The invention discloses a targeted
protein degradation agent utilizing an
autophagy-
lysosome pathway as well as a preparation method and application of the targeted
protein degradation agent, and belongs to the technical field of degradation agent preparation. The preparation method comprises the following steps: carrying out
nucleophilic substitution reaction on a GW5074 derivative and a
linker arm precursor to obtain a GW5074 derivative-
linker arm intermediate, and
coupling the GW5074 derivative-
linker arm intermediate with demethylated
imatinib to obtain the targeted
protein degradation agent utilizing the
autophagy-
lysosome pathway. The
protein degradation agent disclosed by the invention is relatively few in preparation steps, easy to synthesize and relatively high in yield, and can be used for preparing medicines for treating cancers, particularly antitumor medicines for treating
chronic granulocytic leukemia.