LY-3214996 is an orally bioavailable, potent and highly selective inhibitor of ERK1 and ERK2, with IC50 of 5 nM for both enzymes in biochemical assays. It potently inhibits cellular phospho-RSK1 in BRAF and RAS mutant cancer cell lines. In an unbiased tumor cell panel sensitivity profiling for inhibition of cell proliferation, tumor cells with MAPK pathway alterations including BRAF, NRAS or KRAS mutation are generally sensitivity to LY-3214996. In tumor xenograft models, LY-3214996 inhibits PD biomarker phospho-p90RSK1 in tumors and the PD effects are correlated with compound exposures and anti-tumor activities.

KEYWORDS: LY-3214996 | Supplier | ERK1 and ERK2 inhibitor | Temuterkib | LY3214996 | LY 3214996 | CT-LY321  | CAS [1951483-29-6] | MAPK | ERK | Inhibitor | Enzymes