ZB-60

ZB-60 is a novel, orally bioavailable, selective, and potent small molecule inhibitor of the Receptor d'origine nantais (RON) kinase, also known as macrophage-stimulating protein receptor (MST1R). Developed by the Translational Genomics Research Institute (TGen) and the University of Utah (Huntsman Cancer Institute), ZB-60 targets both full-length and truncated isoforms of RON kinase, which is aberrantly activated or overexpressed in various solid tumors, including breast and colorectal cancers. By inhibiting RON kinase activity (with an IC50 of 56 nM) and its downstream signaling pathways, ZB-60 aims to promote anti-tumor immunity within the tumor microenvironment and block pro-metastatic signaling. In preclinical studies, ZB-60 has demonstrated favorable oral bioavailability, low clearance, and significant in vivo tumor growth inhibition in syngeneic mouse models of breast and colorectal cancer, both as a monotherapy and in potential combination with immune checkpoint inhibitors.