A 484954
目录号 : GC12739
An eEF-2K inhibitor
Cas No.:142557-61-7
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
A 484954 is a selective inhibitor of eEF2K with IC50 value of 0.28 μM [1].
Eukaryotic elongation factor-2 kinase (eEF2K) is a calcium/calmodulin-dependent protein kinase and regulates protein synthesis. It phosphorylates eEF2 and inhibits the activity of eEF2 [1].
A 484954 is a selective eEF2K inhibitor. A 484954 inhibited eEF2K and the phosphorylation of eEF2. While, it didn’t inhibit cancer cell growth. In enzymatic assay, the IC50 value of A-484954 was increased in an ATP-dependent way but not affected by the concentrations of calmodulin. In H1299 cells, A 484954 inhibited the phosphorylation of eEF2 but didn’t affect the protein level of eEF2. In PC3 cells, A 484954 (10 μM) inhibited peEF2 by 50% and the inhibition reached the maximum level at 100 μM. While A 484954 didn’t inhibit cell proliferation. In PC3 cells, NH125 induced eEF2 phosphorylation, while A 484954 had little effect on peEF2 induced by NH125 [1].
Reference:
[1]. Chen Z, Gopalakrishnan SM, Bui MH, et al. 1-Benzyl-3-cetyl-2-methylimidazolium iodide (NH125) induces phosphorylation of eukaryotic elongation factor-2 (eEF2): a cautionary note on the anticancer mechanism of an eEF2 kinase inhibitor. J Biol Chem, 2011, 286(51): 43951-43958.
| Cas No. | 142557-61-7 | SDF | |
| 化学名 | 7-amino-1-cyclopropyl-3-ethyl-2,4-dioxo-1,2,3,4-tetrahydropyrido[2,3-d]pyrimidine-6-carboxamide | ||
| Canonical SMILES | O=C(N(CC)C1=O)N(C2=NC(N)=C(C(N)=O)C=C21)C3CC3 | ||
| 分子式 | C13H15N5O3 | 分子量 | 289.29 |
| 溶解度 | <2.89mg/ml in DMSO | 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 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 3.4567 mL | 17.2837 mL | 34.5674 mL |
| 5 mM | 0.6913 mL | 3.4567 mL | 6.9135 mL |
| 10 mM | 0.3457 mL | 1.7284 mL | 3.4567 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。