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    TAK-901
    TAK-901

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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 #: V0362
    CAS #: 934541-31-8Purity ≥98%

    Description: TAK-901 (TAK901) is a novel and potent inhibitor of Aurora A/B kinases with potential antitumor activity. It inhibits Aurora A/B with IC50s of 21 nM and 15 nM, respectively, and shows little/no activity against JAK2, c-Src or Abl. TAK-901 displayed potent in vitro antiproliferative activity and high in vivo antitumor efficacy by binding to and inhibiting the activity of Aurora B, leading to a decrease in the proliferation of tumor cells that overexpress Aurora B. 

    References: Mol Cancer Ther. 2013 Apr;12(4):460-70.

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    Molecular Weight (MW)504.64
    FormulaC28H32N4O3S
    CAS No.934541-31-8
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 101 mg/mL (200.1 mM)
    Water: <1 mg/mL
    Ethanol: <1 mg/mL
    Other infoChemical Name: 5-(3-(ethylsulfonyl)phenyl)-3,8-dimethyl-N-(1-methylpiperidin-4-yl)-9H-pyrido[2,3-b]indole-7-carboxamide
    InChi Key: WKDACQVEJIVHMZ-UHFFFAOYSA-N
    InChi Code: InChI=1S/C28H32N4O3S/c1-5-36(34,35)21-8-6-7-19(14-21)23-15-22(28(33)30-20-9-11-32(4)12-10-20)18(3)26-25(23)24-13-17(2)16-29-27(24)31-26/h6-8,13-16,20H,5,9-12H2,1-4H3,(H,29,31)(H,30,33)
    SMILES Code: O=C(C1=C(C)C2=C(C(C3=CC=CC(S(=O)(CC)=O)=C3)=C1)C4=CC(C)=CN=C4N2)NC5CCN(C)CC5
    SynonymsTAK-901, TAK 901, TAK901


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    In Vitro

    In vitro activity: TAK-901 inhibits Aurora A-TPX2 and Aurora B-INCENP in tight binding, time-dependent manner. Dissociation of TAK-901 from Aurora B-INCENP is slow with at 1/2 of 920 minutes, and the affinity constant for TAK-901 binding to Aurora B-INCENP is determined to be 0.02 nM. TAK-901 induces inhibition of cell proliferation in cultured human cancer cell lines from different tissues with IC50s ranging from 40 to 500nM. Consistent with Aurora B inhibition, TAK-901 treatment produces polyploidy in human PC3 prostate cancer and HL60 acute myeloid leukemia cells as measured by immunofluorescence and flow cytometry. Examination of a broad panel of kinases reveals that multiple kinases, including FLT3, FGFR and the Src family kinases, are inhibited by TAK-901 with IC50 values similar to those for Aurora A and B. In cells, TAK-901 suppresses the Flt3 and FGFR2 autophosphorylation with IC50 values close to that of Aurora B as measured by cellular histone H3 phosphorylation, whereas the IC50s for inhibition of cellular Src and Bcr Abl are 20-fold weaker. In a panel of pathway specific reporter-based cell models, TAK-901 inhibits the NFkB and JAK/STAT pathways with submicromolar potency.


    Kinase Assay: TAK-901 is a novel inhibitor of Aurora A/B with IC50 of 21 nM/15 NM. TAK-901 inhibits Aurora A-TPX2 and Aurora B-INCENP in tight binding, time-dependent manner. Dissociation of TAK-901 from Aurora B-INCENP is slow with at 1/2 of 920 minutes, and the affinity constant for TAK-901 binding to Aurora B-INCENP is determined to be 0.02 NM.


    Cell Assay: TAK-901 induces inhibition of cell proliferation in cultured human cancer cell lines from different tissues with IC50s ranging from 40 to 500nM. Consistent with Aurora B inhibition, TAK-901 treatment produces polyploidy in human PC3 prostate cancer and HL60 acute myeloid leukemia cells as measured by immunofluorescence and flow cytometry. Examination of a broad panel of kinases reveals that multiple kinases, including FLT3, FGFR and the Src family kinases, are inhibited by TAK-901 with IC50 values similar to those for Aurora A and B. In cells, TAK-901 suppresses the Flt3 and FGFR2 autophosphorylation with IC50 values close to that of Aurora B as measured by cellular histone H3 phosphorylation, whereas the IC50s for inhibition of cellular Src and Bcr Abl are 20-fold weaker. In a panel of pathway specific reporter-based cell models, TAK-901 inhibits the NFkB and JAK/STAT pathways with submicromolar potency.

    In VivoIn rodent xenografts, TAK-901 exhibited potent activity against multiple human solid tumor types, and complete regression was found in the ovarian cancer A2780 model. In vivo biomarker studies showed that TAK-901 induced PD responses consistent with Aurora B inhibition and correlating with retention of TAK-901 in tumor tissue
    Animal modelMice and rats
    Formulation & DosageIntravenously twice daily (b.i.d.)  
    ReferencesMol Cancer Ther. 2013 Apr;12(4):460-70.


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

    TAK-901

    A, chemical structure of TAK-901. B, TAK-901 inhibition of Aurora A and B kinase/coactivator complexes and kinetic data of the Aurora B/INCENP enzyme complex. C, kinase inhibition profile of TAK-901. D, enzyme reaction progression curves showing TAK-901 time-dependent binding to (D) and dissociation (E) from Aurora B/INCENP enzyme complex.  Mol Cancer Ther. 2013 Apr;12(4):460-70.

    TAK-901

    TAK-901 inactivates cellular Aurora B kinase and inhibits cell proliferation. A, immunoblot analysis of histone H3 phosphorylation in PC3 cells treated with TAK-901. B, PC3 cells were incubated for 48 hours with dimethyl sulfoxide or 0.2 μmol/L TAK-901 and stained for actin (green) and DNA (blue). C, DNA content histograms of HL60 cells after incubation for 48 hours with a concentration dilution series of TAK-901. D, TAK-901 EC50 values for cell proliferation (DNA synthesis) inhibition in cells. Mol Cancer Ther. 2013 Apr;12(4):460-70.

    TAK-901

    Profile of various TAK-901 kinase targets. A, MV4-11 cells, 2 μmol/L FLT3/MTK inhibitor. B, KATO-III cells, 10 μmol/L Aurora B inhibitor. C, profile of TAK-901 cellular activity against Aurora B kinase and several cross-reacting kinases. EC50 values derived from dose–response immunoblotting or cellular reporter. Mol Cancer Ther. 2013 Apr;12(4):460-70.

    TAK-901

    In vivo antitumor activity of TAK-901 in human tumor and leukemia xenograft models. Mol Cancer Ther. 2013 Apr;12(4):460-70.

    TAK-901

    In vivo effects of TAK-901 on Aurora B pharmacodynamic markers. A, histone H3 phosphorylation in nude rat A2780 xenograft tumors.  B, polyploidy in nude mice A2780 xenograft tumors. Mol Cancer Ther. 2013 Apr;12(4):460-70.



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