Tomivosertib (eFT-508)
For research use only. Not for use in humans.
Catalog No.S8275
Molecular Weight(MW): 340.38
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.
Purity & Quality Control
Choose Selective MNK Inhibitors
Biological Activity
| Description | 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. | |||||||||||||||||||||||||||||||||||||
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| 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]. |
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| Cell Data |
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| Assay |
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| 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]. |
Protocol
| Cell Research: |
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Solubility (25°C)
| In vitro | DMSO | 13 mg/mL (38.19 mM) |
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| Water | Insoluble | |
| Ethanol | Insoluble |
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Chemical Information
| Molecular Weight | 340.38 |
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| Formula | C17H20N6O2 |
| CAS No. | 1849590-01-7 |
| Storage | powder |
| in solvent | |
| Synonyms | N/A |
| Smiles | CC1=C2N(C(=O)C(=C1)NC3=NC=NC(=C3)N)C4(CCCCC4)NC2=O |
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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.
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