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CAS No. : 722543-31-9
MCE 国际站:Barasertib
产品活性:Barasertib (AZD1152) 是 Barasertib-hQPA 的前体药物,是高度选择性的 Aurora B 抑制剂,IC50 值为 0.37 nM。Barasertib (AZD1152) 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 is used for the in vitro experiments.
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 (AZD1152, 25 mg/kg) markedly suppresses the growth and weights of AZD1152-treated tumors.
Barasertib (AZD1152, 5 mg/kg) enhances the ability of vincristine or daunorubicin to inhibit the proliferation of human MOLM13 leukemic xenografts.
Barasertib (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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