SCH772984 is a potent and selective inhibitor of ERK1/ERK2 with IC50 of 4 nM/1 nM, respectively.
SCH772984 is highly selective, with only seven kinases of 300 showing >50% inhibition at 1 uM.
SCH772984 prevents MEK-mediated ERK phosphorylation, reduces pCRAF S289/S296/S301 phosphorylation.
SCH772984 has nanomolar cellular potency in tumor cells with mutations in BRAF, NRAS, or KRAS and induces tumor regressions in xenograft models.
