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.
パッケージサイズ | 在庫状況 | 単価(税別) | |||
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1 mg | 在庫あり | ¥ 13,500 | |||
5 mg | 在庫あり | ¥ 39,500 | |||
10 mg | 在庫あり | ¥ 58,500 | |||
25 mg | 在庫あり | ¥ 110,000 | |||
50 mg | 在庫あり | ¥ 158,500 | |||
100 mg | 在庫あり | ¥ 225,500 | |||
1 mL * 10 mM (in DMSO) | 在庫あり | ¥ 43,500 |
説明 | Tomivosertib (eFT508) is a potent, highly selective MNK1 and MNK2 inhibitor with IC50 value of 1-2 nM. |
ターゲット&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]. |
細胞研究 | 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) |
別名 | eFT508 |
分子量 | 340.38 |
分子式 | 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. 詳細
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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 eFT-508 eFT508 inhibit inhibitor