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Barasertib-HQPA

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产品编号 T2602Cas号 722544-51-6
别名 Barasertib, AZD2811, AZD1152-HQPA|AZD2811, AZD1152-HQPA, 1H-Pyrazole-3-acetamide

Barasertib-HQPA (AZD2811) 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-HQPA

Barasertib-HQPA

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纯度: 99.29%
产品编号 T2602 别名 Barasertib, AZD2811, AZD1152-HQPA|AZD2811, AZD1152-HQPA, 1H-Pyrazole-3-acetamideCas号 722544-51-6

Barasertib-HQPA (AZD2811) 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。

规格价格库存数量
2 mg¥ 339现货
5 mg¥ 498现货
10 mg¥ 698现货
25 mg¥ 1,450现货
50 mg¥ 2,820现货
100 mg¥ 4,180现货
500 mg¥ 9,120现货
1 mL x 10 mM (in DMSO)¥ 589现货
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产品介绍

生物活性
产品描述
Barasertib-HQPA (AZD2811) is a highly selective Aurora B inhibitor (IC50: 0.37 nM) and demonstrates ~3,700-fold greater selectivity than Aurora A.
靶点活性
Aurora B:0.37 nM (cell free)
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]。
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].
别名Barasertib, AZD2811, AZD1152-HQPA|AZD2811, AZD1152-HQPA, 1H-Pyrazole-3-acetamide
化学信息
分子量507.56
分子式C26H30FN7O3
CAS No.722544-51-6
SmilesCCN(CCO)CCCOc1ccc2c(Nc3cc(CC(=O)Nc4cccc(F)c4)[nH]n3)ncnc2c1
密度1.359 g/cm3 (Predicted)
储存&溶解度
存储Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
溶解度信息
Ethanol: 3 mg/mL (5.91 mM)
H2O: < 1 mg/mL (insoluble or slightly soluble)
DMSO: 94 mg/mL (185.2 mM)
溶液配制表
1mg5mg10mg50mg
1 mM1.9702 mL9.8511 mL19.7021 mL98.5105 mL
5 mM0.3940 mL1.9702 mL3.9404 mL19.7021 mL
1mg5mg10mg50mg
10 mM0.1970 mL0.9851 mL1.9702 mL9.8511 mL
20 mM0.0985 mL0.4926 mL0.9851 mL4.9255 mL
50 mM0.0394 mL0.1970 mL0.3940 mL1.9702 mL
100 mM0.0197 mL0.0985 mL0.1970 mL0.9851 mL

计算器

  • 摩尔浓度 计算器
  • 稀释 计算器
  • 配液 计算器
  • 分子量 计算器

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法:
TargetMol | Animal experiments比如您的给药剂量是 10 mg/kg ,每只动物体重 20 g ,给药体积 100 μLTargetMol | Animal experiments 一共给药动物 10 只 ,您使用的配方为 5% TargetMol | reagent DMSO+ 30%PEG300+ 5%Tween 80 + 60% ddH2O. 那么您的工作液浓度为 2 mg/mL
母液配置方法: 2 mg 药物溶于 50 μLDMSOTargetMol | reagent ( 母液浓度为 40 mg/mL ), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:50μLDMSOTargetMol | reagent 母液,添加 300 μLPEG300TargetMol | reagent 混匀澄清,再加 50μLTween 80, 混匀澄清,再加 600μLddH2OTargetMol | reagent 混匀澄清

以上为“体内实验配液计算器”的使用方法举例,并不是具体某个化合物的推荐配制方式,请根据您的实验动物和给药方式选择适当的溶解方案。

1 请输入动物实验的基本信息
mg/kg
g
μL
2 请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
% DMSO
%
%Tween 80
%ddH2O

剂量转换

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