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N1,N11-Diethylnorspermine tetrahydrochloride

MCE China：N1,N11-Diethylnorspermine tetrahydrochloride

Brand：MedChemExpress (MCE)

Cat. No.HY-13610A

CAS：156886-85-0

Synonyms：DENSPM tetrahydrochloride; BENSPM tetrahydrochloride

Purity：98.0%

Storage：4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Shipping：Room temperature in continental US; may vary elsewhere.

Description：N1, N11-Diethylnorspermine tetrahydrochloride (DENSPM tetrahydrochloride) is a potent anticancer agent. N1,N11-Diethylnorspermine tetrahydrochloride activates polyamine catabolism and downregulates mTOR protein. N1,N11-Diethylnorspermine tetrahydrochloride induces the release of cytochrome c from mitochondria, resulting in activation of caspase 3. N1,N11-Diethylnorspermine tetrahydrochloride kills glioblastoma multiforme (GBM) through induction of SSAT (spermidine/spermine N1-acetyltransferase) coupled with H2O2 production.

In Vivo：N1,N11-Diethylnorspermine (40 mg/kg, three times per day for two cycles of 6 days) tetrahydrochloride clearly prevents tumor growth in mice bearing xenografts of the DU-145 cell line[1]. N1,N11-Diethylnorspermine (120-360 mg/kg, s.c., 4 days) tetrahydrochloride results in prolonged inhibition of tumor growth and long-term tumor regressions in nude athymic mice with MALME-3M melanoma xenografts[5]. N1,N11-Diethylnorspermine (12.5-50 mg/kg, i.v., 5 days) tetrahydrochloride is well tolerated and induces no physical signs in CD rats[6].

IC50 & Target：Caspase 3

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References：

[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.  [Content Brief]

[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.  [Content Brief]

[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.  [Content Brief]

[4]. Jiang R, et al. Activation of polyamine catabolism by N1, N11-diethylnorspermine alters the cellular localization of mTOR and downregulates mTOR protein level in glioblastoma cells. Cancer Biol Ther. 2007 Oct;6(10):1644-8.  [Content Brief]

[5]. Bernacki RJ, et al. Preclinical antitumor efficacy of the polyamine analogue N1, N11-diethylnorspermine administered by multiple injection or continuous infusion. Clin Cancer Res. 1995 Aug;1(8):847-57.  [Content Brief]

[6]. Kanter PM, et al. Preclinical toxicologic evaluation of DENSPM (N1,N11-diethylnorspermine) in rats and dogs. Anticancer Drugs. 1994 Aug;5(4):448-56.  [Content Brief]