keep away from direct sunlight
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Tomivosertib (eFT508) is a potent, highly selective MNK1 and MNK2 inhibitor with IC50 value of 1-2 nM.
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
1 mg | In stock | $ 59.00 | |
5 mg | In stock | $ 172.00 | |
10 mg | In stock | $ 255.00 | |
25 mg | In stock | $ 478.00 | |
50 mg | In stock | $ 691.00 | |
100 mg | In stock | $ 983.00 | |
1 mL * 10 mM (in DMSO) | In stock | $ 189.00 |
Description | Tomivosertib (eFT508) is a potent, highly selective MNK1 and MNK2 inhibitor with IC50 value of 1-2 nM. |
Targets&IC50 | MNK1:1-2 nM, MNK2:1-2 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) |
Synonyms | eFT508 |
Molecular Weight | 340.38 |
Formula | C17H20N6O2 |
CAS No. | 1849590-01-7 |
keep away from direct sunlight
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
H2O: <1 mg/mL
DMSO: 11 mg/mL (32.3 mM)
Ethanol: <1 mg/mL
You can also refer to dose conversion for different animals. More
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Tomivosertib 1849590-01-7 Apoptosis Cell Cycle/Checkpoint Immunology/Inflammation MAPK PD-1/PD-L1 MNK Inhibitor MAP kinase interacting kinase Mitogen activated protein kinase interacting kinase MAPK interacting kinase eFT 508 eFT-508 eFT508 inhibit inhibitor