Trametinib

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

一种有效且高度特异性的 MEK1/2 抑制剂，IC50 为 0.92 nM/1.8 nM。

A potent and highly specific MEK1/2 inhibitor with IC50 of 0.92 nM/1.8 nM; exhibits no inhibition on the kinase activities of c-Raf, B-Raf, ERK1/2.Skin Cancer Approved(In Vitro):Trametinib (GSK1120212;JTP-74057) (0.1-100 nM) blocks tumor necrosis factor-α and interleukin-6 production from peripheral blood mononuclear cells (PBMCs). Trametinib (JTP-74057) inhibits the growth of 9 out of 10 human colorectal cancer cell lines, and they shows cell-cycle arrest at the G1 phase after drug tratment.The combination of GSK2118436 and Trametinib (GSK1120212) effectively inhibits cell growth, decreases ERK phosphorylation, decreases cyclin D1 protein, and increases p27(kip1) protein in the resistant clones.(In Vivo):Adjuvant-induced arthritis (AIA) and type II collageninduced arthritis (CIA) development are suppressed almost completely by 0.1 mg/kg of Trametinib (GSK1120212; JTP-74057) or 10 mg/kg of HWA486.Trametinib (0.3 mg/kg, 1 mg/kg, p.o.) is effective in inhibiting the HT-29 xenograft growth in a nude mouse xenograft model.

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GSK-1120212 | JTP 74057 | GSK1120212 | GSK 1120212 | JTP-74057 | JTP74057

MAPK/ERK Signaling

MEK

MEK1|MEK2

Cancer

Skin Cancer

871700-17-3

615.3948

C26H23FIN5O4

>98% (HPLC)

10 mM in DMSO

CC(NC1=CC=CC(N(C(C(C(N2C3CC3)=O)=C(NC4=CC=C(I)C=C4F)N5C)=C(C)C5=O)C2=O)=C1)=O

Acetamide, 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]-

(-20℃)

With Ice Pack

≥ 2 years