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Tomivosertib
Tomivosertib (eFT508) is a potent and highly selective MNK1 and MNK2 inhibitor with an IC50 value of 1-2 nM.
Catalog No. T3468Cas No. 1849590-01-7
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Purity:99.67%
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Tomivosertib
Catalog No. T3468Cas No. 1849590-01-7
Tomivosertib (eFT508) is a potent and highly selective MNK1 and MNK2 inhibitor with an IC50 value of 1-2 nM.
All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose. | Pack Size | Price | Availability | Quantity |
|---|---|---|---|
| 1 mg | $59 | In Stock | |
| 5 mg | $172 | In Stock | |
| 10 mg | $255 | In Stock | |
| 25 mg | $478 | In Stock | |
| 50 mg | $691 | In Stock | |
| 100 mg | $983 | In Stock | |
| 1 mL x 10 mM (in DMSO) | $189 | In Stock |
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Product Introduction
Bioactivity
Chemical Properties
Storage & Solubility Information
| Description | Tomivosertib (eFT508) is a potent and highly selective MNK1 and MNK2 inhibitor with an IC50 value of 1-2 nM. |
| Targets&IC50 | MNK1:1-2 nM, MNK2:1-2 nM |
| In vitro | Tomivosertib 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 Tomivosertib leads to a dose-dependent reduction in eIF4E phosphorylation at serine 209 (IC50 = 2-16 nM). In a panel of ~50 hematological cancers, Tomivosertib shows anti-proliferative activity against multiple DLBCL cell lines. Sensitivity to Tomivosertib 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) |
| Alias | eFT508 |
| Molecular Weight | 340.38 |
| Formula | C17H20N6O2 |
| Cas No. | 1849590-01-7 |
| Storage | keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||
| Solubility Information | H2O: <1 mg/mL DMSO: 11 mg/mL (32.3 mM) Ethanol: <1 mg/mL | |||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||
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Please enter your animal experiment information in the following box and click Calculate to obtain the mother liquor preparation method and in vivo formula preparation method:
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(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.Preparation method for in vivo formula: Take 50 μL DMSO main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarify
main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarifyFor Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
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