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Merck
CN

SML0268

Sigma-Aldrich

AZD1152-HQPA

≥98% (HPLC)

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别名:
3-[[7-[3-[乙基(2-羟基乙基)氨基]丙氧基]-4-喹唑啉]氨基]-N-(3-氟苯基)-1H-吡唑-3-乙酰胺
经验公式(希尔记法):
C26H30FN7O3
分子量:
507.56
MDL编号:
UNSPSC代码:
12352200
PubChem化学物质编号:
NACRES:
NA.77

质量水平

检测方案

≥98% (HPLC)

形式

powder

颜色

white to beige

溶解性

DMSO: >15 mg/mL

储存温度

2-8°C

SMILES字符串

CCN(CCO)CCCOc1ccc2c(Nc3cc(CC(=O)Nc4cccc(F)c4)[nH]n3)ncnc2c1

InChI

1S/C26H30FN7O3/c1-2-34(10-11-35)9-4-12-37-21-7-8-22-23(16-21)28-17-29-26(22)31-24-14-20(32-33-24)15-25(36)30-19-6-3-5-18(27)13-19/h3,5-8,13-14,16-17,35H,2,4,9-12,15H2,1H3,(H,30,36)(H2,28,29,31,32,33)

InChI key

QYZOGCMHVIGURT-UHFFFAOYSA-N

应用

AZD1152-HQPA已被用作极光激酶B (AURKB) 的特异性抑制剂,以检查IRG(诱导不规则核形的比中化合物)处理细胞积累并衰老的细胞周期阶段,并研究细胞周期蛋白的作用依赖性激酶6 (CDK6) 和AURKB在限制肠道病毒71 (EV71) 感染方面的作用。
AZD1152-HQPA已被:
  • 用于剂量依赖性抑制极光激酶B(AURKB)
  • 用作一种识别成分,以识别对于调节人类细胞脱落时间至关重要的复制时间调节因子1 (RIF1)和蛋白磷酸酶1 (PP1)
  • 用作一种研究成分,以研究AURKB作为癌症治疗靶标的相关性

生化/生理作用

AZD1152-HQPA 是AZD-1152的活性代谢产物,而后者是一种强效选择性 Aurora 激酶 B 抑制剂。 AZD1152 对 Aurora 激酶 B 的选择性是 Aurora 激酶 C 的 50 倍,对 Aurora 激酶 B 的选择性是 Aurora 激酶 A 的1000倍。(IC50s: aurora-A, 1,369 nmol/L; aurora-B, 0.36 nmol/L; aurora-C, 17.0 nmol/L)。它在血浆中转化为活性形式 AZD1152-HQPA,后者在多种动物模型和人类癌细胞系中表现出了抗肿瘤活性。

其他说明

Chemical Probes 门户页面已对 AZD1152-HQPA 进行了专家评审和推荐。欲了解更多信息,请访问 Chemical Probes 门户页面上的 AZD1152-HPQA 探针摘要

WGK

WGK 3

闪点(°F)

Not applicable

闪点(°C)

Not applicable


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The RIF1-PP1 Axis Controls Abscission Timing in Human Cells
Bhowmick R, et al.
Current Biology (2019)
Ali Zekri et al.
Anti-cancer drugs, 28(8), 841-851 (2017-06-24)
Aurora-B kinase overexpression plays important roles in the malignant progression of prostate cancer (PCa). AZD1152-HQPA, as an inhibitor of Aurora-B, has recently emerged as a promising agent for cancer treatment. In this study, we aimed to investigate the effects of
Xiaoxu Gang et al.
Gene, 599, 60-67 (2016-11-12)
Aurora B kinase, a member of serine/threonine kinase family, is the catalytic subunit of the chromosomal passenger complex and is essential for chromosome alignment, chromosome segregation, and cytokinesis during mitosis. Here, we cloned the full-length cDNA sequence of silkworm Aurora
Human genome-wide RNAi screen reveals host factors required for enterovirus 71 replication
Wu KX, et al.
Nature Communications, 7, 13150-13150 (2016)
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In vitro cellular & developmental biology. Animal, 54(1), 71-84 (2017-12-03)
Liposarcoma is a malignant soft tissue tumor that originates from adipose tissue and is one of the most frequently diagnosed soft tissue sarcomas in humans. There is great interest in identifying novel chemotherapeutic options for treating liposarcoma based upon molecular

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