ETS-001

ETS-001 is a potent, selective, and orally bioavailable small-molecule allosteric inhibitor of SHP2 (Src homology region 2 domain-containing phosphatase 2), developed by Shanghai ETERN Biopharma. SHP2, encoded by the PTPN11 gene, is a non-receptor protein tyrosine phosphatase that acts as a critical signaling node downstream of various receptor tyrosine kinases (RTKs), facilitating the full activation of the RAS/MAPK pathway. By inhibiting SHP2, ETS-001 suppresses RAS/MAPK signaling and inhibits cell growth in cancers driven by RTK or RAS mutations. Preclinical studies have demonstrated its efficacy as a monotherapy and in combination with other targeted therapies, such as EGFR inhibitors (osimertinib), KRAS G12C inhibitors (sotorasib), and CDK4/6 inhibitors (ribociclib), to overcome or delay drug resistance in models of non-small cell lung cancer, pancreatic cancer, and esophageal cancer.