AZD0530, a powerful small-molecule inhibitor from the Src kinase family, is definitely an anticancer drug utilized in treating various cancers. Within the situation of glioblastoma (GBM), where potential to deal with radiotherapy frequently occurs, Src kinase is famous among the molecules accountable for imparting radioresistance to GBM. Thus, we evaluated the result of AZD0530 around the radiosensitivity of human GBM cells and human glioblastoma stem-like cells (GSCs). We reveal that Src activity of GBM and GSC is elevated by radiation and inhibited by AZD0530, and taking advantage of clonogenic assays, AZD0530 improves the radiosensitivity of GBM and GSCs. Also, AZD0530 caused a prolongation of radiation-caused γH2AX without specific cell cycle and mitotic index changes, suggesting that AZD0530-caused radiosensitization in GBM cells and GSCs is a result of the inhibition of DNA repair. Additionally, AZD0530 was proven to hinder rays-caused EGFR/PI3K/AKT path, which may promote and regulate radioresistance and survival of GBM cells by radiation. Finally, rodents bearing orthotopic xenografts initiated from GBM cells were then accustomed to assess the in vivo reaction to AZD0530 and radiation. The mixture of AZD0530 and radiation demonstrated a long median survival in contrast to any single modality. Thus, these results reveal that AZD0530 improves the radiosensitivity of GBM cells and GSCs and suggest the potential of AZD0530 like a clinical radiosensitizer to treat GBM.