biostudies-literatureFang YNational Natural Science Foundation of China10333-10345https://www.ebi.ac.uk/biostudies/studies/S-EPMC9078890biostudies-literatureUnknown8(19)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 <i>in vivo</i> 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 RSC advancesPreparation, <i>in vitro</i> and <i>in vivo</i> evaluation, and molecular dynamics (MD) simulation studies of novel F-18 labeled tumor imaging agents targeting focal adhesion kinase (FAK).PMC907889021371026Fang YLi XLiu JZhang JWang DXue QZhang HDava GWang HXu XfalsePreparation, <i>in vitro</i> and <i>in vivo</i> evaluation, and molecular dynamics (MD) simulation studies of novel F-18 labeled tumor imaging agents targeting focal adhesion kinase (FAK).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 <i>in vivo</i> 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 2018-01-01T00:00:00Z2018 Mar2026-05-30T18:48:48.753Z2024-12-04T03:40:39.669ZS-EPMC90788903554045110.1039/c8ra00652k