• • dIR-CDF achieves covalent tumor targeting via sulfenic acid-specific reaction, enhancing tumor accumulation and retention; in vivo studies demonstrate efficient NSCLC tumor suppression in living mice, underscoring its clinical potential for precise theranostics.
• • The probe enables NIR imaging-guided therapy under 808 nm irradiation, combining photodynamic effect (1O2 generation) with ferrocene-mediated ferroptosis (·OH production via Fenton reaction), synergistically amplifying oxidative damage and lipid peroxidation.
• • The system specifically targets integrin αvβ3-positive NSCLC cells, leveraging the overexpression of sulfenated proteins in the tumor microenvironment, which significantly improves specificity over conventional untargeted agents.
• • The covalent immobilization strategy, based on 1,3-cyclohexanedione-sulfenic acid reaction, ensures prolonged retention at the tumor site, addressing the bottleneck of rapid clearance and low drug accumulation seen in traditional nanomedicines.