| 产品描述: | CDK8-IN-13 is a potent, selective and orally active CDK8 inhibitor with an IC50 value of 51.9 nM. CDK8-IN-13 induces Apoptosis. CDK8-IN-13 decreases the expression of p-STAT1 S727 and p-STAT5 S726. CDK8-IN-13 shows antitumor activity. |
| 靶点: |
CDK8:51.9 nM (IC50);Apoptosis; CDK |
| 体外研究: |
CDK8-IN-13 (compound 43; 1, 2.5, 5, 10 µM; 12 h) 以剂量依赖性方式降低 HCT-116 细胞中 p-STAT1 S727 和 p-STAT5 S726 的表达. CDK8-IN-13 (0, 1, 5, 10 µM; 48 h) 以剂量依赖的方式诱导细胞凋亡。 |
| 体内研究: |
CDK8-IN-13 (40、80 mg/kg;口服;持续 15 天) 在小鼠体内以剂量依赖性方式抑制肿瘤生长。 |
| 参考文献: |
1. Zhang XX, et al. Discovery of a novel oral type Ⅰ CDK8 inhibitor against acute myeloid leukemia. Eur J Med Chem. 2023 May 5;251:115214. |
| 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 |
4.215 ml |
21.074 ml |
42.148 ml |
| 5 mM |
0.843 ml |
4.215 ml |
8.43 ml |
| 10 mM |
0.421 ml |
2.107 ml |
4.215 ml |
| 50 mM |
0.084 ml |
0.421 ml |
0.843 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。 |