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。Barasertib-HQPA (AZD2811) 对可引起癌细胞生长阻滞和凋亡。
| 生物活性 | Barasertib-HQPA (AZD2811) is a highly selectiveAurora Binhibitor with anIC50of 0.37 nM in a cell-free assay. Barasertib-HQPA (AZD2811) induces growth arrest andapoptosisincancercells[1]. |
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体外研究
(In Vitro) | Barasertib-HQPA (3 μM, 3 hours) significantly decreases expression of the phosphorylated forms of histone H3 in freshly isolated leukemia cells[1].
Barasertib-hydroxyquinazoline pyrazol anilide (HQPA)] is converted rapidly to the active Barasertib-HQPA in plasma[2].
Barasertib-HQPA treatment induced defective cell survival, polyploidy, and cell death in LNCaP cell line[3].
Barasertib-HQPA induces a marked anti-propliferative effect accompanied by the appearance of a polyploid population, which in most cases led to apoptosis[4].
Cell Proliferation Assay[1]. | Cell Line: | 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. | | Concentration: | 0-100 nM. (Barasertib -HQPA) | | Incubation Time: | 48 h. | | Result: | IC50values ranged from 3 nM to 40 nM. |
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体内研究
(In Vivo) | Barasertib (AZD1152, 25 mg/kg) markedly suppresses the growth and weights of AZD1152-treated tumors[1].
Barasertib (AZD1152, 5 mg/kg) enhances the ability of vincristine or daunorubicin to inhibit the proliferation of human MOLM13 leukemic xenografts[1].
Barasertib (AZD1152, (10-150 mg/kg/d) potently inhibited the growth of human colon, lung, and hematologic tumor xenografts (mean tumor growth inhibition range, 55% to z100%; P< 0.05) in immunodeficient mice[2].
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | | Powder | -20°C | 3 years | | 4°C | 2 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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| 溶解性数据 | In Vitro: DMSO : ≥ 22 mg/mL(43.34 mM) *"≥" means soluble, but saturation unknown. 配制储备液 | 1 mM | 1.9702 mL | 9.8511 mL | 19.7021 mL | | 5 mM | 0.3940 mL | 1.9702 mL | 3.9404 mL | | 10 mM | 0.1970 mL | 0.9851 mL | 1.9702 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂： ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂： 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.5 mg/mL (4.93 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (4.93 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。 2. 请依序添加每种溶剂： 10% DMSO 90%corn oil Solubility: ≥ 2.5 mg/mL (4.93 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (4.93 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。 *以上所有助溶剂都可在本网站选购。
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