AMG 410

AMG410 is a non-covalent, selective inhibitor of pan-KRAS with IC50 of 1–4 nM for KRAS G12D, G12V, and G13D. It binds both GDP- and GTP-bound KRAS with Kd of 1 nM and 22 nM, respectively. AMG410 inhibits KRAS signaling in a nucleotide cycling-independent manner. It also suppresses proliferation in KRAS-amplified wild-type tumor cells.