In this study, we investigated the in vitro potential of axially 1-morpholiniumpropan-2-ol disubstituted silicon (IV) phthalocyanine (SiPc) which was synthesized previously, on HCT-116 cells as a photodynamic therapy (PDT) agent. The singlet oxygen and photodegradation quantum yields of SiPc were calculated using UV-vis spectrophotometer. The cytotoxic and phototoxic effects of SiPc were evaluated by 3-[4,5-dimethylthiazol-2-yl]-2,5 diphenyl tetrazolium bromide (MTT) assay. Annexin V-FITC/PI double staining kit, cell cycle kit, and mitochondria membrane potential (Delta Psi m) assay kit with JC-1 were used to indicate the cell death pathway. Caspase-3 and beta-catenin protein expressions were evaluated by western blotting. The singlet oxygen and photodegradation quantum yields of SiPc were calculated as 0.73 and 3.64 x 10(-4) in DMSO. The cell viability assays showed that IC50 value of SiPc did not reach to 100 mu M without irradiation. However, excellent phototoxicity was observed in the presence of SiPc upon light irradiation. The cells undergoing early/late apoptosis significantly increased in the presence SiPc at 5 mu M upon light irradiation. Besides, the proportion of cells at S and G2/M phase increased. Moreover, mitochondria membrane potentials significantly decreased at 1 and 5 mu M of SiPc with light irradiation. While caspase-3 expression increased, beta-catenin expression significantly decreased on HCT-116 in the presence of SiPc (p < 0.01). The results indicated that the PDT could be related to apoptosis and Wnt/beta-catenin signaling pathway. Based on our findings, SiPc exhibited a significant PDT effect on HCT-116 cells therefore, worthy of more detailed study.