化合物eFT508 T3468

Product Introduction
Bioactivity


英文名: Tomivosertib

描述: Tomivosertib (eFT508) 是一种具有口服活性的MNK1和MNK2高选择性抑制剂，IC50值均为 1-2 nM。它可降低肿瘤细胞中eIF4E 的磷酸化水平 (位点为 Ser209，IC50=2-16 nM)，下调PD-L1蛋白的平均含量。

细胞实验: TMD8 cells are treated with the indicated concentrations of eFT508 for 24 h. Cell lysates are subjected to m7-GTP Sepharose pull-down and bound proteins are analyzed by immunoblotting with the indicated antibodies. (Only for Reference)

体外活性: eFT508 has a half-maximal inhibitory concentration (IC50) of 1-2 nM against both MNK isoforms in enzyme assays and inhibits the kinase through a reversible, ATP-competitive mechanism of action. Treatment of tumor cell lines with eFT508 leads to a dose-dependent reduction in eIF4E phosphorylation at serine 209 (IC50 = 2-16 nM). In a panel of ~50 hematological cancers, eFT508 shows anti-proliferative activity against multiple DLBCL cell lines. Sensitivity to eFT508 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[1].

体内活性: eFT508 is well-tolerated and shows efficacy against MyD88-mutant DLBCL models in vivo. Significant anti-tumor activity of eFT508 is observed in the TMD8 and HBL-1 ABC-DLBCL models(subcutaneous human lymphoma xenograft models), both of which harbor activating MyD88 mutations[1].

存储条件: keep away from direct sunlightPowder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: H2O : <1 mg/mL
DMSO : 11 mg/mL (32.3 mM)
Ethanol : <1 mg/mL


关键字: Inhibitor | MAP kinase interacting kinase | MNK | Mitogen activated protein kinase interacting kinase | MAPK interacting kinase | eFT 508 | eFT-508 | Tomivosertib | inhibit

相关产品: DS12881479 | CGP 57380 | QL-X-138 | QL-X-138 HCl | AZ7550 | ETC-206 | SLV-2436 | MK2-IN-3 hydrate | EB1

相关库: Drug Repurposing Compound Library | Anti-Cancer Drug Library | Immuno-Oncology Compound Library | Anti-Lung Cancer Compound Library | Anti-Ovarian Cancer Compound Library | Anti-Cancer Clinical Compound Library | Kinase Inhibitor Library | Highly Selective Inhibitor Library | Anti-Cancer Active Compound Library | Apoptosis Compound Library

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