Trametinib (GSK-1120212)

    • 货号:MC0039
      • CasNo:
      • 871700-17-3
      • 分子式:
      • C26H23FIN5O4
      • 纯度:
      • >98%
      • 靶点:
      • MEK
      • IC50:
      • IC50: 2 nM (MEK1/2)[1]
      • 体外研究:
      • Trametinib (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-cyclearrest at the G1 phase after drug tratment[1]. 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[2].
      • 体内研究:
      • Adjuvant-induced arthritis (AIA) and type II collageninduced arthritis (CIA) development are suppressed almost completely by 0.1 mg/kg of JTP-74057 or 10 mg/kg of Leflunomide. In the CIA, JTP-74057 suppresses collagen-reactive T-cell proliferation ex vivo[1]. Trametinib (0.3 mg/kg, 1 mg/kg, p.o.) effective in inhibiting the HT-29 xenograft growth in a nude mouse xenograft model[2].
      • 简介:
      • GSK1120212 (JTP-74057, trametinib) is a highly specific and potent MEK1 and MEK2 inhibitor with IC50 of 0.92 nM and 1.8 nM, respectively.
      • 特异性:
      • Target: MEK. Fields: GSK1120212 (JTP-74057, trametinib) is a highly specific and potent MEK1 and MEK2 inhibitor with IC50 of 0.92 nM and 1.8 nM, respectively.
      • 稀释:
      • IC50: 2 nM (MEK1/2)[1]
      • 浓度:
      • >98%
      • 储存:
      • 2 years -20°C Powder, 2 weeks4°C in DMSO,6 months-80°C in DMSO
      • 其他名称:
      • GSK212, GSK 1120212 , JTP-74057, trametinib, GSK1120212
      • 分子量:
      • 615.39
      • 产品图片