N1,N11-Diethylnorspermine

N1,N11-Diethylnorspermine is a synthetic analog of the naturally occurring polyamine spermine, can induce polyamine depletion and inhibit tumor cell growth. N1,N11-Diethylnorspermine activates polyamine catabolism and downregulates mTOR protein. N1,N11-Diethylnorspermine 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]}. In Vivo:N1,N11-Diethylnorspermine (40 mg/kg, three times per day for two cycles of 6 days) 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) 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) is well tolerated and induces no physical signs in CD rats^[6].