Trametinib

Trametinib is a potent and selective MEK1 and MEK2 inhibitor (IC₅₀ = 0.92 and 1.8 nM, respectively, in cell-free assays). In vitro, it inhibits the growth of human colorectal cancer cell lines expressing either B-RAF or K-RAF (IC₅₀ values range from 0.48 to 36 nM). In vivo, it suppresses tumor growth of HT-29 and COLO205 xenografts in nude mice. Trametinib induces apoptosis. This compound is orally bioavailable.