Vacquinol-1
(Synonyms: NSC13316) 目录号 : GC17818
An activator of cell death in glioblastoma cells
Cas No.:5428-80-8
Sample solution is provided at 25 µL, 10mM.
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IC50: 3.14 μM for glioma cells
Vacquinol-1 is a MAPK kinase 4 (MKK4) activator.
Mitogen-activated protein kinase (MAPK) is a type of protein kinase that is specific to the amino acids serine, threonine, and tyrosine. MAPKs regulate cell functions such asgene expression, mitosis, proliferation, differentiation, cell survival, as well as apoptosis.
In vitro: Previous study showed that vacquinol-1 displayed high cytotoxicity against glioma cells, resulting in a complete loss of viability as measured by ATP depletion. Vacquinol-1 could selectively target GCs in mixed cocultures with human fibroblasts. Moreover, vacquinol-1 had no effect on caspase activity at any concentration or time point, which was unlike that of staurosporin. In addition, the fluorescence staining and western blot analyses of GCs for activating MKK4 phosphorylation revealed a rapid and pronounced activation by vacquinol-1 at 7.5 μM [1].
In vivo: The ability of vacquinol-1 to attenuate tumor progression was previously tested in a mouse model for human GBM. Vacquinol-1 or vehicle (DMSO) were intracranially administered into the site of original cell deposit 6 weeks after engraftment. Results showed that tumors were invariantly smaller, and the area of necrosis and hGFAP and hNestin immunoreactivity was significantly reduced. Moreove, only tumor cells in vacquinol-1-treated mice showed a massive LAMP1 staining [1].
Clinical trial: Up to now, vacquinol-1 is still in the preclinical development stage.
Reference:
[1] Kitambi SS et al. Vulnerability of glioblastoma cells to catastrophic vacuolization and death induced by a small molecule. Cell. 2014 Apr 10;157(2):313-28.
| Cas No. | 5428-80-8 | SDF | |
| 别名 | NSC13316 | ||
| 化学名 | (2-(4-chlorophenyl)quinolin-4-yl)(piperidin-2-yl)methanol | ||
| Canonical SMILES | OC(C1=CC(C2=CC=C(Cl)C=C2)=NC3=CC=CC=C13)C4NCCCC4 | ||
| 分子式 | C21H23Cl3N2O | 分子量 | 425.78 |
| 溶解度 | DMF: 10 mg/ml,DMF:PBS(pH 7.2)(1:1): 0.5 mg/ml,DMSO: 1 mg/ml,Ethanol: 0.25 mg/ml | 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 | 2.3486 mL | 11.7432 mL | 23.4863 mL |
| 5 mM | 0.4697 mL | 2.3486 mL | 4.6973 mL |
| 10 mM | 0.2349 mL | 1.1743 mL | 2.3486 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: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet