中文名：Tomivosertib (eFT-508)
英文名：Tomivosertib (eFT-508)
纯度：Moligand™，≥97%
货号：T413958
Cas号：1849590-01-7
存储温度：-20°C储存
运输条件：超低温运输
产品介绍：
Information
Tomivosertib (eFT-508) Tomivosertib (eFT-508) is a potent and selective MNK1/2 inhibitor with IC50s of 2.4 nM and 1 nM, respectively. It potentially results in decreased tumor cell proliferation and tumor growth. Tomivosertib (eFT-508) inhibits eIF4E phosphorylation and dramatically downregulates PD-L1 protein abundance.
Targets
MNK2 (Cell-free assay); MNK1 (Cell-free assay) 1 nM; 2.4 nM
In vitro
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.
In vivo
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.
Cell Research(from reference)
Cell lines：TMD8 cells
Concentrations：0.01, 0.1, 1, 3, 10 μM
Incubation Time：24 h
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关键字： 6'-[(6-氨基-4-嘧啶基)氨基]-8'-甲基螺[环己烷-1,3'(2'H)-咪唑并[1,5-a]吡啶]-1',5'-二酮 ; 托米沃塞替尼 (eFT-508);(R)-Pulegone - 90% ; 1849590-01-7
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