In the present study, we have attempted to evaluate the potential of developing acetylshikonin, a major biologically active compound present in Lithospermum erythrorhizon root (Cho, Paik, & Hahn, 1999; Rajasekar et al., 2012), as a TOPK inhibitor and assess its anti‐cancer effects in cultureds of colorectal cancer cells and in patient‐derived xenograft (PDX) tumour models in mice. This evidence concerns the gene PBK and colorectal cancer.