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Barasertib-HQPA

CAS No. : 722544-51-6

MCE 国际站：Barasertib-HQPA

产品活性：Barasertib-HQPA (AZD2811) 是一种高度选择性的极光激酶B抑制剂，在非细胞试验中 IC₅₀ 值为0.37 nM。Barasertib-HQPA (AZD2811) 对可引起癌细胞生长阻滞和凋亡。

研究领域：Cell Cycle/DNA Damage  |  Epigenetics  |  Apoptosis

作用靶点：Aurora Kinase  |  Apoptosis

In Vitro: Barasertib-HQPA (3 μM, 3 hours) significantly decreases expression of the phosphorylated forms of histone H3 in freshly isolated leukemia cells.
?Barasertib-hydroxyquinazoline pyrazol anilide (HQPA) is converted rapidly to the active Barasertib-HQPA in plasma.
?Barasertib-HQPA treatment induced defective cell survival, polyploidy, and cell death in LNCaP cell line.
?Barasertib-HQPA induces a marked anti-propliferative effect accompanied by the appearance of a polyploid population, which in most cases led to apoptosis.

In Vivo: Barasertib-HQPA (AZD1152, 25 mg/kg) markedly suppresses the growth and weights of AZD1152-treated tumors.
?Barasertib-HQPA (AZD1152, 5 mg/kg) enhances the ability of vincristine or daunorubicin to inhibit the proliferation of human MOLM13 leukemic xenografts.
?Barasertib-HQPA (AZD1152, (10-150 mg/kg/d) potently inhibited the growth of human colon, lung, and hematologic tumor xenografts (mean tumor growth inhibition range, 55% to z100%; P < 0.05) in immunodeficient mice.

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