DATA TYPE OF TEST : Mutation test systems - not otherwise specified TEST SYSTEM : Rodent - hamster Ovary DOSE/DURATION : 28 nmol/L REFERENCE : CNREA8 Cancer Research. (Public Ledger Building, Suit 816, 6th & Chestnut Sts., Philadelphia, PA 19106) V.1- 1941- Volume(issue)/page/year: 38,2886,1978

安全

• 危害码 (欧洲): Xn: Harmful;
• 风险声明 (欧洲): R40
• 安全声明 (欧洲): 26-36
• 危险品运输编码: UN 1544
• RTECS号: YY8090000
• 包装等级: II
• 危险类别: 6.1(a)
• 海关编码: 2942000000

海关

海关编码	2942000000