N1,N11-Diethylnorspermine tetrahydrochloride  (Synonyms: Diethylnorspermine tetrahydrochloride; DENSPM tetrahydrochloride; BENSPM tetrahydrochloride)

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^{[1][2][3][4][5][6]}.

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

390.26

C₁₃H₃₆Cl₄N₄

156886-85-0

Solid

White to off-white

CCNCCCNCCCNCCCNCC.[H]Cl.[H]Cl.[H]Cl.[H]Cl

Room temperature in continental US; may vary elsewhere.

4°C, sealed storage, away from moisture

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

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

• [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]