Barasertib-HQPA (AZD2811) is a highly selective Aurora B inhibitor with an IC50 of 0.37 nM in a cell-free assay. Barasertib-HQPA (AZD2811) induces growth arrest and apoptosis in cancer cells.
IC50&Target
Aurora B
0.37 nM (IC50)
体外研究
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.
Cell Proliferation Assay.
Cell Line:
AML lines (HL-60, NB4, MOLM13), ALL line (PALL-2), biphenotypic leukemia (MV4-11), acute eosinophilic leukemia (EOL-1), and the blast crisis of chronic myeloid leukemia K562 cells.
Concentration:
0-100 nM. (Barasertib -HQPA)
Incubation Time:
48 h.
Result:
IC50 values ranged from 3 nM to 40 nM.
体内研究
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.
分子式
C26H30FN7O3
分子量
507.56
CAS号
722544-51-6
中文名称
巴拉塞替-HQPA
运输条件
Room temperature in continental US; may vary elsewhere.