品牌	貨號	產品規格	價格(RMB)	庫存（上海）	北京	武漢	南京
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

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

注意：

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