Barasertib, also known as AZD1152, is the precursor to Barasertib-hQPA and is a potent inhibitor of Aurora B kinase, demonstrating an IC50 value of 0.37 nM in cell-free assays. It is known to halt cell proliferation and promote apoptosis in various cancer cells. When applied to freshly isolated leukemia cells at a concentration of 3 μM for 3 hours, Barasertib-HQPA markedly reduces the levels of phosphorylated histone H3[1]. Barasertib-hydroxyquinazoline pyrazol anilide (HQPA) is swiftly transformed into the active form, Barasertib-HQPA, within the plasma[2]. Barasertib-HQPA elicits a significant anti-proliferative response, resulting in the emergence of a polyploid cell population, often culminating in apoptosis[3].
Barasertib 动物研究
Animal study
Barasertib at a dosage of 25 mg/kg, significantly reduces the growth and mass of tumors treated with AZD1152. Furthermore, Barasertib at 5 mg/kg improves the efficacy of vincristine or daunorubicin in curbing the growth of human MOLM13 leukemic xenografts[1]. When administered at doses ranging from 10 to 150 mg/kg/day, Barasertib effectively hampers the growth of xenografts of human colon, lung, and blood tumors in immunodeficient mice. The average inhibition of tumor growth observed was between 55% to 100%[2].
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