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Tomivosertib

Tomivosertib
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Purity:99.67%
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Tomivosertib

Catalog No. T3468Cas No. 1849590-01-7
Tomivosertib (eFT508) is a potent, highly selective MNK1 and MNK2 inhibitor with IC50 value of 1-2 nM.
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Pack SizePrice/USDAvailabilityQuantity
1 mg$59In Stock
5 mg$172In Stock
10 mg$255In Stock
25 mg$478In Stock
50 mg$691In Stock
100 mg$983In Stock
1 mL x 10 mM (in DMSO)$189In Stock
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Product Introduction

Bioactivity
Description
Tomivosertib (eFT508) is a potent, highly selective MNK1 and MNK2 inhibitor with IC50 value of 1-2 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[1].
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[1].
Cell Research
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)
AliaseFT508
Chemical Properties
Molecular Weight340.38
FormulaC17H20N6O2
Cas No.1849590-01-7
Storage & Solubility Information
Storagekeep away from direct sunlight Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Solubility Information
H2O: <1 mg/mL
DMSO: 11 mg/mL (32.3 mM)
Ethanol: <1 mg/mL
Solution Preparation Table
DMSO
1mg5mg10mg50mg
50 mM0.0588 mL0.2938 mL0.5876 mL2.9379 mL
100 mM0.0294 mL0.1469 mL0.2938 mL1.4689 mL

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Preparation method for in vivo formula: Take 50 μLDMSOTargetMol | reagent main solution, add 300 μLPEG300TargetMol | reagent mix well and clarify, then add 50 more μLTween 80, mix well and clarify, then add 600 more μLddH2OTargetMol | reagent mix well and clarify.
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