Cat No:LP000067
Product Name:GSK1070916
CAS NO:942918-07-2
Purity: ≥99%
Solubility: In DMSO
Storage: -20°C
The dual specificity mitogen-activated protein kinase kinases (MEK) isoforms MEK1 and MEK2 function in a RAS/RAF/MEK/ERK signaling pathway to control cell growth, survival, and differentiation. Trametinib is a potent inhibitor of both MEK 1 and 2 that works in an ATP-noncompetitive fashion (IC50s = 0.7 and 0.9 nM, respectively).1 It shows specificity for MEK1/2 over a panel of more than 180 kinases, including B-Raf, c-Raf, and MEK5.1 Trametinib blocks dual phosphorylation of ERK1/2 and stops cell cycling in cancer cell lines, both in vitro and in multiple tumor models in mice.1 Trametinib, alone or in combination with other chemotherapeutic drugs, targets a subset of cancer cells that can be characterized by specific biomarkers, such as B-Raf, RAS, or CTNNB1 mutations.
