SML0268

AZD1152-HQPA

≥98% (HPLC)

• Synonym(s): 3-[[7-[3-[Ethyl(2-hydroxyethyl)amino]propoxy]-4-quinazolinyl]amino]-N-(3-fluorophenyl)-1H-pyrazole-5-acetamide
• Empirical Formula (Hill Notation): C₂₆H₃₀FN₇O₃
• CAS Number: 722544-51-6
• Molecular Weight: 507.56
• MDL number: MFCD10687152
• UNSPSC Code: 12352200
• PubChem Substance ID: 329825276
• NACRES: NA.77

Properties

• 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

Description

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 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.

Safety Information

• Storage Class: 11 - Combustible Solids
• wgk_germany: WGK 3
• flash_point_f: Not applicable
• flash_point_c: Not applicable