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GSK1120212(Trametinib)
Cat No.
CEI-0161
Description
GSK1120212 can inhibit MEK1 and MEK2 with IC50 of 0.92 nM and 1.8 nM.
Alias
JTP-74057
CAS No.
871700-17-3
Molecular Weight
615.3947932
Purity
>99%
Storage
2 years at -20centigrade Powder
Synonyms
JTP-74057
Targets
MEK1, MEK2
Molecular Formula
C26H23FIN5O4
Chemical Name
N-(3-(3-cyclopropyl-5-(2-fluoro-4-iodophenylamino)-6,8-dimethyl-2,4,7-trioxo-3,4,6,7-tetrahydropyrido[4,3-d]pyrimidin-1(2H)-yl)phenyl)acetamide
Solubility
DMSO 5 mg/mL Water
In vitro
GSK1120212 inhibits MEK1/2 kinase activity and prevents Raf-dependent MEK phosphorylation (S217 for MEK1), producing prolonged p-ERK1/2 inhibition. GSK1120212 also reduced tumor Ki67, increased p27(Kip1/CDKN1B), and caused tumor growth inhibition in multiple tumor models. Treatment by GSK1120212 would result in growth inhibition accompanied with upregulation of p15INK4b and/or p27KIP1 in most of the colorectal cancer cell lines.
In vivo
The capability of GSK1120212 to inhibit ERK1/2 phosphorylation (p-ERK) in vivo was assessed in A-375P(F11) (melanoma encoding BRAFV600E mutation) xenograft model. GSK1120212(3 mg/kg), the 14-day MTD in nude mice, was administrated daily by oral gavage.
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