TAK-733

TAK-733 is an inhibitor of MEK1 (IC₅₀ = 3.2 nM), a MAP kinase in the Raf/MEK/ERK pathway that plays a major role in the regulation of cellular growth, differentiation, and proliferation.¹,² It is selective for MEK1 over a panel of 18 kinases, receptors, and ion channels up to a concentration of 10 µM. TAK-733 inhibits ERK phosphorylation in vitro (EC₅₀ = 1.9 nM). It also inhibits proliferation of A375 and COLO 205 cells (EC₅₀s = 3.1 and 2.1 nM, respectively) and 14 cutaneous melanoma cell lines (IC₅₀s = <1-10 nM), particularly those with B-RAF^V600E mutations.¹,³ TAK-733 has antitumor activity in mouse xenograft models using a variety of cancer types.¹

WARNING This product is not for human or veterinary use.

1. Dong, Q., Dougan, D.R., Gong, X., et al. Discovery of TAK-733, a potent and selective MEK allosteric site inhibitor for the treatment of cancer. Bioorg. Med. Chem. Lett. 21(5), 1315-1319 (2011).

2. Cowan, K.J., and Storey, K.B. Mitogen-activated protein kinases: New signaling pathways functioning in cellular responses to environmental stress. J. Exp. Biol. 206(Pt 7), 1107-1115 (2003).

3. von Euw, E., Atefi, M., Attar, N., et al. Antitumor effects of the investigational selective MEK inhibitor TAK733 against cutaneous and uveal melanoma cell lines. Mol. Cancer 11, 22 (2012).