The disclosure relates to azaindolizines of formula (I-a) with anti-cancer and/or anti-inflammatory activity and more specifically to azaindolizines which inhibit MEK kinase activity. The disclosure also relates to compositions and methods useful for inhibiting abnormal cell growth or treating a hyperproliferative disorder, or treating an inflammatory disease in a mammal. The disclosure further relates to methods of using the compounds for in vitro, in situ, and in vivo diagnosis or treatment of mammalian cells, or associated pathological conditions.