TCS PIM-1 1
(Synonyms: SC 204330) 目录号 : GC17178
A Pim-1 kinase inhibitor
Cas No.:491871-58-0
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
TCS PIM-1 1 is a selective inhibitor of Pim-1 with IC50 value of 50 nM [1].
Pim-1 is a proto-oncogene serine/threonine-protein kinase and plays an important role in cell cycle progression, apoptosis, transcriptional activation and more general signal transduction pathways. It has been shown that Pim-1 over-expression is correlated with a variety of human cancers [2].
TCS PIM-1 1 is a potent Pim-1 inhibitor and has a better selectivity to Pim-1 than to Pim-2. It was revealed that TCS PIM-1 1 was the most potent inhibitor of Pim-1 by outlining the crystal structure and it was also shown that TCS PIM-1 1 had better inhibitory activity to Pim-1 compared with Pim-2 [1].
References:
[1]. Cheney, I.W., et al., Identification and structure-activity relationships of substituted pyridones as inhibitors of Pim-1 kinase. Bioorg Med Chem Lett, 2007. 17(6): p. 1679-83.
[2]. Cen, B., et al., The Pim-1 protein kinase is an important regulator of MET receptor tyrosine kinase levels and signaling. Mol Cell Biol, 2014. 34(13): p. 2517-32.
| Cas No. | 491871-58-0 | SDF | |
| 别名 | SC 204330 | ||
| 化学名 | 6-(5-bromo-2-hydroxyphenyl)-2-oxo-4-phenyl-1,2-dihydropyridine-3-carbonitrile | ||
| Canonical SMILES | O=C1C(C#N)=C(C2=CC=CC=C2)C=C(C3=C(O)C=CC(Br)=C3)N1 | ||
| 分子式 | C18H11BrN2O2 | 分子量 | 367.2 |
| 溶解度 | ≥ 12.8mg/mL in DMSO | 储存条件 | Store at 4°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 | 2.7233 mL | 13.6166 mL | 27.2331 mL |
| 5 mM | 0.5447 mL | 2.7233 mL | 5.4466 mL |
| 10 mM | 0.2723 mL | 1.3617 mL | 2.7233 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。