| 名称 | Barasertib-HQPA |
| 描述 | Barasertib-HQPA (AZD2811) is a highly selective Aurora B inhibitor (IC50: 0.37 nM) and demonstrates ~3,700-fold greater selectivity than Aurora A. |
| 细胞实验 | 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]. |
| 动物实验 | 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]. |
| 体外活性 | Barasertib抑制了急性髓性白血病（AML）系列（HL-60, NB4, MOLM13）、急性淋巴性白血病（ALL）系列（PALL-2）、双表型白血病（MV4-11）、急性嗜酸性白血病（EOL-1）以及慢性髓性白血病爆发期K562细胞的增殖，其半抑制浓度（IC50）范围为3 nM至40 nM [1]。Barasertib-HQPA处理导致LNCaP细胞系的存活能力缺陷、多倍体以及细胞死亡，并降低了AR表达 [2]。 |
| 体内活性 | Barasertib对AML系列(HL-60, NB4, MOLM13)、ALL系列(PALL-2)、双表型白血病(MV4-11)、急性嗜酸性白血病(EOL-1)以及慢性髓性白血病危重期K562细胞的增殖抑制作用显著，IC50值介于3 nM至40 nM之间[1]。Barasertib-HQPA处理导致LNCaP细胞系存活能力受损、多倍体形成及细胞死亡。此外，Barasertib-HQPA治疗降低了AR表达[2]。Barasertib强力抑制了免疫缺陷小鼠中人类结肠、肺和血液肿瘤异种移植物的生长。在用Barasertib静脉治疗携带SW620结直肠肿瘤的无胸腺大鼠中，首先观察到组蛋白H3磷酸化的暂时抑制，随后细胞中4N DNA含量比对照组高出2.4倍，继而多倍体细胞比例增加[3]。 |
| 存储条件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
| 溶解度 | 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 3.3 mg/mL (6.5 mM), Sonication is recommended.
Ethanol : 3 mg/mL (5.91 mM), Sonication is recommended.
H2O : < 1 mg/mL (insoluble or slightly soluble)
DMSO : 250 mg/mL (492.55 mM), Sonication is recommended.
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| 关键字 | INH-34 | INH34 | INH 34 | colon | Barasertib-HQPA | BarasertibHQPA | Barasertib HQPA | AZD-2811 | AZD1152-HQPA|AZD-2811 | AZD1152-HQPA|AZD 2811 | AZD 2811 | AuroraKinase | Aurora Kinase | Aurora B | Apoptosis |
| 相关产品 | Urea | L-Methionine | Dimethyl phthalate | Aceglutamide | Alginic acid | Cysteamine hydrochloride | Sodium butanoate | Metronidazole | Dextran sulfate sodium salt (MW 5000) | Citric Acid Triammonium | Stavudine | Sodium 4-phenylbutyrate |
| 相关库 | 抑制剂库 | 经典已知活性库 | 抗癌活性化合物库 | 已知活性化合物库 | 激酶抑制剂库 | 抗衰老化合物库 | 高选择性抑制剂库 | 膜蛋白靶向化合物库 | 药物功能重定位化合物库 | 抗癌临床化合物库 | 人代谢物化合物库 | 抗癌药物库 |