BI3406

BI3406 is a potent, selective, and orally bioavailable small-molecule inhibitor of the Son of Sevenless homolog 1 (SOS1), a guanine nucleotide exchange factor (GEF) that facilitates the activation of RAS proteins. By binding to the catalytic site of SOS1, BI3406 prevents the interaction between SOS1 and RAS-GDP, thereby blocking the exchange of GDP for GTP and inhibiting the activation of various RAS isoforms, including KRAS, HRAS, and NRAS. It is particularly effective against KRAS-mutant tumors, including those with G12 and G13 mutations. BI3406 has demonstrated synergistic activity when combined with MEK inhibitors or direct KRAS G12C inhibitors, helping to overcome adaptive resistance mechanisms. It was developed by Boehringer Ingelheim as a first-in-class tool to target the RAS pathway by inhibiting its universal activator.

Brand names

BI-3406BI3406BI 3406

Other names

BI-3406BI3406BI 3406