Trametinib is an allosteric reversible, selective MEK1/MEK2 kinase activity inhibitor with IC50 of 0.7 and 0.9 nM for MEK1 and MEK2.
Storage Temp
Store at -20°C
Shipped In
Ice chest + Ice pads
Grade
Moligand™
Action Type
INHIBITOR
Mechanism of action
Dual specificity mitogen-activated protein kinase kinase; MEK1/2 inhibitor
Note
500mg卖完停产，不再备货
Product Description
Trametinib (GSK1120212) is a highly specific and potent MEK1/2 inhibitor with IC50 of 0.92 nM/1.8 nM, no inhibition of the kinase activities of c-Raf, B-Raf, ERK1/2. An allosteric inhibitor of MEK1/MEK2.
Product Properties
ALogP
3.4
Associated Targets
CGGBP1Tbio CGG triplet repeat-binding protein 1 0 Activities
Soluble in DMSO (100 mg/mL at 25 °C), water (<1 mg/mL at 25 °C), ethanol (<1 mg/mL at 25 °C), and 30% PEG400/0.5% Tween80/5% propylene glycol (15 mg/ml).
1.Gilmartin AG, Bleam MR, Groy A, Moss KG, Minthorn EA, Kulkarni SG, Rominger CM, Erskine S, Fisher KE, Yang J et al.. (2011) GSK1120212 (JTP-74057) is an inhibitor of MEK activity and activation with favorable pharmacokinetic properties for sustained in vivo pathway inhibition.. Clin Cancer Res, 17 (5):(989-1000). [PMID:21245089]
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H2209663