产品说明书
BX-912
 |
同义名 : | - |
| CAS号 : | 702674-56-4 | |
| 货号 : | A348390 | |
| 分子式 : | C20H23BrN8O | |
| 纯度 : | 99%+ | |
| 分子量 : | 471.354 | |
| MDL号 : | MFCD10565925 | |
| 存储条件： |
粉末 Keep in dark place,Sealed in dry,Store in freezer, under -20°C 液体 -20°C:3-6个月-80°C:12个月 |
|
| 溶解度 : |
DMSO: 105 mg/mL(222.76 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO |
|
| 动物实验配方： |
| 生物活性 | |||
|---|---|---|---|
| 靶点 |
|
||
| 描述 | The phosphoinositide 3-kinase/3-phosphoinositide-dependent kinase 1 (PDK1)/Akt signaling pathway plays a key role in cancer cell growth, survival, and tumor angiogenesis and represents a promising target for anticancer drugs. BX-912 is a direct, selective, and ATP-competitive PDK1 inhibitor with an IC50 value of 26 nM. BX-912 blocks PDK1/Akt signaling in tumor cells and inhibits the anchorage-dependent growth of a variety of tumor cell lines in culture or induces apoptosis. When treating asynchronously growing cultures of tumor cells for 18 h with 10 μM BX-912, it promoted a pronounced increase in the population of MDA-468 cells with 4 N DNA content, indicative of a block at the G2/M phase of the cell cycle. BX-912 also potently inhibited the growth of HCT-116 and PC-3 cells in soft agar, showing a 96% inhibitory effect at a dose of 1 μM for HCT-116 and IC50 value of 0.32 μM for PC-3. | ||
| 作用机制 | BX-912 binds to the ATP binding pocket of PDK1. The structure of enzyme-inhibitor complexes reveals two hydrogen bonds between two aminopyrimidine nitrogens and the amino acid backbone of Ala162, which lies in the hinge region of the molecule. | ||
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
|
1 mM 5 mM 10 mM |
2.12mL 0.42mL 0.21mL |
10.61mL 2.12mL 1.06mL |
21.22mL 4.24mL 2.12mL |
| 参考文献 |
|---|