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eFT508 99%

eFT508

源葉(MedMol)
S81408
1849590-01-7
C17H20N6O2
340.3797
品牌 貨號 產品規格 價格(RMB) 庫存(上海) 北京 武漢 南京 購買數量
源葉(MedMol) S81408-1mg 99% ¥400.00元 9 - - -
源葉(MedMol) S81408-2mg 99% ¥700.00元 8 - - -
源葉(MedMol) S81408-5mg 99% ¥1200.00元 8 - - -
源葉(MedMol) S81408-10mg 99% ¥2050.00元 6 - - -
源葉(MedMol) S81408-25mg 99% ¥2700.00元 6 - - -
源葉(MedMol) S81408-50mg 99% ¥4600.00元 預計交期:2-3天 - - -
源葉(MedMol) S81408-100mg 99% ¥6400.00元 預計交期:2-3天 - - -
產品介紹 參考文獻 質檢證書(COA) 摩爾濃度計算器 相關產品

產品介紹

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
產品描述: 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
靶點: MNK1:1-2 nM (IC50);MNK2:1-2 nM (IC50);PD-L1;MNK;?PD-1/PD-L1
體外研究:
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
體內研究:
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
參考文獻:
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
保存條件: -20℃
配置溶液濃度參考:
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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參考文獻

質檢證書(COA)

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批號:C10000001 貨號:A800001-25g
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摩爾濃度計算器

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