TD-19

TD-19 is a novel small molecule erlotinib derivative that acts as a SET/PP2A protein-protein interaction antagonist and a CIP2A inhibitor. Unlike erlotinib, TD-19 is designed to be devoid of EGFR tyrosine kinase inhibitory activity. It exerts its anti-tumor effects by disrupting the interaction between the oncoprotein SET and the catalytic subunit of protein phosphatase 2A (PP2Ac), thereby restoring PP2A activity. This reactivation of PP2A leads to the downregulation of cancerous inhibitor of PP2A (CIP2A) and the dephosphorylation of Akt and ERK, which induces apoptosis in cancer cells. TD-19 has demonstrated preclinical efficacy in triple-negative breast cancer (TNBC) and epidermal growth factor receptor (EGFR) wild-type non-small-cell lung cancer (NSCLC).

Other names

CIP2A Inhibitor, TD-19N4-(3-ethynylphenyl)-6,7-dimethoxy-N2-(4-phenoxyphenyl)quinazoline-2,4-diamine