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Barasertib-HQPA

产品编号 T2602 CAS 722544-51-6

别名: Barasertib, AZD1152-HQPA, 1H-Pyrazole-3-acetamide, AZD2811, AZD1152-HQPA|AZD2811

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。

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Barasertib-HQPA, CAS 722544-51-6

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选择批次

纯度: 99.29%

纯度: 98.46%

纯度: 98.43%

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生物活性

化学信息

存储 & 溶解度

参考文献

相关产品

产品描述	Barasertib (AZD1152-HQPA) 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	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].
体内活性	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].
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, AZD1152-HQPA, 1H-Pyrazole-3-acetamide, AZD2811, AZD1152-HQPA\|AZD2811
分子量	507.56
分子式	C26H30FN7O3
CAS No.	722544-51-6

存储

Powder: -20°C for 3 years | In solvent: -80°C for 2 years

溶解度

Ethanol: 3 mg/mL (5.91 mM)

H2O: <1 mg/mL

DMSO: 94 mg/mL (185.2 mM)

( < 1 mg/mL refers to the product slightly soluble or insoluble )

参考文献

1. Yang, Jing., et al. AZD1152, a novel and selective aurora B kinase inhibitor, induces growth arrest, apoptosis, and sensitization for tubulin depolymerizing agent or topoisomerase II inhibitor in human acute leukemia cells in vitro and in vivo. Blood. 2007 Sep 15;110(6):2034-40. 2. Zekri A, et al. AZD1152-HQPA induces growth arrest and apoptosis in androgen-dependent prostate cancer cell line (LNCaP) via producing aneugenic micronuclei and polyploidy. Tumour Biol. 2015 Feb;36(2):623-32. 3. Wilkinson RW, et al. AZD1152, a selective inhibitor of Aurora B kinase, inhibits human tumor xenograft growth by inducing apoptosis. Clin Cancer Res. 2007 Jun 15;13(12):3682-8. 5. Kuang Y, Chai Y, Xu L, et al. Glabrone as a specific UGT1A9 probe substrate and its application in discovering the inhibitor glycycoumarin[J]. European Journal of Pharmaceutical Sciences. 2021: 105786.

文献引用

1. Kuang Y, Chai Y, Xu L, et al. Glabrone as a specific UGT1A9 probe substrate and its application in discovering the inhibitor glycycoumarin. European Journal of Pharmaceutical Sciences. 2021: 105786. 2. Qi J, Gao X, Zhong X, et al. Selective inhibition of Aurora A and B kinases effectively induces cell cycle arrest in t(8;21) acute myeloid leukemia. Biomedicine & Pharmacotherapy. 2019, 117: 109113. 3. Wang D, Wang Y, Di X, et al.Cortical tension drug screen links mitotic spindle integrity to Rho pathway.Current Biology.2023

剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

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：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 μL，一共给药动物10 只，您使用的配方为5% 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 μL DMSO (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：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

第一步：请输入动物实验的基本信息

剂量

mg/kg

每只动物体重

给药体积

μL

动物数量

第二步：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

%DMSO+

计算重置

计算结果如下:

工作液浓度: mg/ml;

母液配置方法: mg 药物溶于 μL DMSO (母液浓度为 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：取 μL DMSO 主液，加入 μL PEG300，混匀澄清，再加 μL Tween 80，混匀澄清，再加 μL ddH₂O, 混匀澄清。

备注:

要按顺序从左向右依次添加助溶剂。可配合物理方法，如涡流、超声波或热水浴使之帮助溶解。

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

质量

浓度

容积

分子量

浓度 (起始)

容积 (起始)

浓度 (终)

容积 (终)

溶液体积

质量

配液浓度

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技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到，包括如何准备库存溶液，如何存储产品，以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

Barasertib-HQPA 722544-51-6 Apoptosis Cell Cycle/Checkpoint Chromatin/Epigenetic Aurora Kinase AZD-2811 colon Inhibitor Barasertib BarasertibHQPA AZD 2811 AZD1152-HQPA cancer INH 34 leukemia breast inhibit 1H-Pyrazole-3-acetamide AZD2811 AZD1152-HQPA|AZD2811 lung INH-34 INH34 Barasertib HQPA inhibitor

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Barasertib-HQPA

存储

溶解度

参考文献

文献引用

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剂量换算

体内实验配液计算器

计算器

输入分子式，点击计算，可计算出产品的分子量。

技术支持

Keywords