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    ZM 447439
    ZM 447439

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V0346
    CAS #: 331771-20-1Purity ≥98%

    Description: ZM 447439 (ZM-447439) is a novel, potent, selective and ATP-competitive inhibitor of Aurora A and Aurora B with potential antitumor activity. It inhibits Aurora A and Aurora B with IC50s of 110 nM and 130 nM, respectively. It shows 8-fold higher selectivity for Aurora A/B over MEK1, Src, Lck and has little effect against CDK1/2/4, Plk1, Chk1, etc. Being specifically for Aurora kinases, ZM 447439 barely inhibits the majority of other protein kinases (IC50 > 10 μM), such as CDK1/2/4, IKK1/2, PLK1, CHK1, cFLT2, KDR2, FAK and Zap-70, except for MEK1, SRC and LCK (IC50 values of 1.79 μM, 1.03 and 0.88 μM respectively.

    References: Neuroendocrinology. 2010;91(2):121-30; J Cell Biol. 2003 Apr 28;161(2):267-80.

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    Molecular Weight (MW)513.59
    FormulaC29H31N5O4
    CAS No.331771-20-1
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 103 mg/mL (200.5 mM)
    Water: <1 mg/mL
    Ethanol: <1 mg/mL
    Solubility (In vivo)30% PEG400+0.5% Tween80+5% propylene glycol: 30 mg/mL
    Synonyms

    Synonym: ZM-447439; ZM 447439; ZM447439.

    Chemical Name: N-(4-((6-methoxy-7-(3-morpholinopropoxy)quinazolin-4-yl)amino)phenyl)benzamide

    InChi Key: OGNYUTNQZVRGMN-UHFFFAOYSA-N

    InChi Code: InChI=1S/C29H31N5O4/c1-36-26-18-24-25(19-27(26)38-15-5-12-34-13-16-37-17-14-34)30-20-31-28(24)32-22-8-10-23(11-9-22)33-29(35)21-6-3-2-4-7-21/h2-4,6-11,18-20H,5,12-17H2,1H3,(H,33,35)(H,30,31,32)

    SMILES Code: O=C(NC1=CC=C(NC2=C3C=C(OC)C(OCCCN4CCOCC4)=CC3=NC=N2)C=C1)C5=CC=CC=C5


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    In Vitro

    In vitro activity: In vitro, ZM-447439 selectively inhibits recombinant human Aurora A and B with IC50 values of 110 and 130 nM, respectively, while other protein kinases of diverse structural types including the mitotic kinases CDK1 and PLK1 are inhibited with IC50 values >10 μM. Aurora kinase inhibitor, ZM-447439 time- and dose-dependently inhibits the growth of all three cell lines with IC50 values of 3 μM (BON), 0.9 μM (QGP-1) and 3 μM (MIP-101) after 72 hours of continuous exposure. In addition, ZM-447439 potently induces cell apoptosis by promoting DNA fragmentation and caspase 3 and 7 activation, and arrests GEP-NET cells in the G0 /G1and G2/M phase of the cell cycle. In mouse embryo, inhibition of Aurora kinase activity by ZM-447439 results in abnormalities during mitosis by regulating the phosphorylation of histone H3 serine 10 (H3S10Ph) from G2 to metaphase with different perturbations in each embryonic cycle. A recent study shows that ZM-447439 exhibits growth inhibitory and proapoptotic effect on cervical cancer SiHa cells, and enhances the chemosensitivity to cisplatin.


    Kinase Assay: Recombinant Aurora A and B are expressed as NH2-terminal His6-tagged fusion proteins using a baculovirus expression system. Aurora A is purified by affinity chromatography using Ni-NTA agarose, and Aurora B is purified by ion exchange chromatography using CM Sepharose Fast Flow. 1 ng purified recombinant enzyme is added to a reaction cocktail containing 25 mM Tris-HCl, pH 7.5, 12.5 mM KCl, 2.5 mM NaF, 0.6 mM DTT, 6.25 mM MnCl2, 10 μM peptide substrate, 10 μM for Aurora A or 5 μM ATP for Aurora B, and 0.2 μCi γ-[33P]ATP (specific activity ≥2,500 Ci/mmol), and is then incubated at RT for 60 minutes. Reactions are stopped by addition of 20% phosphoric acid, and the products are captured on P30 nitrocellulose filters and assayed for incorporation of 33P with a BetaplateTM counter. No enzyme and no compound control values are used to determine the concentration of ZM447439, which gave 50% inhibition of enzyme activity. Further details are available on request from Nicholas Keen


    Cell Assay: In BON, QGP-1 and MIP-101 cells, ZM 447439 time- and dose-dependently inhibited cell growth with IC50 values of 3 μM, 0.9 μM and 3 μM, respectively.

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    References

    Neuroendocrinology. 2010;91(2):121-30; J Cell Biol. 2003 Apr 28;161(2):267-80


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

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