N1,N11-二乙基去甲精胺四盐酸盐

N1,N11-二乙基去甲精胺四盐酸盐用途

N1,N11二乙基去甲精胺(DENSPM)是一种有效的抗癌药物。N1,N11二乙基去甲精胺是一种精胺类似物,可激活多胺分解代谢。N1,N11二乙基去甲精胺诱导线粒体释放细胞色素c,导致半胱氨酸蛋白酶3激活。N1,N11二乙基去甲亚精胺通过诱导SSAT(亚精胺/精胺N1乙酰转移酶)结合H2O2生成杀死多形性胶质母细胞瘤(GBM)细胞[1][2][3]。

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N1,N11-二乙基去甲精胺四盐酸盐名称

[ CAS 号 ]:
121749-39-1

[ 中文名 ]:
N1,N11-二乙基去甲精胺四盐酸盐

[ 英文名 ]:
N(1),N(11)-Diethylnorspermine tetrahydrochloride

[英文别名 ]:

Bisethyl norspermine
denspm
de333
be3-3-3
3,7,11,15-Tetraazaheptadecane
N1,N11-Diethylnorspermine4HCl
N1,N11-Diethylnorspermine tetrahydrochloride

N1,N11-二乙基去甲精胺四盐酸盐生物活性

[ 描述 ]:

[ 相关类别 ]:

研究领域 >> 癌症

信号通路 >> 细胞凋亡 >> 胱天蛋白酶

[ 靶点 ]

Caspase 3

[体内研究]

N1,N11二乙基去甲亚精胺(40 mg/kg,每天三次,连续两个周期,共6天)可明显防止携带DU-145细胞系异种移植物的小鼠的肿瘤生长[1]。

[参考文献]

[1]. Schipper RG, et al. Antitumor activity of the polyamine analog N(1), N(11)-diethylnorspermine against human prostate carcinoma cells. Prostate. 2000 Sep 1;44(4):313-21.

[2]. Holst CM, et al. Molecular mechanisms underlying N1, N11-diethylnorspermine-induced apoptosis in a human breast cancer cell line. Anticancer Drugs. 2008 Oct;19(9):871-83.

[3]. Jiang R, et al. Activation of polyamine catabolism by N1,N11-diethylnorspermine leads to cell death in glioblastoma. Int J Oncol. 2007 Aug;31(2):431-40.

N1,N11-二乙基去甲精胺四盐酸盐物理化学性质

[ 密度 ]:
0.877 g/cm3

[ 沸点 ]:
357.1ºC at 760 mmHg

[ 分子式 ]:
C₁₃H₃₂N₄

[ 分子量 ]:
244.42

[ 闪点 ]:
171.9ºC

[ 精确质量 ]:
388.16900

[ PSA ]:
48.12000

[ LogP ]:
5.32650

[ 蒸汽压 ]:
2.79E-05mmHg at 25°C

[ 折射率 ]:
1.462

N1,N11-二乙基去甲精胺四盐酸盐毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: TX7032250

CHEMICAL NAME :: 1,3-Propanediamine, N,N'-bis(3-(ethylamino)propyl)-

CAS REGISTRY NUMBER :: 121749-39-1

LAST UPDATED :: 199510

DATA ITEMS CITED :: 2

MOLECULAR FORMULA :: C13-H32-N4

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 100 mg/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity) Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - dyspnea

REFERENCE :: ANTDEV Anti-Cancer Drugs. (Rapid Communications of Oxford Ltd., The Old Malthous, Paradise St., Oxford OX1 1LD, UK) V.1- 1990- Volume(issue)/page/year: 5,448,1994

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 325 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: JMCMAR Journal of Medicinal Chemistry. (American Chemical Soc., Distribution Office Dept. 223, POB POB 57136, West End Stn., Washington, DC 20037) V.6- 1963- Volume(issue)/page/year: 37,3464,1994