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当前位置: 首页 > 信号通路研究 > MEK > Trametinib (GSK1120212)
Trametinib (GSK1120212)
Trametinib (GSK1120212)
Trametinib (GSK1120212)
商品货号:MB5401
CAS 号:871700-17-3
英文名字:曲美替尼
质量标准:>99%,MEK抑制剂
分子式:C26H23FIN5O4
  • 包装规格:
    规格 库存 发货时间
    100MG [¥980.00]14 现货
    1G [¥3800.00]15 现货
  • 购买数量:
  • 会员尊享价:

    商品信息

    质检证书(coa)

    说明书下载

    曲美替尼

    分子式:C26H23FIN5O4    分子量:615.39

    相关谱图:

    HNMR

    产品描述

    GSK1120212 (JTP-74057, Trametinib)是高特异性的,有效的MEK1/2抑制剂,IC500.92 nM/1.8 nM,c-Raf, B-Raf, ERK1/2没有抑制活性。

    靶点

    MEK1

    MEK2

           

    IC50

    0.92 nM

    1.8 nM

           

    体外研究

    GSK1120212 inhibits the phosphorylation of MBP regardless of the isotype of Raf and MEK, with IC50 ranging from 0.92 nM to 3.4 nM. GSK1120212 demonstrates no inhibition of the kinase activities of c-Raf, B-Raf, ERK1 and ERK2. In addition, GSK1120212 does not show drastic inhibitory activity against the other 98 kinases. GSK1120212 displays potent inhibitory activity against human colorectal cancer cell lines. HT-29 and COLO205 cells, which are known to have a constitutively active B-Raf mutant, are most sensitive to GSK1120212 with IC50 0.48 nM and 0.52 nM, respectively. The cell lines bearing a K-Ras mutation show a wide range of sensitivity to GSK1120212 with IC50 of 2.2-174 nM. In contrast, COLO320 DM cells, bearing the wild-type gene in both B-Raf and K-Ras, are found to be resistant to GSK1120212 even at 10 μM. GSK1120212 treatment for 24 hours induces cell-cycle arrest at the G1 phase in all sensitive cell lines. Consistently, GSK1120212 treatment leads to upregulation of p15INK4b and/or p27KIP1 in most of the colorectal cancer cell lines. GSK1120212 inhibits constitutive ERK phosphorylation in all sensitive cell lines. GSK1120212 induces apoptosis both in HT-29 and COLO205 cells, but that COLO205 cells are more sensitive to GSK1120212 than HT-29 cells in terms of apoptosis induction.GSK1120212 blocks tumor necrosis factor-α and interleukin-6 production from peripheral blood mononuclear cells (PBMCs).

    体内研究

    Oral administration of GSK1120212 at 0.3 mg/kg or 1 mg/kg once daily for 14 days is effective in inhibiting the HT-29 xenograft growth, and 1 mg/kg of GSK1120212 almost completely blocks the tumor increase. The phosphorylation of ERK1/2 is completely inhibited in the established tumor tissues by single oral dose of 1 mg/kg GSK1120212, and both p15INK4b and p27KIP1 protein levels are upregulated after 14 days of treatment with GSK1120212. In the COLO205 xenograft model, tumor regression is observed even at a dose of 0.3 mg/kg. At a dose of 1 mg/kg, a complete regression is obtained in 4 out of 6 mice in which the tumor degenerates to the point that tumor volume is not measurable.Administration of GSK1120212 at 0.1 mg/kg almost completely suppresses adjuvant-induced arthritis (AIA) and type II collagen-induced arthritis (CIA) in Lewis rats or DBA1/J mice, respectively.

    溶解性

    DMSO 100 mg/mL heat,水 <1 mg/mL,乙醇 <1 mg/mL

    稳定性

    2 -20°C粉状,6-80°C溶于DMSO

    特征

    More potent than PD0325901 or AZD6244

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    http://www.meilune.com/article.php?id=374

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