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Biological Activity:
Highly potent and selective MEK inhibitor, with IC50 values to be 0.7 and 0.9 nM for MEK1 and MEK2 respectively and with long circulating half-life.
References:
AG Gilmartin et al. GSK1120212 (JTP-74057) is an inhibitor of MEK activity and activation with favorable pharmacokinetic properties for sustained in vivo pathway inhibition. Clin. Cancer Res. 2011, 17(5), 989-1000. [online]
T Yamaguchi et al. Antitumor activities of JTP-74057 (GSK1120212), a novel MEK1/2 inhibitor, on colorectal cancer cell lines in vitro and in vivo. Int J Oncol. 2011, 39(1), 23-31. [online]
H Abe et al. Discovery of a Highly Potent and Selective MEK Inhibitor: GSK1120212 (JTP-74057 DMSO Solvate). ACS Med. Chem. Lett., 2011, 2(4), 320–324. [online]
Chemical Name: N-{3-[3-cyclopropyl-5-(2-fluoro-4-iodophenylamino)-6,8-dimethyl-2,4,7-trioxo-3,4,6,7-tetrahydro-2H-pyrido[4,3-d]pyrimidin-1-yl]phenyl}acetamide
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