Preparation and evaluation of fluorine-18-labeled insulin as a molecular imaging probe for studying insulin receptor expression in tumors.

Abstract

A convenient emulsion-based labeling method was used to synthesize fluorine-18-labeled insulin specifically B(1)-(4-[(18)F]fluorobenzoyl)insulin ((18)F-4b) in 6% overall radiochemical yield in 240 min. In vitro screening in MCF7 breast cancer cells demonstrated that the nonradioactive analogue (19)F-4a effectively competed with (125)I-insulin for the insulin receptor (IC50 = 10.6 nM) comparable to that for insulin (IC50 = 7.4 nM). (18)F-4b was also more stable than (125)I-insulin in mouse plasma with 50% remaining intact after 30 min. A biodistribution study in normal mice showed initial uptake of the tracer in the kidneys, liver, and gall bladder but rapid clearance via the urine/bladder which was also observed in murine models bearing insulin receptor positive tumors.

• Authors: Dong Hyun Kim, Megan Blacker, John F Valliant
• Journal: Journal of medicinal chemistry (J Med Chem) Vol. 57 Issue 9 Pg. 3678-86 (May 08 2014) ISSN: 1520-4804 [Electronic] United States
• PMID: 24712894 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)

Chemical References

• Fluorine Radioisotopes
• Insulin
• Molecular Probes
• Receptor, Insulin

Topics

• Animals
• Breast Neoplasms (metabolism)
• Chromatography, High Pressure Liquid
• Fluorine Radioisotopes (administration & dosage, chemistry)
• Humans
• Insulin (administration & dosage, chemistry)
• MCF-7 Cells
• Mass Spectrometry
• Mice
• Mice, Inbred BALB C
• Molecular Probes
• Receptor, Insulin (metabolism)
• Tissue Distribution