Discovery of Thiazolo[5,4-c]pyridine Derivatives as Novel Hematopoietic Progenitor Kinase 1 Inhibitors for Tumor Immunotherapy.
This new inhibitor exhibits potent HPK1 inhibition, high selectivity within the MAP4K family, along with improved metabolic properties and reduced hERG liability, and demonstrates robust monotherapy efficacy and synergizes with an anti-PD-1 antibody or an anti-PD-L1/IL-15 immunocytokine prodrug.