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