Many malignant tumors, including breast cancer, exhibit
amplification
and overexpression of cyclin-dependent kinase 4 and 6 (CDK4/6). Ribociclib,
approved and used in clinical treatment, acts as a highly selective
CDK4/6 inhibitor for ER+/HER2- breast cancer. By modifying ribociclib
with the chelator DOTA, we designed and synthesized a novel CDK4/6-positive
PET imaging agent, which was radiolabeled by 68Ga for radioactive
tagging. The radiotracer demonstrates high radiochemical purity, excellent
stability in vitro and in vivo,
and favorable pharmacokinetic characteristics. Cell uptake experiments
using MCF-7 cells indicate that an excess of ribociclib (RBB) can
inhibit cellular uptake of 68Ga-DOTA-RBB. Imaging and biodistribution
experiments in MCF-7 tumor-bearing nude mice show significant radioactive
accumulation in the tumor. However, preadministration of excess ribociclib
results in a substantial reduction in radioactive accumulation within
the tumor. On the basis of our explorations, 68Ga-DOTA-RBB,
as a targeted imaging agent for CDK4/6-positive tumors, holds significant
potential application values.