Temuterkib (LY-3214996) is a novel potent, selective, orally active ERK1/2 inhibitor with IC50 of 5 nM for both enzymes in biochemical assays.
Temuterkib (LY-3214996) potently inhibits cellular phospho-RSK1 in BRAF and RAS mutant cancer cell lines.
Temuterkib (LY-3214996) demonstrates inhibition of cell proliferation, general sensitivitity against tumor cells with MAPK pathway alterations including BRAF, NRAS or KRAS mutation.
Temuterkib (LY-3214996) significantly inhibits tumor growth in vivo and is well tolerated in BRAF or NRAS mutant melanoma, BRAF or KRAS mutant colorectal, lung and pancreatic cancer xenografts or PDX models.
