| 应用 |
A highly selective ARK-2 inhibitor |
| 产品介绍 |
AZD1152-HQPA是AZD-1152的活性代谢物，AZD1152-HQPA (Barasertib)是Aurora B 高选择性抑制剂，IC50为0.37 nM，比对Aurora A的抑制性高100倍。 |
| 备注 |
AZD1152-HQPA (Barasertib) is a highly selective Aurora B inhibitor with IC50 of 0.37 nM, ~100 fold more selective for Aurora B over Aurora A. |
| 生化机理 |
AZD1152-HQPA is the active metabolite of AZD-1152, a potent selective Aurora Kinase B inhibitor. AZD1152 is 50-fold selective for Aurora kinase B over Aurora kinase C and over 1000-fold selective for Aurora kinase B over Aurora Kinase A. (IC50s: aurora-A, 1,369 nmol/L; aurora-B, 0.36 nmol/L; aurora-C, 17.0 nmol/L). It is converted in plasma to the active form AZD1152-HQPA, which has been shown to have antineoplastic activity in a variety of animal models and human cancer cell lines. |
| 别名 |
AZD1152; AZD 1152; 5-((7-(3-(乙基(2-羟基乙基)氨基)丙氧基)-4-喹唑啉)氨基)-N-(3-氟苯基)-1H-吡唑-3-乙酰胺;;Barasertib;5-((7-(3-(ethyl(2-hydroxyethyl)amino)propoxy)-4-quinazolinyl)amino)-n-(3-fluorophenyl)-1h-pyrazole-3-acetamide；3-[[7-[3-[Ethyl(2-hydroxyethyl)amino]propoxy]-4-quinazolinyl]amino]-N-(3-fluorophenyl)-1H-pyrazole-5-acetamide |
