Powder: -20°C for 3 years | In solvent: -80°C for 1 year
ETC-206 是选择性 MNK1和 MNK2抑制剂,IC50分别为 64 和 86 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 638 | 现货 | ||
2 mg | ¥ 938 | 现货 | ||
5 mg | ¥ 1,530 | 现货 | ||
10 mg | ¥ 2,360 | 现货 | ||
25 mg | ¥ 3,930 | 现货 | ||
50 mg | ¥ 5,720 | 现货 | ||
100 mg | ¥ 7,970 | 现货 | ||
500 mg | ¥ 15,900 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 1,660 | 现货 |
产品描述 | ETC-206 is a selective inhibitor of MNK1 and MNK2 (IC50s: 64 nM and 86 nM). |
靶点活性 | MNK1:64 nM, MNK2:86 nM |
体外活性 | The anti-proliferative effects of ETC-206 are assessed in vitro, using CellTiter-Glo viability assay against 25 hematological cancer cell lines including the K562 cell line that overexpresses eIF4E (K562 o/e eIF4E). ETC-206 inhibits eIF4E phosphorylation in HeLa cell line (IC50: 321 nM). The IC50s are 1.71 μM, 3.36 μM, 3.70 μM, 4.81 μM, 5.13 μM, 5.05 μM, 6.70 μM, 9.76 μM, and 48.8 μM for SU-DHL-6, GK-5, MC 116, P3HR-1, DOHH2, MPC-11, Ramos.2G6.4C10, AHH-1, and K562 o/e eIF4E cells, respectively. |
体内活性 | The antitumor effect of ETC-206 is then assessed in a K562 e/o eIF4E mouse xenograft model after oral administration at 25, 50, or 100 mg/kg alone or in combination with a 2.5 mg/kg fixed-dose of Dasatinib throughout the study. ETC-206 with 2.5 mg/kg of Dasatinib not only increases tumor growth inhibition in a dose-dependent manner but, more importantly, leads to 2, 5, and 8 out of 8 tumor-free animals at 25, 50, and 100 mg/kg, respectively. The combination of ETC-206 and Dasatinib inhibits tumor growth at all tested doses, and no weight loss is recorded. Both the combination of ETC-206 and Dasatinib and, on the other hand, the dual MNK1/2 and BCR-ABL1 inhibitors prevent tumor growth in the same mouse xenograft model. ETC-206 alone only yields a maximum TGI of 23% at the highest administered dose of 100 mg/kg, which does not impede tumor growth, and is similar to the nontreated animals. ETC-206 has moderate terminal elimination half-life (t1/2=1.7 h, and 1.77 h for mouse (1 mg/kg, i.v.), mouse (5 mg/kg, p.o.)). |
分子量 | 408.45 |
分子式 | C25H20N4O2 |
CAS No. | 1464151-33-4 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 50 mg/mL (122.41 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.4483 mL | 12.2414 mL | 24.4828 mL | 61.207 mL |
5 mM | 0.4897 mL | 2.4483 mL | 4.8966 mL | 12.2414 mL | |
10 mM | 0.2448 mL | 1.2241 mL | 2.4483 mL | 6.1207 mL | |
20 mM | 0.1224 mL | 0.6121 mL | 1.2241 mL | 3.0604 mL | |
50 mM | 0.049 mL | 0.2448 mL | 0.4897 mL | 1.2241 mL | |
100 mM | 0.0245 mL | 0.1224 mL | 0.2448 mL | 0.6121 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。
ETC-206 1464151-33-4 MAPK MNK MAP kinase interacting kinase Inhibitor inhibit MAPK interacting kinase ETC 206 ETC206 Mitogen activated protein kinase interacting kinase inhibitor