TAK-733 (TAK733,TAK 733) is a potent, selective, allosteric inhibitor of MEK with IC50 of 3.2 nM (MEK1).
TAK-733 shows selectivity for MEK1 over a panel of 18 kinases, receptors, and ion channels at 1 uM.
TAK-733 inhibits ERK phosphorylation in vitro with EC50 of 1.9 nM, also inhibits proliferation of A375 and COLO 205 cells with IC50 of 3.1 nM and 2.1 nM, respectively.
TAK-733 demonstrates antitumor activity in multiple mouse xenograft models.
