BX-320 是一种选择性的、ATP 竞争性的、口服活性的直接 PDK1 抑制剂，在直接激酶测定中其 IC50 为 30 nM。 BX-320 还诱导细胞凋亡。抗癌作用。
| Cas No. | 702676-93-5 |
| 别名 | N1-[3-[[5-溴-2-[[3-[(1-吡咯烷基羰基)氨基]苯基]氨基]-4-嘧啶基]氨基]丙基]-2,2-二甲基丙烷二酰胺 |
| Canonical SMILES | O=C(N1CCCC1)NC2=CC(NC3=NC(NCCCNC(C(C)(C)C(N)=O)=O)=C(Br)C=N3)=CC=C2 |
| 分子式 | C23H31BrN8O3 |
| 分子量 | 547.5 |
| 溶解度 | DMSO: soluble |
| 储存条件 | -20°C |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request |
| 产品描述 | BX-320 is an inhibitor of the serine/threonine kinase 3-phosphoinositide-dependent protein kinase 1 (PDK1; IC50= 30 nM).1It is selective for PDK1 over a panel of 10 additional kinases (IC50s = >820 nM for all). BX-320 inhibits Akt and p70S6K1 phosphorylation in PC3 cells (IC50s = 1-3 µM). It induces apoptosis in, and inhibits the growth of, MDA-MB-468 breast cancer cells (IC50s = 0.5 and 0.6 µM, respectively), as well as inhibits cell growth in a panel of cancer cells (IC50s = 0.12-1.2 µM). BX-320 (200 mg/kg) inhibits the growth of lung tumors in a LOX melanoma mouse model of blood-borne metastasis. 1.Feldman, R.I., Wu, J.M., Polokoff, M.A., et al.Novel small molecule inhibitors of 3-phosphoinositide-dependent kinase-1J. Biol. Chem.280(20)19867-19874(2005) |
