AZD8330 (ARRY-424704, ARRY-704) is a potent, selective, non-ATP competitive MEK1/2 inhibitor with IC50 of 7 nM.
AZD8330 displays no inhibitory activity against a panel of >200 other kinases.
AZD8330 demonstrates sub-nanomolar potency in mechanistic (pERK) and low to sub-nanomolar potency in functional (proliferation) assays in MEK1/2 inhibitor sensitive cell lines.
AZD8330 inhibits ERK phosphorylation and causes tumor growth inhibition in Calu-6 rat xenograft.
