Tomivosertib,1849590-01-7

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Tomivosertib

CAS No. : 1849590-01-7

MCE 国际站：Tomivosertib

产品活性：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。

研究领域：MAPK/ERK Pathway  |  Immunology/Inflammation

作用靶点：MNK  |  PD-1/PD-L1

In Vitro: 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.

In Vivo: 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.

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