Tomivosertib (eFT508) 是一种有效的，高度选择性的，口服活性的 MNK1 和 MNK2 抑制剂，IC₅₀ 值均为 1-2 nM。Tomivosertib (eFT508) 处理可降低肿瘤细胞中 eIF4E 的磷酸化水平 (位点为 Ser209，IC₅₀=2-16 nM)。Tomivosertib (eFT508) 还显著下调 PD-L1 蛋白的丰度。

Tomivosertib (eFT508) is a potent, highly selective, and orally active MNK1 and MNK2 inhibitor, with IC 50 s of 1-2 nM against both isoforms. Tomivosertib (eFT508) treatment leads to a dose-dependent reduction in eIF4E phosphorylation at serine 209 (IC 50 =2-16 nM) in tumor cell lines. Tomivosertib (eFT508) also dramatically downregulates PD-L1 protein abundance.

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MNK1 1-2 nM (IC50) MNK2 1-2 nM (IC50

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. has not independently confirmed the accuracy of these methods. They are for reference only.

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. has not independently confirmed the accuracy of these methods. They are for reference only.

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[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.

In Vitro: DMSO : 4.35 mg/mL (12.78 mM; Need ultrasonic)配制储备液