tomivosertib eFT508

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Chemical Information

Product name：tomivosertib eFT508	Purity：98% min
CAS NO：1849590-01-7	Solubility：Soluble in DMSO
Molecular Formula：C₁₇H₂₀N₆O₂	Package：Package according to customer requirements
Molecular Weight：340.38	Storage：Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

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Remarks

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.

References

[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;