| 产品描述: | Elraglusib(9-ING-41)是一种有效的 glycogen synthase kinase-3 (GSK-3) 的抑制剂,并具有抗肿瘤活性。9-ING-41 可在细胞分裂前期通过靶向中心体和结合微管的GSK3β诱导凋亡和细胞周期停滞 |
| 靶点: |
GSK-3;Apoptosis; GSK-3; Autophagy |
| 体外研究: |
9-ING-41, a clinically relevant small molecule GSK-3β inhibitor with broad spectrum pre-clinical antitumor activity, suppresses the growth of neuroblastoma cells.9-ING-41 induces apoptosis and cell cycle arrest at prophase by targeting centrosomes and microtubule-bound GSK3β. |
| 体内研究: |
9-ING-41 has single-agent antitumor activity in a mouse model of MCL.Mouse xenograft studies shows that the combination of clinically relevant doses of CPT-11 and 9-ING-41 lead to greater antitumor effect than is observed with either agent alone. |
| 细胞实验: |
Cell lines: Neuroblastoma cell lines SK-N-DZ, SK-N-BE Concentrations: 0.1 μM–1 μM Incubation Time: 48 h Method: Measurement of cell viability. Relative number of viable cancer cells is determined by measuring the optical density using CellTiter 96 Aqueous One Solution Cell Proliferation Assay kit according to the manufacturer’s instructions. A GI50 value for each compound is calculated with a non-linear regression model of standard slope using GraphPad Prism 6.0 software. |
| 动物实验: |
Animal Models: 6–8 week-old female athymic nude mice Dosages: 70 mg/kg Administration: IP |
| 参考文献: |
1. Andrey V Ugolkov, et al. 9-ING-41, a small-molecule glycogen synthase kinase-3 inhibitor, is active in neuroblastoma. Anticancer Drugs. 2018 Sep;29(8):717-724. 2. Xiaosheng Wu, et al. Targeting glycogen synthase kinase 3 for therapeutic benefit in lymphoma. Blood. 2019 Jul 25;134(4):363-373. |
| 溶解性: |
Soluble in DMSO |
| 保存条件: |
-20℃ |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
2.473 ml |
12.366 ml |
24.731 ml |
| 5 mM |
0.495 ml |
2.473 ml |
4.946 ml |
| 10 mM |
0.247 ml |
1.237 ml |
2.473 ml |
| 50 mM |
0.049 ml |
0.247 ml |
0.495 ml |
|
| 注意: |
部分产品我司仅能提供部分信息,我司不保证所提供信息的权威性,仅供客户参考交流研究之用。 |