For the first time, we evaluated the efficacy of systemic targeting of the TGF-β pathway by a TGβRI kinase inhibitor, SD-208, on a high-grade colon adenocarcinoma cell line, SW-48, in vitro and in developed heterotopic colon tumors in model that shares similarities with human colon cancer. This evidence concerns the gene TGFB1 and malignant colon neoplasm.