Palbociclib-derived multifunctional molecules for lysosomal targeting and diagnostic-therapeutic integration.

Lysosomal pH changes are associated with drug resistance, cell growth and invasion of tumors, but effective and specific real-time monitoring of lysosomal pH compounds for cancer therapy is lacking. Here, based on the covalent linkage of the anticancer drug palbociclib and fluorescent dye fluorescein isothiocyanate (FITC), we designed and developed a novel palbociclib-derived multifunctional molecule (Pal-FITC) for lysosomal targeting and diagnostic therapeutic integration. Pal-FITC fluoresces is 20-fold stronger than that of FITC and shows a linear response in the pH range of 4.0-8.2 (R = 0.9901). Pal-FITC blocks cells in G1 phase via . Our study provides new strategies for tumor-targeted imaging and personalized therapy.