Journal
MOLECULAR PHARMACEUTICS
Volume 18, Issue 4, Pages 1634-1642Publisher
AMER CHEMICAL SOC
DOI: 10.1021/acs.molpharmaceut.0c01088
Keywords
focal adhesion kinase (FAK); FAK inhibitor; F-18-labeled; radiotracers
Funding
- National Major Scientific and Technological Special Project for Significant New Drugs Development [2014ZX09507007-001, 2014ZX09507007-003]
- National Natural Science Foundation of China [21771022, U1804188]
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A series of 2,4-diaminopyrimidine derivatives labeled with F-18 were found to have potential as PET tumor imaging agents, with Q6 showing good inhibition of FAK activity and biodistribution in S180-bearing mice.
There are two important topics in the field of cancer research: one is targeted molecular therapy and the other is tumor molecular imaging. Focal adhesion kinase (FAK) is considered as an attractive target for oncologic diagnosis and therapy. A series of 2,4-diaminopyrimidine derivatives were labeled with F-18 to study their biological properties and their potential as positron emission tomography tumor imaging agents. They inhibited the activity of FAK with IC50 values in the wide range of 0.6-2164 nM, among which the IC50 of Q6 was 3.2 nM. For the biodistribution in S180-bearing mice, the corresponding [F-18]Q6 was relatively good, with the highest uptake of 3.35 +/- 0.32 % ID/g at 30 min postinjection, with a tumor/muscle ratio of 2.08 and a tumor/bone ratio of 2.48. Accordingly, [F-18]Q6 was considered as a potential PET imaging agent for tumor diagnosis.
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