A　novel　multifunctional　nano-system,　ZnPc-UCNPs-PEG-G,　was　designed　for　targeted　and　in-depth　photodynamic　therapy.　The　nano-system　was　built　via　covalent　conjugation,　in　which　phthalocyanine　zinc　(ZnPc),　Gefitinib　(G),　NaYF4:　Yb,　Er　(UCNPs)　and　PEG　derivatives　were　employed　as　the　photosensitizer,　target　moiety,　upconversion　nanomaterial　and　linker　unit,　respectively.　The　photophysical/chemical　properties,　in-depth　photodynamic　activity,　cancer　cell　specificity　and　anticancer　activity　of　ZnPc-UCNPs-PEG-G　were　investigated.　The　as-prepared　ZnPc-UCNPs-PEG-G　exhibits　excellent　photosensitizing　ability,　generating　reactive　oxygen　species　(ROS)　via　effective　energy　transfer　from　UCNP　to　phthalocyanine　zinc.　In　addition,　the　composite　exhibits　specific　affinity　to　HepG2　cancer　cells　and　high　anticancer　activity.　To　the　best　of　our　knowledge,　this　is　the　only　example　of　a　UCNP　platform　that　is　capable　of　molecular　targeted　and　in-depth　photodynamic　and　chemo-anticancer　therapy　via　the　introduction　of　a　small　molecular　targeting　drug　moiety.