trametinib-dmso-solvate

Description: Trametinib DMSO solvate is the solvated form of trametinib (trametinib: dimethyl sulfoxide=1:1) and a potent MEK inhibitor that specifically inhibits MEK1/2 with an IC50 value of about 2 nM. Trametinib, also known as GSK1120212 or JTP 74057, is a highly specific and potent MEK1/2 inhibitor with IC50 of 0.92 nM/1.8 nM in cell-free assays, it has no inhibition of the kinase activities of c-Raf, B-Raf, ERK1/2. Trametinib has potential antineoplastic activity and was originally identified as a p15 inductive compound but was later found to be an allosteric inhibitor of MEK kinase.Trametinib exhibits ATP non-competitive inhibition against MEK1 and MEK2 kinase. Trametinib specifically binds to and inhibits MEK 1 and 2, resulting in an inhibition of growth factor-mediated cell signaling and cellular proliferation in various cancers. MEK 1 and 2, dual specificity threonine/tyrosine kinases often upregulated in various cancer cell types, play a key role in the activation of the RAS/RAF/MEK/ERK signaling pathway that regulates cell growth. FDA approved Trametinib for the treatment of melanoma on May 29, 2013.

References: Int J Oncol. 2011 Jul; 39(1):23-31; Inflamm Res. 2012 May; 61(5):445-54.

Related CAS#: 871700-17-3 (Trametinib)