Abstract: The invention provides a 7-ethyl-10-hydroxycamptothecin drug precursor with fluorescence activity and a preparation method and use thereof. The method involves that a carboxyl group of a boron dipyrromethene dye molecule is condensed with a hydroxyl group at the 10 position of 7-ethyl-10-hydroxycamptothecin, yielding a 7-ethyl-10-hydroxy-camptothecin drug precursor (BDP-SN38) with fluorescent activity. BDP-SN38 shows good solubility and stability in most pharmaceutically acceptable solvents. Compared with SN38, BDP-SN38 exhibits comparable antitumor activity, has high tumor uptake capacity, and produces strong green fluorescence with the excitation of visible light, thus providing fluorescence-guided bioimaging and further treatment of residual tumors after drug treatment, and having good application prospects in the research of integrated diagnosis and treatment and effective tumor treatment.