3-IODOBENZYL-GUANIDINE HEMISULFATE
3-IODOBENZYL-GUANIDINE HEMISULFATE Basic information
- Product Name:
- 3-IODOBENZYL-GUANIDINE HEMISULFATE
- Synonyms:
-
- M-IBG
- MIBG HEMISULFATE SALT
- M-IODOBENZYLGUANIDINE HEMISULFATE SALT
- M-IODOBENZYLGUANIDINE 1/2H2SO4
- Guanidine, [(3-iodophenyl)methyl]-, sulfate (2:1)
- meta-Iodobenzylguanidine hemisulfate
- MIBG hemisulfate
- m-iodobenzylguanidine sulfate
- CAS:
- 87862-25-7
- MF:
- C16H22I2N6O4S
- MW:
- 648.26
- Mol File:
- 87862-25-7.mol
3-IODOBENZYL-GUANIDINE HEMISULFATE Chemical Properties
- storage temp.
- 2-8°C
- solubility
- DMSO: 2 mg/ml; DMSO:PBS (pH 7.2) (1:4): 0.2 mg/ml
- form
- A crystalline solid
- color
- White to off-white
MSDS
- Language:English Provider:SigmaAldrich
3-IODOBENZYL-GUANIDINE HEMISULFATE Usage And Synthesis
Description
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.
Chemical Properties
Colourless to off-white solid
Uses
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.
Biochem/physiol Actions
Antitumor agent which inhibits ADP ribosylation.
in vivo
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. |
References
[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
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