The cGAMP-siPDL1@GalNPs nanocarriers effectively and selectively activated the STING pathway in cancer cells via GLUT-1 to increase the biological activity of cGAMP, which stimulated a series of immune responses, and down-regulated the PD-L1 expression in cancer cells and tumors to prohibit the immune escape and eliminate the side effects of STING agonists. This evidence concerns the gene STING1 and cancer.