Batoprotafib (TNO155) is a highly potent, selective, orally active, and allosteric SHP2 (PTPN11) inhibitor with IC50 of 11 nM.
TNO155 is efficacious in acquired resistance models of EGFRi and demonstrates combination benefits with EGFR inhibitors, inhibits EGFR-mutant NSCLC cell lines NCI-H3255, HCC827, and PC9 with IC50 of <1.5 uM.
TNO155 also sensitizes BRAF-mutant colorectal cancer to inhibitors of BRAF and MEK, and enhances the efficacy of KRASG12C inhibitors against KRASG12C lung and colorectal cancers.
Ribociclib enhances the efficacy of TNO155 in both RTK-activated and KRAS-mutant cancers.
NO155 inhibits immune-suppressive macrophages and synergizes with PD1 blockade.
