BaRasertib-HQPA 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。它可阻滞癌细胞生长，诱导凋亡。

Barasertib (AZD1152-HQPA) is a highly selective Aurora B inhibitor (IC50: 0.37 nM) and demonstrates ~3,700-fold greater selectivity than Aurora A.

AZD1152 inhibited the proliferation of 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 with an IC50 ranging from 3 nM to 40 nM [1]. AZD1152-HQPA treatment induced defective cell survival, polyploidy, and cell death in LNCaP cell line. Treatment of AZD1152-HQPA decreased expression of AR [2].

AZD1152 inhibited the proliferation of 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 with an IC50 ranging from 3 nM to 40 nM [1]. AZD1152-HQPA treatment induced defective cell survival, polyploidy, and cell death in LNCaP cell line. Treatment of AZD1152-HQPA decreased expression of AR [2]. AZD1152 potently inhibited the growth of human colon, lung, and hematologic tumor xenografts in immunodeficient mice. In colorectal SW620 tumor-bearing athymic rats treated i.v. with AZD1152, transient suppression of histone H3 phosphorylation followed by accumulation of 4N DNA in cells (2.4-fold higher compared with controls) and then an increased proportion of polyploid cells [3].

LNCaP cells were cultured in RPMI 1640 medium supplemented with 10 % fetal bovine serum, in 5 % CO2 at 37 °C. The cells were treated with 5, 10, 50, 100, and 500 nM of AZD1152-HQPA for 48 h. After 48-h treatment with AZD1152-HQPA, cells were further incubated with 100 μl of MTT (0.5 mg/ml) at 37 °C for 2 h. Precipitated formazan was solubilized with 100 μl of DMSO, and the optical densitometry was measured at a wavelength of570 nm. Cell treated with 0.1 % DMSO was defined as the control group [2].

Female immune-deficient BALB/c nude mice at 4 weeks of age were maintained in pathogen-free conditions with irradiated chow. Animals were bilaterally, subcutaneously injected with 2 × 10^6 MOLM13 cells/tumor in 0.1 mL Matrigel. When MOLM13 cells formed palpable tumors, mice were divided randomly into control (n=5) and treatment groups (n=5), and treatment was begun. AZD1152 (5 or 25 mg/kg) with or without vincristine (0.2 mg/kg) was given to mice by intraperitoneal injection 4 times a week or every another day, respectively. Daunorubicin (1 mg/kg) was given to mice by intraperitoneal injection 6 times during 2 weeks of treatment either alone or in combination with AZD1152 (5 mg/kg). The dose of these agents was determined by our preliminary studies (data not shown). Control diluent was given to the untreated control mice. Body weight and tumors were measured twice a week. Tumor sizes were calculated by the formula: a × b × c, where "a" is the length, "b" is the width, and "c" is the height in millimeters. At the end of the experiment, animals were killed by CO2 asphyxiation and tumor weights were measured after their careful resection. Tumor tissue was collected for analysis [1].

722544-51-6

C26H30FN7O3

507.57

AZD1152-HQPA|AZD2811;AZD1152-HQPA;Barasertib;1H-Pyrazole-3-acetamide;AZD2811

Ethanol:3 mg/mL (5.91 mM)
H2O:<1 mgml
DMSO:94 mg/mL (185.2 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years