Phthalocyanine　zinc(ZnPc)　and　its　derivatives　is　a　class　of　promising　photosensitizer　due　to　its　superior　photodynamic　activity.　However,　the　poor　water　solubility　and　the　difficulty　to　obtain　pure　ZnPc　compounds　limit　the　clinical　development　of　this　class　of　photosensitizer.　We　developed　a　large　scale　preparation　and　purification　of　a　new　asymmetric　phthalocyanine　zinc　compound,　2-carboxyphthalocyanine　zinc.　Here　we　report　the　synthesis　of　pentalysine　2-carbonylphthalocyanine　zinc　and　its　photodynamic　activity.　The　compound　was　characterized　by　analytical　and　spectroscopic　methods.　The　phototoxicity　of　this　compound　was　evaluated　in　vitro　with　human　liver　cancer　cell　line　(Bel7402),　human　gastric　carcinoma　cell　line　(BGC823),　human　leukemia　cell　line(K562)　and　human　embryo　lung　fibroblast　cell　line　(HELF).　This　compound　shows　not　only　the　phototoxicity　to　these　cells,　but　also　improves　water　solubility.　We　also　demonstrate　that　the　presence　of　cell　breaks　down　the　aggregation　of　pentalysine　2-carbonylphthalocyanine　zinc　in　aqueous　solution.