Synthesis and bioevaluation of a novel 99mTc-labeled complex with a crizotinib HYNIC derivative for imaging of c-Met–positive expression

Abstract

c-Met, a transmembrane receptor tyrosine kinase, is implicated in the process of tumor progression and metastasis and is regarded as a therapeutic target with its small molecular inhibitor, such as crizotinib. However, there are few radiolabeled small molecular inhibitors used for the evaluation of c-Met expression. Herein, a ^99mTc labeled crizotinib derivative ([^99mTc]Tc-HYNIC-Cri) was prepared with high stability in vitro, and there was a significant difference in biodistribution and SPECT studies between U87 MG tumors with high c-Met expression and A549 tumors with low c-Met expression. These initial findings reveal that [^99mTc]Tc-HYNIC-Cri holds great potential for imaging of c-Met–positive tumors.