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    Barasertib ( INH-34; AZD-1152-HQPA)
    Barasertib ( INH-34; AZD-1152-HQPA)

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    InvivoChem Cat #: V0345
    CAS #: 722544-51-6 Purity ≥98%

    Description: Barasertib ( INH34; AZD1152 or AZD1152-HQPA) is a novel, potent, highly selective, orally bioavailable small-molecule Aurora B inhibitor with potential antitumor activity. It inhibits Aurora B with an IC50 of 0.37 nM in a cell-free assay. As a dihydrogen phosphate pro-drug of Barasertib-hQPA, it shows potent in vitro antiproliferative activity and high in vivo antitumor efficacy. Barasertib shows inhibitory effects against a broad range of aurora kinases, including aurora A kinase (AKB), aurora B kinase (ABK), and aurora C kinase (ACK) with inhibition constant (Ki) of 1369 nM, 0.36 nM, and 17.0 nM respectively, as well as the FMS-like tyrosine kinase 3 internal tandem duplication (FLT3-ITD) mutation. 

    References: Blood. 2007 Sep 15;110(6):2034-40; Clin Cancer Res. 2007 Jun 15;13(12):3682-8.

    Related CAS: 722543-31-9 (Barasertib); 722543-50-2  

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    Molecular Weight (MW)507.56
    FormulaC26H30FN7O3
    CAS No.722544-51-6
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 102 mg/mL (201 mM)
    Water: <1 mg/mL
    Ethanol: <1 mg/mL
    Solubility (In vivo)30% PEG400+0.5% Tween80+5% propylene glycol: 30 mg/mL
    Synonyms

    INH-34;  INH34; AZD 2811; AZD2811;  INH 34; AZD1152-HQPA; AZD1152; AZD-1152; AZD 1152 HQPA; AZD-2811; AZD-1152HQPA; AZD 1152HQPA; AZD1152HQPA; AZD1152 HQPA; AZD1152-HQPA; AZD1152HQPA.

    Chemical Name: 2-(3-((7-(3-(ethyl(2-hydroxyethyl)amino)propoxy)quinazolin-4-yl)amino)-1H-pyrazol-5-yl)-N-(3-fluorophenyl)acetamide

    InChi Key: QYZOGCMHVIGURT-UHFFFAOYSA-N

    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)

    SMILES Code: O=C(NC1=CC=CC(F)=C1)CC2=CC(NC3=C4C=CC(OCCCN(CC)CCO)=CC4=NC=N3)=NN2 


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    In Vitro

    In vitro activity: AZD1152 displays >3000-fold selectivity for Aurora B as compared with Aurora A which has an IC50 of 1.368 μM. AZD1152 has even less activity against 50 other serine-threonine and tyrosine kinases including FLT3, JAK2, and Abl. AZD1152 inhibits the proliferation of hematopoietic malignant cells such as HL-60, NB4, MOLM13, PALL-1, PALL-2, MV4-11, EOL-1, THP-1, and K562 cells with IC50 of 3-40 nM, displaying ~100-fold potency than another Aurora kinase inhibitor ZM334739 which has IC50 of 3-30 μM. AZD1152 inhibits the clonogenic growth of MOLM13 and MV4-11 cells with IC50 of 1 nM and 2.8 nM, respectively, as well as the freshly isolated imatinib-resistant leukemia cells with IC50 values of 1-3 nM, more significantly compared with bone marrow mononuclear cells with IC50 values of >10 nM. AZD1152 induces accumulation of cells with 4N/8N DNA content, followed by apoptosis in a dose- and time-dependent manner.


    Kinase Assay: AZD1152 displays >3000-fold selectivity for Aurora B as compared with Aurora A which has an IC50 of 1.368 μM. AZD1152 has even less activity against 50 other serine-threonine and tyrosine kinases including FLT3, JAK2, and Abl. 


    Cell Assay: Cells are exposed to various concentrations of AZD1152 for 24 or 48 hours. Cell proliferation is measured by 3H-thymidine uptake (isotope added 6 hours before harvest), and the concentration that induced 50% growth inhibition (IC50) is calculated from dose-response curves. Cell cycle analysis is performed by flow cytometry. Cell apoptosis is measured by annexin V–FITC apoptosis detection kit.

    In VivoAdministration of AZD1152 (25 mg/kg) alone markedly suppresses the growth of MOLM13 xenografts, confirmed by the observation of necrotic tissue with infiltration of phagocytic cells. In addition, AZD1152 (10-150 mg/kg/day) significantly inhibits the growth of a variety of human solid tumor xenografts, including colon, breast, and lung cancers, in a dose-dependent manner.
    Animal modelFemale immune-deficient BALB/c nude mice subcutaneously injected with MOLM13 cells
    Formulation & DosageDissolved in 3M Tris, pH 9.0, at a concentration of 2.5 mg/mL; 5, 25 mg/kg;  i.p. injection
    ReferencesBlood. 2007 Sep 15;110(6):2034-40; Clin Cancer Res. 2007 Jun 15;13(12):3682-8.


    These protocols are for reference only. InvivoChem does not independently validate these methods.

    Barasertib (AZD1152-HQPA)

    Summary of the number of progenitor colonies formed/ml of methylcellulose medium supplemented with differing concentrations of AZD1152 ().  2009 May 15;69(10):4150-8.

    Barasertib (AZD1152-HQPA)

    The induction of polyploidy by AZD1152-HQPA in HL-60 and THP-1 cells.   2009 May 15;69(10):4150-8.

    Barasertib (AZD1152-HQPA)

    AZD1152-HQPA inhibited cell proliferation, induced cytotoxicity and inhibited phosphorylation of histone H3 (ser10) in AML cell lines.  2009 May 15;69(10):4150-8.


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