AZD 8330 is a selective allosteric inhibitor of MEK1/2 (IC50 = 7 nM). It blocks phosphorylation of ERK1/2 and inhibits proliferation of certain cancer cells. AZD 8330 is orally bioavailable, inhibits ERK phosphorylation in vivo, and reduces tumor growth in a Calu-6 nude rat xenograft model.
1. feng k, wang c, zhou h, yang j, dong l, zhou k, et al. [effect of erk1/2 inhibitor azd8330 on human burkitt's lymphoma cell line raji cells and its mechanism]. zhonghua xue ye xue za zhi 2015,36:148-152.2. cohen rb, aamdal s, nyakas m, cavallin m, green d, learoyd m, et al. a phase i dose-finding, safety and tolerability study of azd8330 in patients with advanced malignancies. eur j cancer 2013,49:1521-1529.