Biological Activity
CGP 48664 (SAM486A; Sardomozide) is a polyamine (PA) biosynthesis inhibitor (73% and 97% downregulation of murine leukemia L1210 cellular spermidine and spermine, respectively, by 0.5 μM Sardomozide in 4 days) th at targets the rate-limiting enzyme S-adenosylmethionine decarboxylase (AdoMetDC, SAMDC, AMD1) in a potent (IC50 = 5 nM against r at AMD1) and selective manner with little or no inhibitory efficacy toward diamine oxidase or ornithine decarboxylase (IC50 = 18 μM and >50 μM against r at DAO and ODC, respectively). CGP 48664 effectively inhibits the proliferation of murine (GI50 = 0.5 μM against L1210 in 4 days) and human cancer cell lines in cultures (GI50 from 0.26 to 0.6 μM in 5 days; GI50 = 0.8 μM against human melanoma SK MEL-24 in 10 days) and suppresses the growth of murine and human tumor xenografts in mice in vivo (ED50 ≤0.5 mg/kg i.p.). CGP 48664 (Sardomozide) potently inhibits growth of PFA ependymoma cells.
