Powder: -20°C for 3 years
In solvent: -80°C for 2 years
eFT508 is a potent, highly selective <a href="/target/MNK" style="display: inline; color: #c13a36">MNK</a>1 and <a href="/target/MNK" style="display: inline; color: #c13a36">MNK</a>2 inhibitor with IC50 value of 1-2 nM.
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
1 mg | In stock | $ 73.00 | |
5 mg | In stock | $ 194.00 | |
10 mg | In stock | $ 284.00 | |
25 mg | In stock | $ 499.00 | |
50 mg | In stock | $ 858.00 | |
100 mg | In stock | $ 1,219.00 | |
1 mL * 10 mM (in DMSO) | In stock | $ 212.00 |
Description | 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 | 340.387 |
Formula | C17H20N6O2 |
CAS No. | 1849590-01-7 |
Powder: -20°C for 3 years
In solvent: -80°C for 2 years
H2O: <1 mg/mL
DMSO: 11 mg/mL (32.3 mM)
Ethanol: <1 mg/mL
( < 1 mg/ml refers to the product slightly soluble or insoluble )
You can also refer to dose conversion for different animals. More
bottom
Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.
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 eFT508 eFT 508 inhibit inhibitor