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Barasertib

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Chemical Structure| 722543-31-9 同义名 : Azd1152
CAS号 : 722543-31-9
货号 : A363646
分子式 : C26H31FN7O6P
纯度 : 99%+
分子量 : 587.54
MDL号 : MFCD15146330
存储条件：

粉末 Keep in dark place,Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 35 mg/mL(59.57 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 Barasertib, also known as AZD1152, is the precursor to Barasertib-hQPA and is a potent inhibitor of Aurora B kinase, demonstrating an IC50 value of 0.37 nM in cell-free assays. It is known to halt cell proliferation and promote apoptosis in various cancer cells. When applied to freshly isolated leukemia cells at a concentration of 3 μM for 3 hours, Barasertib-HQPA markedly reduces the levels of phosphorylated histone H3[1]. Barasertib-hydroxyquinazoline pyrazol anilide (HQPA) is swiftly transformed into the active form, Barasertib-HQPA, within the plasma[2]. Barasertib-HQPA elicits a significant anti-proliferative response, resulting in the emergence of a polyploid cell population, often culminating in apoptosis[3].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.70mL

0.34mL

0.17mL

8.51mL

1.70mL

0.85mL

17.02mL

3.40mL

1.70mL
参考文献

[1]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

[2]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.

[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.