| 产品描述: | Nutlin-3是一种有效的,选择性的Mdm2(依赖环指状的泛素蛋白连接酶和p53)拮抗剂,IC50为90 nM。可稳定p53缺陷的细胞中的p73。 |
| 靶点: |
Ki: 90 nM (p53-MDM2) |
| 体内研究: |
Nutlin-3 can suppress the growth of xenograft tumors derived from human osteosarcoma or leukemia cells, the anti-tumor activity of Nutlin-3 even at the dose of 200 mg/kg per oral administration is marginal in an HCT116-derived xenograft tumor model. Nutlin-3 may be a useful adjunct to improve the therapeutic ratio using precision radiotherapy targeted to hypoxic cells and warrants further study in vivo. |
| 参考文献: |
1. Yu Z, et al. Design, synthesis and biological evaluation of sulfamide and triazole benzodiazepines as novel p53-MDM2 inhibitors. Int J Mol Sci. 2014 Sep 5;15(9):15741-53. 2. Zhang Y, et al. Inauhzin and Nutlin3 synergistically activate p53 and suppress tumor growth.Cancer Biol Ther. Cancer Biol Ther. 2012 Aug;13(10):915-24. 3. Supiot S, et al. Nutlin-3 radiosensitizes hypoxic prostate cancer cells independent of p53. Mol Cancer Ther. 2008 Apr;7(4):993-9. |
| 溶解性: |
Soluble in ethanol (25 mg/ml), DMSO (20 mg/ml), DMF, methanol, and acetonitrile. Insoluble in water. Sparingly soluble in ethano |
| 保存条件: |
-80℃(运输条件:冰袋低温运输) |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
1.72 ml |
8.599 ml |
17.197 ml |
| 5 mM |
0.344 ml |
1.72 ml |
3.439 ml |
| 10 mM |
0.172 ml |
0.86 ml |
1.72 ml |
| 50 mM |
0.034 ml |
0.172 ml |
0.344 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。 |