• 咨询热线
    客服服务热线 13671568941/15317326293
  • 在线咨询
  • 微信客服
    微信客服
  • 公众号
    扫码关注公众号

GDC-0623

CAS No. 1168091-68-6

GDC-0623 ( GDC0623 | GDC-0632 | GDC 0632 | G868 | G 868 | G-868 )

产品货号. M17163 CAS No. 1168091-68-6

GDC-0623 是一种有效的 ATP 非竞争性 MEK1 抑制剂,Ki 为 0.13 nM。

纯度: >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
规格 价格/人民币 库存 数量
2MG ¥543 有现货
5MG ¥988 有现货
10MG ¥1596 有现货
25MG ¥2730 有现货
50MG ¥3823 有现货
100MG ¥5484 有现货
200MG 获取报价 有现货
500MG 获取报价 有现货
1G 获取报价 有现货

生物学信息

  • 产品名称
    GDC-0623
  • 注意事项
    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
  • 产品简述
    GDC-0623 是一种有效的 ATP 非竞争性 MEK1 抑制剂,Ki 为 0.13 nM。
  • 产品描述
    GDC-0623, also known as G-868, is an orally active, selective MEK inhibitor with potential antineoplastic activity. MEK inhibitor GDC-0623 specifically inhibits mitogen-activated protein kinase kinase (MEK or MAP/ERK kinase), resulting in inhibition of growth factor-mediated cell signaling and tumor cell proliferation. MEK is a key component of the RAS/RAF/MEK/ERK signaling pathway that regulates cell growth; constitutive activation of this pathway has been implicated in many cancers. Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus).(In Vitro):GDC-0623 (RG 7421) and G-573 are able to prevent MEK phosphorylation by CRAF in vitro, and able to block MEK phosphorylation by BRAF(V600E). GDC-0623 (RG 7421) is potent, ATP-uncompetitive inhibitors of MEK1 but shows distinct shifts in cellular activity compared with the other two inhibitors, only 6-fold half-maximum effective concentration (EC50) decreases.(In Vivo):GDC-0623 (RG 7421) (40 mg/kg, p.o.) shows percent tumour growth inhibition (%TGI) in MiaPaCa-2 xenograft model. GDC-0623 (RG 7421) and G-573 show superior antitumour activity compared to GDC-0623 (RG 7421) in all three KRAS models.
  • 体外实验
    GDC-0623 (RG 7421) and G-573 are able to prevent MEK phosphorylation by CRAF in vitro, and able to block MEK phosphorylation by BRAF(V600E). GDC-0623 (RG 7421) is potent, ATP-uncompetitive inhibitors of MEK1 but shows distinct shifts in cellular activity compared with the other two inhibitors, only 6-fold half-maximum effective concentration (EC50) decreases.
  • 体内实验
    GDC-0623 (RG 7421) (40 mg/kg, p.o.) shows percent tumour growth inhibition (%TGI) in MiaPaCa-2 xenograft model. GDC-0623 (RG 7421) and G-573 show superior antitumour activity compared to GDC-0623 (RG 7421) in all three KRAS models.
  • 同义词
    GDC0623 | GDC-0632 | GDC 0632 | G868 | G 868 | G-868
  • 通路
    Others
  • 靶点
    Other Targets
  • 受体
    MEK1
  • 研究领域
    Cancer
  • 适应症
    ——

化学信息

  • CAS Number
    1168091-68-6
  • 分子量
    456.21
  • 分子式
    C16H14FIN4O3
  • 纯度
    >98% (HPLC)
  • 溶解度
    DMSO : ≥ 30 mg/mL. 65.76 mM
  • SMILES
    OCCONC(=O)C1=C(NC2=C(F)C=C(I)C=C2)N2C=NC=C2C=C1
  • 化学全称
    5-((2-fluoro-4-iodophenyl)amino)-N-(2-hydroxyethoxy)imidazo[1,5-a]pyridine-6-carboxamide

运输与储存

  • 储存条件
    (-20℃)
  • 运输条件
    With Ice Pack
  • 稳定性
    ≥ 2 years

参考文献

产品手册
关联产品
  • ADWX 1

    Potent and selective KV1.3 channel blocker (IC50 values are 0.0019 and 0.65 nM for KV1.3 and KV1.1, respectively). Inhibits CD4+ CCR7- T cell activation. Ameliorates rat experimental autoimmune encephalomyelitis, in a model for multiple sclerosis.

  • m-PEG2-Br

    m-PEG2-Br 是一种基于 PEG 的 PROTAC 连接子,可用于 PROTAC 的合成。

  • 1,3-BUTANEDIOL

    1,3-丁二醇(BD)是一种生酮物质。在缺乏外源营养素的情况下,酮体是必需的能量底物,最近也是如此。