keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Tomivosertib (eFT508) 是一种具有口服活性的MNK1和MNK2高选择性抑制剂,IC50值均为 1-2 nM。它可降低肿瘤细胞中eIF4E 的磷酸化水平 (位点为 Ser209,IC50=2-16 nM),下调PD-L1蛋白的平均含量。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 479 | 现货 | ||
5 mg | ¥ 1,490 | 现货 | ||
10 mg | ¥ 2,320 | 现货 | ||
25 mg | ¥ 3,930 | 现货 | ||
50 mg | ¥ 5,620 | 现货 | ||
100 mg | ¥ 7,850 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 1,630 | 现货 |
产品描述 | Tomivosertib (eFT508) is a potent, highly selective MNK1 and MNK2 inhibitor with IC50 value of 1-2 nM. |
靶点活性 | MNK1:1-2 nM, MNK2:1-2 nM |
体外活性 | 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]. |
体内活性 | 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]. |
细胞实验 | 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) |
别名 | 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
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.9379 mL | 14.6895 mL | 29.3789 mL | 73.4473 mL |
5 mM | 0.5876 mL | 2.9379 mL | 5.8758 mL | 14.6895 mL | |
10 mM | 0.2938 mL | 1.4689 mL | 2.9379 mL | 7.3447 mL | |
20 mM | 0.1469 mL | 0.7345 mL | 1.4689 mL | 3.6724 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
Tomivosertib 1849590-01-7 Apoptosis Cell Cycle/Checkpoint Immunology/Inflammation MAPK MNK PD-1/PD-L1 Inhibitor MAP kinase interacting kinase Mitogen activated protein kinase interacting kinase MAPK interacting kinase eFT 508 eFT-508 eFT508 inhibit inhibitor