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S80364

GDC-0994

源叶(MedMol) 98%
  • 英文名:
  • GDC-0994
  • 别名:
  • ERK抑制剂;GDC0994; (S)-1-(1-(4-chloro-3-fluorophenyl)-2-hydroxyethyl)-4-(2-((1-methyl-1H-pyrazol-5-yl)amino)pyrimidin-4-yl)pyridin-2(1H)-one;
  • CAS号:
  • 1453848-26-4
  • 分子式:
  • C21H18ClFN6O2
  • 分子量:
  • 440.858
  • 核磁/质谱:
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源叶(MedMol) S80364-5mg 98% ¥640.00元 预计交期:2-3天 - - - EA 加入购物车
源叶(MedMol) S80364-10mg 98% ¥1200.00元 预计交期:2-3天 - - - EA 加入购物车
源叶(MedMol) S80364-25mg 98% ¥2560.00元 2 - - - EA 加入购物车
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参考文献

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  • 提示:详情请下载说明书。
  • 产品描述: Ravoxertinib (GDC-0994) is an orally active ERK kinase inhibitor with an IC50 of 6.1 nM and 3.1 nM for ERK1 and ERK2, respectively
  • 靶点: ERK1:6.1 nM (IC50);ERK2:3.1 nM (IC50);p-RSK:12 nM (IC50);ERK
  • 体外研究:
    Ravoxertinib (GDC-0994) also inhibits p90RSK with an IC50 of 12 nM. Ravoxertinib (GDC-0994) is highly selective for ERK1 and ERK2, with biochemical potency of 1.1 nM and 0.3 nM, respectively. Ravoxertinib (GDC0994; 50 nM, 0.5 µM, and 5 µM; 48 hours) decreases the viability of lung adenocarcinoma cell lines (A549, HCC827, HCC4006)
  • 体内研究:
    In CD-1 mice, a 10 mg/kg oral dose of Ravoxertinib (GDC-0994) is sufficient to achieve the desired target coverage for at least 8 h. Daily, oral dosing of Ravoxertinib results in significant single-agent activity in multiple in vivo cancer models, including KRAS-mutant and BRAF-mutant human xenograft tumors in mice
  • 参考文献:
    1. Blake JF, et al. Discovery of (S)-1-(1-(4-Chloro-3-fluorophenyl)-2-hydroxyethyl)-4-(2-((1-methyl-1H-pyrazol-5-yl)amino)pyrimidin-4-yl)pyridin-2(1H)-one (GDC-0994), an Extracellular Signal-Regulated Kinase 1/2 (ERK1/2) Inhibitor in Early Clinical Developmement. J Med Chem. 2016 Jun 23;59(12):5650 2. Kirk Robarge, et al. Abstract DDT02-03: Discovery of GDC-0994, a potent and selective ERK1/2 inhibitor in early clinical development. Proceedings: AACR Annual Meeting 2014; April 5-9, 2014. 3. MICHAEL LAI. Opportunity for Pharmaceutical Intervention in Lung Cancer: Selective Inhibition of JAK1/2 to Eliminate EMT-Derived Mesenchymal Cells.
  • 溶解性: soluble  in  DMSO
  • 保存条件: -20℃
  • 配置溶液浓度参考:
    1mg 5mg 10mg
    1 mM 2.268 ml 11.342 ml 22.683 ml
    5 mM 0.454 ml 2.268 ml 4.537 ml
    10 mM 0.227 ml 1.134 ml 2.268 ml
    50 mM 0.045 ml 0.227 ml 0.454 ml
  • 注意:部分产品我司仅能提供部分信息,我司不保证所提供信息的权威性,仅供客户参考交流研究之用。
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质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)


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