Enzyme‐Activatable Probe for Tumor Bimodal Imaging, Intraoperative Navigation, and Urinalysis

We develope an enzyme‐activatable platform ( NO 2 ‐RGD‐Gd ) for the integrated urinary biomarker detection, highcontrast fluorescence‐magnetic resonance (MR) dualmodal imaging, and real‐time image‐guided surgical navigation within a single molecule. The advantages, including the favorable tumor‐targeting affinity (RGD peptide), high renal clearance efficiency, and tumor‐specific fluorescence activation, are achieved by rationally engineering the molecular architecture. Benefiting from these characteristics, the NO 2 ‐RGD‐Gd effectively bridges the boundary between diagnosis and therapy, achieving outstanding combinatorial performance in in vivo applications. It allows early and precise diagnosis through urinary biomarkers, provides anatomical‐pathological and molecular imaging information of tumor lesions via fluorescence‐MR dual‐modal imaging, and delineates tumor boundaries for accurate surgical navigation relying on tumor‐targeted activatable fluorescence imaging signals. Furthermore, all these processes can be realized simply via intravenous injection, offering a more efficient and feasible strategy for integrated diagnostic and therapeutic applications.