A selective Aurora kinase B inhibitor
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Pro-drug Form(s)
13647AZD 1152 (hydrochloride)
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AZD 1152-HQPA

Item No. 11602

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
5-[[7-[3-[ethyl(2-hydroxyethyl)amino]propoxy]-4-quinazolinyl]amino]-N-(3-fluorophenyl)-1H-pyrazole-3-acetamide
CAS Number
722544-51-6
Synonyms
  • Barasertib-HQPA
Molecular Formula
C26H30FN7O3
Formula Weight
507.6
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 1 mg/mlDMSO: 15 mg/mlDMSO:PBS(pH 7.2) (1:2): 0.33 mg/mlEthanol: slightlyPBS (pH 7.2): slightly
λmax
223, 235, 324 nm
SMILES
OCCN(CC)CCCOC1=CC2=C(C(NC3=CC(CC(NC4=CC(F)=CC=C4)=O)=NN3)=NC=N2)C=C1
InChi Code
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
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

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    Product Description

    AZD 1152-HQPA is an inhibitor of Aurora kinase B (IC50 = 0.37 nM) that demonstrates ~3,700-fold greater selectivity for Aurora kinase B over Aurora kinase A (IC50 = 1.368 µM).1,2 It does not have activity against a panel of 50 other serine-threonine or tyrosine kinases, including FLT3, JAK2, and Abl.1,2 AZD 1152-HQPA has been shown to inhibit the proliferation of hematopoietic malignant cells (IC50s = 3-40 nM), disrupting spindle checkpoint functions and chromosome alignment, resulting in inhibition of cytokinesis followed by apoptosis, and to inhibit tumor xenograft growth in vivo.2,3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Mortlock, A.A., Foote, K.M., Heron, N.M., et al. Discovery, synthesis, and in vivo activity of a new class of pyrazoloquinazolines as selective inhibitors of aurora B kinase. J. Med. Chem. 50(9), 2213-2224 (2007).

    2. Yang, J., Ikezoe, T., Nishioka, C., 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 110(6), 2034-2040 (2007).

    3. Wilkinson, R.W., Odedra, R., Heaton, S.P., et al. AZD1152, a selective inhibitor of Aurora B kinase, inhibits human tumor xenograft growth by inducing apoptosis. Clin. Cancer. Res 13(12), 3682-3688 (2007).

    Product Citations

    Li, T., Huang, T., Du, M., et al. Phosphorylation and chromatin tethering prevent cGAS activation during mitosis. Science (2021).