产品描述: | BX517是有效的、选择性PDK1抑制剂,可与该蛋白的ATP结合口袋结合,IC50为6 nM |
靶点: |
cAKT2:5 nM; PDX1:6 nM;Akt;PDK |
体外研究: |
BX-517 blocks activation of Akt in tumor cells |
体内研究: |
BX517 has poor pharmaceutical properties including short half-life (0.4 h in rat), low metabolic stability, and poor solubility |
参考文献: |
1. Islam I, et al. Indolinone based phosphoinositide-dependent kinase-1 (PDK1) inhibitors. Part 1: design, synthesis and biological activity. Bioorg Med Chem Lett. 2007, 17(14):3814-8. 2. Islam I, et al. Indolinone based phosphoinositide-dependent kinase-1 (PDK1) inhibitors. Part 2: optimization of BX-517. Bioorg Med Chem Lett. 2007, 17(14):3819-25. |
溶解性: |
soluble in DMSO |
保存条件: |
-20℃ |
配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
1 mM |
3.542 ml |
17.712 ml |
35.424 ml |
5 mM |
0.708 ml |
3.542 ml |
7.085 ml |
10 mM |
0.354 ml |
1.771 ml |
3.542 ml |
50 mM |
0.071 ml |
0.354 ml |
0.708 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。 |