An　amphiphilic　2,10-di-sulfonato-18,26-di-phthalimidomethyl　phthalocyanine　zinc　di-potassium　salt　(3)　was　synthesized　by　first　direct　condensation　of　hydrophilic　precursor　4-sulfonic　phthalic　acid　mono-potassium　salt　(1)　with　hydrophobic　precursor　4-phthalimidomethyl　phthalic　acid　(2).　Then　the　condensed　mixture　was　separated　by　reverse　HPLC　method　and　further　purified　by　a　membrane　separation　method.　The　composition　of　the　title　compound　was　characterized　by　elemental　analysis,　UV,　H-1　NMR,　C-13　NMR　as　well　as　TG　and　DTA,　and　its　C-4h-structure　was　identified　according　to　the　H-1　NMR　signal　of　submethyl　protons　of　the　phthalimidomethyl　groups　in　the　phthalocyanine　ring,　polarity　and　synthetic　mechanism.　In　vivo　antitumor　activity　of　the　title　compound　as　photosensitizer　showed　that　its　inhibitory　rate　was　up　to　90.3%.　This　amphiphilic　photosensitizer　has　a　potential　application　in　the　photodynamic　therapy　of　cancer.　(c)　2004　Elsevier　Ltd.　All　rights　reserved.