NM-001 is a theranostic prodrug that targets ανβ3 integrin. It consists of cRGD peptides, GFLG peptides, a dichloromethane fluorophore, and Chlorambucil. The compound enters tumor cell lysosomes through cRGD peptides, where overexpressed cathepsin B (CTSB) facilitates intracellular cleavage of GFLG peptides, generating NM-002 and Chlorambucil. Under physiological conditions, NM-001 exhibits green fluorescence, which switches to near-infrared fluorescence upon CTSB activation. In a HeLa cell xenograft mouse model, NM-001 demonstrates significant antitumor activity with reduced toxicity and is suitable for real-time drug release monitoring studies.