巴拉塞替-HQPA

  • 化学数据
CAS号 722544-51-6 货号 BCP01736
中文名 巴拉塞替-HQPA
英文名 Barasertib-HQPA
中文别名
英文别名 Defosbarasertib;AZD-2811; AZD 2811; AZD2811; AZD-1152HQPA; AZD 1152HQPA; AZD1152HQPA; AZD1152 HQPA; AZD1152-HQPA; AZD1152HQPA;
分子式 C26H30FN7O3 分子量 507.56
  • 用途
生物活性 Barasertib, previously known as AZD1152-hydroxyquinazoline pyrazol anilide (HQPA), is a potent aurora kinase inhibitor, which is resulted from rapid phosphatase-mediated cleavage of the precursor, AZD1152, in serum following parenteral administration in vivo. It shows inhibitory effects against a broad range of aurora kinases, including aurora A kinase (AKB), aurora B kinase (ABK), and aurora C kinase (ACK) with inhibition constant (Ki) of 1369 nM, 0.36 nM, and 17.0 nM respectively, as well as the FMS-like tyrosine kinase 3 internal tandem duplication (FLT3-ITD) mutation. Barasertib has demonstrated anti-tumor activity against a range tumor cell lines including those of leukaemic acute myeloid leukemia (AML) origin.
上下游产品 722543-31-9(巴拉塞替)
信号通路 Cell Cycle/DNA Damage Epigenetics 
靶 点 Aurora 

结构式

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