Barasertib

产品编号: T14371 别名:

AZD1152,巴拉塞替

Barasertib 是 Barasertib-hQPA 的前体药物，在癌细胞中诱导生长停滞和凋亡。它是高度选择性的Aurora B抑制剂，IC50值为 0.37 nM。

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CAS：722543-31-9

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生物活性化学信息储存和溶解度信息参考文献引用文献

产品描述

AZD1152 is a pro-drug of Barasertib-hQPA. Which is a highly selective Aurora B inhibitor with IC50 of 0.37 nM in a cell-free assay.

体外活性

AZD1152 inhibits the proliferation of hematopoietic malignant cells such as HL-60, NB4, MOLM13, PALL-1, PALL-2, MV4-11, EOL-1, THP-1, and K562 cells with IC50 of 3-40 nM, displaying appr 100-fold potency than another Aurora kinase inhibitor ZM334739 which has IC50 of 3-30 μM and it also inhibits the clonogenic growth of MOLM13 and MV4-11 cells with IC50 of 1 nM and 2.8 nM, respectively, as well as the freshly isolated imatinib-resistant leukemia cells with IC50 values of 1-3 nM, more significantly compared with bone marrow mononuclear cells with IC50 values of >10 nM. AZD1152 displays >3000-fold selectivity for Aurora B as compared with Aurora A which has an IC50 of 1.368 μM. AZD1152 causes significant accumulation of cells with 4N/8N DNA content in KMS12 and U266 and induces apoptosis in KMS18 and U266. AZD1152 has even less activity against 50 other serine-threonine and tyrosine kinases including FLT3, JAK2, and Abl. AZD1152 induces accumulation of cells with 4N/8N DNA content, followed by apoptosis in a dose- and time-dependent manner[1]. AZD1152 in combination with DEX, has negative effects on cell viability in comparison with single agent in PMI8226, KMS11 and U266[3].

体内活性

Administration of AZD1152 (25 mg/kg) alone markedly suppresses the growth of MOLM13 xenografts, confirmed by the observation of necrotic tissue with infiltration of phagocytic cells[1]. AZD1152 (25 mg/kg/day) treatment reduces xenograft levels such that they are slightly lower levels than after the first round of treatment, but this is not statistically significant indicating that residual cells might be more resistant to a second cycle of AZD1152[4]. In addition, AZD1152 (10-150 mg/kg/day) significantly inhibits the growth of a variety of human solid tumor xenografts, including colon, breast, and lung cancers, in a dose-dependent manner[2].

Cas No.

722543-31-9

分子式

C26H31FN7O6P

分子量

587.54

别名

AZD1152;巴拉塞替;Barasertib

参考文献

[1]Evans RP, et al. The selective Aurora B kinase inhibitor AZD1152 is a potential new treatment for multiple myeloma. Br J Haematol. 2008 Feb;140(3):295-302.[2]Yang J, 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 [3]Oke A, et al. AZD1152 rapidly and negatively affects the growth and survival of human acute myeloid leukemia cells in vitro and in vivo. Cancer Res. 2009 May 15;69(10):4150-8.[4]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.

储存和溶解度

DMSO:33 mg/mL (56.17 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years

剂量换算 Barasertib 722543-31-9

对于各种应用，安全且有效的用药剂量是很有必要的了解更多

体内实验配液计算器

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 g

给药体积 ul

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 +

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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

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已知质量的化合物在一定体积内形成的溶液的浓度

质量

浓度

体积

分子量

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稀释计算器可以帮助您计算

制备已知体积和浓度溶液所需的化合物质量
将已知质量的化合物溶解到所需浓度所需的溶液体积
已知质量的化合物在一定体积内形成的溶液的浓度

浓度（起始）

体积（起始）

浓度（终点）

体积（终点）

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重组计算器可帮助您快速计算试剂的体积，以重组您的小瓶。

溶液体积

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配液浓度

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分子结构式

总分子量

g/mol

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技术支持

在抑制剂处理说明中可以找到您可能遇到的问题的答案。主题包括如何准备储备溶液，如何存储产品以及基于细胞的测定和动物实验需要特别注意的问题。

Keywords

AZD1152 breast Barasertib cancer colon AZD 1152 Aurora Kinase Inhibitor 巴拉塞替 AZD-1152 leukemia lung inhibit Apoptosis 722543-31-9

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Barasertib

AZD1152,巴拉塞替

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