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S81408

eFT508

源叶(MedMol) 99%
  • 英文名:
  • eFT508
  • 别名:
  • CAS号:
  • 1849590-01-7
  • 分子式:
  • C17H20N6O2
  • 分子量:
  • 340.3797
  • 核磁/质谱:
品牌货号产品规格价格(RMB) 库存(上海) 北京 武汉 南京 数量计量单位 加入购物车...
源叶(MedMol) S81408-1mg 99% ¥510.00元 9 - - - EA 加入购物车
源叶(MedMol) S81408-2mg 99% ¥807.50元 8 - - - EA 加入购物车
源叶(MedMol) S81408-5mg 99% ¥1440.00元 8 - - - EA 加入购物车
源叶(MedMol) S81408-10mg 99% ¥2050.00元 6 - - - EA 加入购物车
源叶(MedMol) S81408-25mg 99% ¥3050.00元 6 - - - EA 加入购物车
源叶(MedMol) S81408-50mg 99% ¥5100.00元 预计交期:2-3天 - - - EA 加入购物车
源叶(MedMol) S81408-100mg 99% ¥7200.00元 预计交期:2-3天 - - - EA 加入购物车
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参考文献

质检证书(COA)

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  • 提示:详情请下载说明书。
  • 产品描述: Tomivosertib (eFT508) is a potent, highly selective, and orally active MNK1 and MNK2 inhibitor, with IC50s of 1-2 nM against both isoforms. Tomivosertib (eFT508) treatment leads to a dose-dependent reduction in eIF4E phosphorylation at serine 209 (IC50=2-16 nM) in tumor cell lines. Tomivosertib (eFT508) also dramatically downregulates PD-L1 protein abundance
  • 靶点: MNK1:1-2 nM (IC50);MNK2:1-2 nM (IC50);PD-L1;MNK; PD-1/PD-L1
  • 体外研究:
    Tomivosertib (eFT508) reduces eIF4E phosphorylation dose-dependently at serine 209 (IC50=2-16 nM) in tumor cell lines. In a panel of appr 50 hematological cancers, Tomivosertib shows anti-proliferative activity against multiple DLBCL cell lines. Sensitivity to Tomivosertib in TMD8, OCI-Ly3 and HBL1 DLBCL cell lines is associated with dose-dependent decreases in production of pro-inflammatory cytokines including TNFα, IL-6, IL-10 and CXCL10. Further evaluation Tomivosertib mechanism of action demonstrates that decreased TNFα production correlates with a 2-fold decrease in TNFα mRNA half-life
  • 体内研究:
    Tomivosertib (eFT508) shows significant anti-tumor activity in the TMD8 and HBL-1 ABC-DLBCL models, both of which harbor activating MyD88 mutations. Besides, Tomivosertib combines effectively with components of R-CHOP and with novel targeted agents, including PCI-32765 and Venetoclax, in human lymphoma models
  • 参考文献:
    1. Kevin R. Webster, et al. eFT508, a Potent and Selective Mitogen-Activated Protein Kinase Interacting Kinase (MNK) 1 and 2 Inhibitor, Is Efficacious in Preclinical Models of Diffuse Large B-Cell Lymphoma (DLBCL). Blood 2015 126:1554. 2. Xu Y, et al. Translation control of the immune checkpoint in cancer and its therapeutic targeting. Nat Med. 2019 Feb;25(2):301-311.
  • 溶解性: soluble  in  DMSO
  • 保存条件: -20℃
  • 配置溶液浓度参考:
    1mg 5mg 10mg
    1 mM 2.938 ml 14.689 ml 29.379 ml
    5 mM 0.588 ml 2.938 ml 5.876 ml
    10 mM 0.294 ml 1.469 ml 2.938 ml
    50 mM 0.059 ml 0.294 ml 0.588 ml
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