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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Tomivosertib (eFT-508)
CAS number：1849590-01-7 molecular formula：C17H20N6O2
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| Chinese alias | - | ||
| English alias | (R)-Pulegone - 90% | 1849590-01-7 | UNII-U2H19X4WBV | 6'-[(6-aminopyrimidin-4-yl)amino]-8'-methyl-2'H-spiro[cyclohexane-1,3'-imidazo[1,5-a]pyridine]-1',5'-dione | HY-100022 | Z2740419312 | 6'-((6-AMINOPYRIMIDIN-4-YL)AMINO)-8'-METHYL-2'HSPIRO(CYCLOHEXANE-1 | ||
| CAS number | 1849590-01-7 | molecular formula | C17H20N6O2 |
| molecular weight | 340.38 g/mol | Exact mass | - |
| PSA | 113.000 Ų | logp | 1.3 |
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