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

溶解度:DMSO

储存条件:-20C 2 years

生物活性

AZD1152 is a dihydrogen phosphate prodrug of a pyrazoloquinazoline Aurora kinase inhibitor [AZD1152�Chydroxyquinazoline pyrazol anilide (HQPA)] and is converted rapidly to the active AZD1152-HQPA in plasma . AZD1152-HQPA is a highly potent and selective inhibitor of Aurora B (Ki, 0.36 nM) compared with Aurora A (Ki, 1,369 nM) and has a high specificity versus a panel of 50 other kinases. Consistent with inhibition of Aurora B kinase, addition of AZD1152-HQPA to tumor cells in vitro induces chromosome misalignment, prevents cell division, and consequently reduces cell viability and induces apoptosis.

参考文献

1. Aihara A, et al. J Hepatol. 2009 Oct 29.

2. Walsby E, et al. Haematologica. 2008 May;93(5):662-9.