TK0019

TK0019 is a small molecule discoidin domain receptor 1 (DDR1) tyrosine kinase inhibitor discovered via target-based small molecule array screening. It binds directly to the extracellular N-terminal region of the DDR1 protein, specifically inhibiting DDR1 kinase activation in response to its ligand. TK0019 also targets downstream proteins involved in the epithelial-mesenchymal transition (EMT) pathway, such as Slug, AKT, and vimentin, thereby suppressing AKT activation and essential EMT pathway proteins involved in tumor migration and invasion. It has demonstrated antiproliferative activity against various DDR1-overexpressing cancer cell lines, including EGFR-targeted drug-resistant cancer cells, and has shown potent anti-growth and anti-metastatic properties in preclinical breast cancer models.