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Merck

SML0268

AZD1152-HQPA

≥98% (HPLC), aurora-B kinase inhibitor, powder

동의어(들):

3-[[7-[3-[Ethyl(2-hydroxyethyl)amino]propoxy]-4-quinazolinyl]amino]-N-(3-fluorophenyl)-1H-pyrazole-5-acetamide

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제품정보 (DICE 배송 시 비용 별도)

실험식(Hill 표기법):
C26H30FN7O3
CAS 번호:
Molecular Weight:
507.56
UNSPSC Code:
12352200
PubChem Substance ID:
NACRES:
NA.77
MDL number:
Assay:
≥98% (HPLC)
Form:
powder
Quality level:
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제품 이름

AZD1152-HQPA, ≥98% (HPLC)

Quality Level

assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

DMSO: >15 mg/mL

storage temp.

2-8°C

SMILES string

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

Application

AZD1152-HQPA has been used as a specific inhibitor of aurora kinase B (AURKB) to examine the cell cycle stage the IRG (hit compound that induces an irregular nuclear shape)-treated cells accumulate and become senescent and also to study the roles of cyclin-dependent kinase 6 (CDK6) and AURKB in restricting enterovirus 71 (EV71) infection.
AZD1152-HQPA has been used:
  • for the dose dependent inhibition of aurora kinase B (AURKB)
  • as a component to identify that, replication timing regulatory factor 1 (RIF1) and protein phosphatase 1 (PP1) are critical for the regulation of abscission timing in human cells
  • as a component to study the relevance of AURKB as a cancer therapeutic target

Biochem/physiol Actions

AZD1152-HQPA is a selective aurora-B kinase inhibitor; anti-cancer agent.
AZD1152-HQPA is the active metabolite of AZD-1152, a potent selective Aurora Kinase B inhibitor. AZD1152 is 50-fold selective for Aurora kinase B over Aurora kinase C and over 1000-fold selective for Aurora kinase B over Aurora Kinase A. (IC50s: aurora-A, 1,369 nmol/L; aurora-B, 0.36 nmol/L; aurora-C, 17.0 nmol/L). It is converted in plasma to the active form AZD1152-HQPA, which has been shown to have antineoplastic activity in a variety of animal models and human cancer cell lines.

Other Notes

AZD1152-HQPA has been expertly reviewed and recommended by the Chemical Probes Portal. For more information, please visit the AZD1152-HPQA probe summary on the Chemical Probes Portal website.


wgk

WGK 3

저장 등급

11 - Combustible Solids

flash_point_f

Not applicable

flash_point_c

Not applicable



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문서 라이브러리 방문



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
The RIF1-PP1 Axis Controls Abscission Timing in Human Cells
Bhowmick R, et al.
Current Biology (2019)
Human genome-wide RNAi screen reveals host factors required for enterovirus 71 replication
Wu KX, et al.
Nature Communications, 7, 13150-13150 (2016)