87862-25-7

Colourless to off-white solid

m-Iodobenzylguanidine (MIBG) is an analogue of norepinephrine with anticancer activity. It inhibits cell growth in a panel of human and mouse leukemia, fibrosarcoma, melanoma, and neuroblastoma cell lines when used at a concentration of 20 μg/ml and reduces clonogenic survival of L1210 leukemia cells in a concentration-dependent manner. MIBG increases survival in N₁E155 and L1210 mouse xenograft models when administered at doses of 40 and 20 mg/kg, respectively. It selectively accumulates in chromaffin tissues and tumors and formulations containing radiolabeled forms of MIBG have been used as imaging agents in the diagnosis and treatment of neuroendocrine tumors. MIBG also inhibits ADP-ribose linkage to membrane proteins in turkey erythrocyte membranes.

m-Iodobenzylguanidine Hemisulfate?can be used to demethylate and oxidize membrane-associated DNA. It has also been employed to develop a cell-based high-throughput screening assay to identify anti-hepatitis C virus compounds.

Antitumor agent which inhibits ADP ribosylation.

[1] L A SMETS  J W  B Bout. Cytotoxic and antitumor effects of the norepinephrine analogue meta-iodo-benzylguanidine (MIBG).[J]. Cancer Chemotherapy and Pharmacology, 1988, 21 1: 9-13. DOI: 10.1007/bf00262730
[2] CORNELIA LOESBERG  Lou A S  Henny van Rooij. Meta-iodobenzylguanidine (MIBG), a novel high-affinity substrate for cholera toxin that interferes with cellular mono(ADP-ribosylation)[J]. Biochimica et Biophysica Acta (BBA) - Protein Structure and Molecular Enzymology, 1990, 1037 1: Pages 92-99. DOI: 10.1016/0167-4838(90)90106-p