| 货号 | 规格 | 价格 | 上海 | 北京 | 珠海 | 重庆 | 武汉 | 购买数量 |
|---|---|---|---|---|---|---|---|---|
S81408-1mg买3赠1 |
99.00% | ￥400.00 |
8 | - | - | - | - |
|
S81408-2mg买3赠1 |
99.00% | ￥700.00 |
8 | - | - | - | - |
|
S81408-5mg促销 |
99.00% | ￥1200.00 ￥960.00 |
7 | - | - | - | - |
|
S81408-10mg促销 |
99.00% | ￥2050.00 ￥1640.00 |
6 | - | - | - | - |
|
S81408-25mg促销 |
99.00% | ￥2700.00 ￥2160.00 |
6 | - | - | - | - |
|
S81408-50mg促销 |
≥99% | ￥4600.00 ￥3680.00 |
货期：2-3天 | - | - | - | - |
|
S81408-100mg促销 |
≥99% | ￥6400.00 ￥5120.00 |
货期：2-3天 | - | - | - | - |
|
| 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 | ||||||||||||||||||||
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| 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： |
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| 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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