A　series　of　novel　symmetric　or　unsymmetric　silicon　(IV)　phthalocyanines　axially　substituted　with　cyclic　Arg-Gly-Asp　(cRGD)　ligands　through　different　ethylene　glycol　chains　have　been　synthesized　by　a　facile　and　mild　＂click＂　reaction.　All　the　compounds　show　efficient　photosensitizing　activities　in　N,N-dimethylformamide,　and　are　essentially　non-aggregated　in　RPMI　1640　medium　with　0.05%　Cremophor　EL.　Owing　to　the　presence　of　two　cRGD　ligands,　the　conjugate　6b　exhibits　highest　selectivity　toward　alpha(v)beta(+)(3)　HT-29　cells　in　photocytotoxicities.　It　shows　higher　cellular　uptake　and　ROS　generation　efficiency　toward　the　alpha(v)beta(+)(3)　HT-29　cells　compared　with　that　of　alpha(v)beta(+)(3)　MCF-7　cells.　The　competitive　cellular　uptake　and　subcellular　localization　indicate　that　6b　is　internalized　mainly　through　integrin-mediated　endocytosis.　In　addition,　the　in　vivo　studies　showed　that　6b　can　mainly　accumulate　in　tumor　sites　and　show　a　significant　PDT　effect　resulting　in　75%　tumor　growth　inhibition.　The　results　indicate　that　6b　is　a　highly　promising　photosensitizer　for　targeted　photodynamic　therapy.　(C)　2018　Elsevier　Masson　SAS.　All　rights　reserved.