In vitro study | AS703026 is a novel selective, Orally Bioavailable MEK1/2 inhibitor that binds to specific MEK allosteric sites with strong kinase selectivity. AS703026 inhibits the growth and survival of human multiple myeloma cells (including U266 and INA-6 cells) with IC50 of 5 and 11 nM, respectively. Cell cycle arrest in the G0-G1 phase modulates the inhibitory effect of AS703026 and is accompanied by a decrease in the expression of the MAF oncogene. AS703026 acts on MM cells to induce apoptosis by lysing caspase-3 and PARP. AS703026 is effective in the treatment of mutated colorectal cancer. 10 μm AS703026 was effective at inhibiting the ERK pathway, proliferation, and transformation in human colorectal cancer cells carrying the K-Ras (D-MUT) mutant allele. |