The mitogen-activated protein kinases, MEK1 and 2, are dual-specificity threonine/tyrosine kinases that play key roles in the activation of the Ras-Raf-MEK-ERK pathway and are often upregulated in a variety of cancer cell types. AS-703026 is an orally bioavailable small molecule that selectively binds to and...

Soluble in DMSO. Slightly soluble (<1mg/ml) in ethanol. AS703026 is a novel, selective, non-competitive, orally bioavailable MEK1/2 inhibitor with experimental IC(50) values of 5-11nM. In use on multiple myeloma cells (MM), AS703026 inhibited growth and survival of MM cells and cytokine-induced osteoclast...

AS-703026 is an inhibitor of MEK1/2 that exhibits anticancer chemotherapeutic activity. In vitro, AS-703026 inhibits proliferation of melanoma cells. In both in vitro and in vivo models of colorectal cancer containing WT Ras or mutant KRAS, AS-703026 inhibits growth of cells and also of tumors. Additionally,...