Preparation and Quality Control of ~111In-Plerixafor for Chemokine Receptor CXCR4

摘要

Developing CXCR4 receptor imaging agents is of great importance for oncological imaging. In this work, N, N'-[l, 4-Phenylenebis(methylene)]bis-l,4,8,ll-tetraazacyclotetradecane was labeled using high purity [~111In]InCl3 in 30-60 min at 60degC in acetate buffer with acceptable yield and radiochemical purity (>97% ITLC, >95% HPLC, specific activity: 120-200 GBq/mmol), Radiolabeled complex of AMD-3100 ([~111In]-AMD3100) showed good stability at room temperature and physiologic conditions in human serum for 24 h. Log P for the complex was determined (-1.18) to be consistent with a water soluble/ionic complex.The biodistribution of the radiolabeled complex of plerixafor in vital organs of rats was determined up to 48 h demonstrating kidneys as the major route of excretion. Considering lungs, spleen and liver as the CXCR4 rich target organs, the best targetnon target ratios (for spleenrblood, limg:blood and livenblood) were obtained 24 h post injection (5.11,2.08 and 10.63 respectively).