Zinc(II)　phthalocyanines　are　favorable　candidates　as　photosensitizers　(PSs)　for　photodynamic　therapy　(PDT).　However,　zinc(II)　phthalocyanines　also　suffer　from　poor　water　solubility　and　low　tumor-targeting　ability.　In　this　study,　a　novel　zinc(II)　phthalocyanine　tetra-substituted　with　sulphonates　using　?sulfur　bridge?　as　the　linkages　was　developed　(ZnPc3),　which　exhibits　high　water-solubility　and　natural　tumor　targeting.　Furthermore,　ZnPc3　possesses　red-shifted　absorption　and　fluorescence　spectra　as　compared　to　the　unsubstituted　zinc(II)　phthalocyanine.　In　vivo　fluorescence　imaging　indicates　that　ZnPc3　possesses　an　excellent　tumor　selectivity　after　intravenous　injection　without　any　help　of　targeting　ligands　or　extra　nanomaterials.　The　results　of　in　vivo　phototherapy　evaluation　suggest　that　ZnPc3-induced　PDT　could　effectively　inhibit　the　tumor　growth　in　a　mouse　model.