Avutometinib (RO 5126766, CH5126766, VS-6766) is a potent, first-in-class dual Raf/MEK inhibitor with IC50 of 56 nM/160 nM for C-Raf/MEK1.
Avutometinib (RO 5126766, CH5126766, VS-6766) shows weak or no inhibition on CYP2C9, CYP3A4 and hERG.
Avutometinib (RO 5126766, CH5126766, VS-6766) inhibits ERK signaling output more effectively than a standard MEK inhibitor PD0325901 that induces MEK phosphorylation and has potent antitumor activity as well.
