Trametinib (GSK1120212)

属性

溶解性	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).
存贮条件	储存温度-20°C

描述

应用	An allosteric inhibitor of MEK1/MEK2.
产品介绍	Trametinib (GSK1120212)是一种高特异性的，有效的MEK1/2抑制剂，IC50为0.92 nM/1.8 nM，对c-Raf， B-Raf， ERK1/2没有抑制活性。
备注	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. Phase 3.
生化机理	Trametinib is an allosteric reversible, selective MEK1/MEK2 kinase activity inhibitor with IC50 of 0.7 and 0.9 nM for MEK1 and MEK2.
别名	GSK-1120212; JTP 74057; GSK1120212; GSK 1120212; JTP-74057; JTP74057;N-[3-[3-环丙基-5-[(2-氟-4-碘苯基)氨基]-3,4,6,7-四氢-6,8-二甲基-2,4,7-三氧代吡啶并[4,3-d]嘧啶-1(2H)-基]苯基]乙酰胺;曲美替尼;GSK-1120212; JTP 74057; GSK1120212; GSK 1120212; JTP-74057; JTP74057;N-[3-[3-Cyclopropyl-5-[(2-fluoro-4-iodophenyl)amino]-3,4,6,7-tetrahydro-6,8-dimethyl-2,4,7-trioxopyrido[4,3-d]pyrimidin-1(2H)-yl]phenyl]acetamide