Preparation, in vitro and in vivo evaluation, and molecular dynamics (MD) simulation studies of novel F-18 labeled tumor imaging agents targeting focal adhesion kinase (FAK).

ABSTRACT: Focal adhesion kinase (FAK) has been identified as a promising target in the early diagnosis and therapy of tumor. In this work, we obtained and evaluated another two novel pyrimidine-based F-18 labeled tumor imaging agents targeting FAK. Among them, the corresponding F-19 standards [¹⁹F]2, displayed inhibition of FAK with IC₅₀ values of 57.1 nM (better than the results in our published work) and showed an good selectivity profile against some other kinds of cancer-related kinases. [¹⁸F]2 also had relatively good results in the in vivo biodistribution in S180-tumor-bearing mice, with tumor uptake of 5.40 ± 0.12 and 5.96 ± 0.09 % ID per g at 15 and 30 min post-injection, respectively. What's more, [¹⁸F]2 could be accumulated in tumor at 30

SUBMITTER: Fang Y 

PROVIDER: S-EPMC9078890 | biostudies-literature | 2018 Mar

REPOSITORIES: biostudies-literature