ETC-206
(Synonyms: 4-[6-[4-(4-吗啉基羰基)苯基]咪唑并[1,2-A]吡啶-3-基]苄腈) 目录号 : GC33033
An inhibitor of MKNK1 and MKNK2
Cas No.:1464151-33-4
Sample solution is provided at 25 µL, 10mM.
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ETC-206 is an inhibitor of MAPK-interacting serine/threonine kinase 1 (MKNK1) and MKNK2 (IC50s = 0.064 and 0.086 ?M, respectively).1 It is selective for MKNK1 and MKNK2 over a panel of 104 kinases at 1 ?M. ETC-206 inhibits phosphorylation of eukaryotic translation initiation factor 4E (eIF4E) in HeLa cells (IC50 = 0.321 ?M). In vivo, ETC-206 enhances tumor growth inhibition induced by dasatinib in a K562 mouse xenograft model. It also prevents weight gain in a mouse model of high-fat diet-induced obesity when administered at a dose of 100 mg/kg.2
1.Yang, H., Chennamaneni, L.R., Ho, M.W.T., et al.Optimization of selective mitogen-activated protein kinase interacting kinases 1 and 2 inhibitors for the treatment of blast crisis leukemiaJ. Med. Chem.61(10)4348-4369(2018) 2.Sandeman, L.Y., Kang, W.X., Wang, X., et al.Disabling MNK protein kinases promotes oxidative metabolism and protects against diet-induced obesityMol. Metab.42101054(2020)
Cell experiment: | 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). The IC50s are in general in the micromolar range[1]. |
Animal experiment: | Mice[1]CD-1 female mice (6-8 weeks old) are weighed, and those selected for dosing are 24±2 g. Three mice are randomly grouped per time point. Mice are administered a single dose of 1 mg/kg of ETC-206 via tail vein injection or a single dose of 5 mg/kg of ETC-206 via oral gavage. The volume of injection for intravenous (i.v.) and oral (p.o.) administration is 4 mL/kg and 8 mL/kg, respectively[1]. |
References: [1]. Yang H, et al. Optimization of Selective Mitogen-Activated Protein Kinase Interacting Kinases 1 and 2 Inhibitors for the Treatment of Blast Crisis Leukemia. J Med Chem. 2018 May 24;61(10):4348-4369. | |
| Cas No. | 1464151-33-4 | SDF | |
| 别名 | 4-[6-[4-(4-吗啉基羰基)苯基]咪唑并[1,2-A]吡啶-3-基]苄腈 | ||
| Canonical SMILES | N#CC1=CC=C(C2=CN=C3C=CC(C4=CC=C(C(N5CCOCC5)=O)C=C4)=CN32)C=C1 | ||
| 分子式 | C25H20N4O2 | 分子量 | 408.45 |
| 溶解度 | DMSO : ≥ 50 mg/mL (122.41 mM) | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.4483 mL | 12.2414 mL | 24.4828 mL |
| 5 mM | 0.4897 mL | 2.4483 mL | 4.8966 mL |
| 10 mM | 0.2448 mL | 1.2241 mL | 2.4483 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet