Iobenguane sulfate

Iobenguane sulfate (MIBG sulfate) is an analogue of the neurotransmitter norepinephrine with antitumor activity. Radioiodinated Iobenguane sulfate is clinically used as a tumor-targeted radiopharmaceutical in the diagnosis and treatment of adrenergic tumors. Iobenguane sulfate is a high-affinity substrate for cholera toxin that interferes with cellular mono(ADP-ribosylation)[1][2].

Research Areas >> Cancer

Signaling Pathways >> Others >> Others

Iobenguane sulfate (MIBG sulfate) (2-20 μg/ml; 72 hours) inhibits cell growth in a panel of human and mouse leukemia, fibrosarcoma, melanoma, and neuroblastoma cell lines[1]. Iobenguane sulfate (MIBG sulfate) is a potent affector of endogenous mono(ADP-ribosyl) transferases of turkey and human erythrocyte membranes, exerting its effect in the μM concentration range[2]. Cell Proliferation Assay[1] Cell Line: 3T3, 3T3-Tl3, BHK, Py-BHK, K562, L1210, RIF1, M5A, B16, LAN-1, N1E115, CHP212 cells Concentration: 2, 20μg/ml Incubation Time: 72 hours Result: Inhibits 3T3, 3T3-Tl3, BHK, Py-BHK, K562, L1210, RIF1, M5A, B16, LAN-1, N1E115, and CHP212 cells growth.

Iobenguane sulfate (MIBG hemisulfate) (20 mg/kg; i.p.; daily on days 3-6) shows antitumor activity[1]. The survival of male strain AF mice inoculates with N1E115 neuroblastoma and treats according to NIH protocols for new drug testing with 9 daily injections of Iobenguane sulfate (40 mg/kg), Marking prolongation of sugvival but no cures were observed[1]. Iobenguane sulfate testes for its toxicity on male strain AF (N1Ell5) mice with 5 daily injections. At 50 mg/kg body weight, all animals died after 1-4 doses and 4/16 animals died on a schedule of 44 mg/kg[1]. Animal Model: DBA/2 (L1210)) mice[1] Dosage: i.p.; daily on days 3-6 Administration: 20 mg/kg Result: Considerable prolongation of survival and some cures were obtained.

[1]. Loesberg C, et al. Meta-iodobenzylguanidine (MIBG), a novel high-affinity substrate for cholera toxin that interferes with cellular mono(ADP-ribosylation). Biochim Biophys Acta. 1990 Jan 19;1037(1):92-9.