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    TAK-960 dihydrochloride
    TAK-960 dihydrochloride

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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 #: V4582
    CAS #: 1137868-52-0Purity ≥98%

    Description: TAK-960 dihydrochloride is  a novel, investigational, orally bioavailable, potent, and selective PLK1 polo-like kinase 1 (PLK1) inhibitor with an IC50 of 0.8 nM at 10 μM ATP; TAK-960 also shows inhibitory activities against PLK2and PLK3, with IC50s of 16.9 and 50.2 nM, respectively. Polo-like kinase 1 (PLK1) is a serine/threonine protein kinase involved in key processes during mitosis. Human PLK1 has been shown to be overexpressed in various human cancers, and elevated levels of PLK1 have been associated with poor prognosis, making it an attractive target for anticancer therapy. TAK-960 has shown activity in several tumor cell lines, including those that express multidrug-resistant protein 1 (MDR1). Consistent with PLK1 inhibition, TAK-960 treatment caused accumulation of G(2)-M cells, aberrant polo mitosis morphology, and increased phosphorylation of histone H3 (pHH3) in vitro and in vivo. TAK-960 inhibited proliferation of multiple cancer cell lines, with mean EC(50) values ranging from 8.4 to 46.9 nmol/L, but not in nondividing normal cells (EC(50) >1,000 nmol/L). The mutation status of TP53 or KRAS and MDR1 expression did not correlate with the potency of TAK-960 in the cell lines tested. In animal models, oral administration of TAK-960 increased pHH3 in a dose-dependent manner and significantly inhibited the growth of HT-29 colorectal cancer xenografts. Treatment with once daily TAK-960 exhibited significant efficacy against multiple tumor xenografts, including an adriamycin/paclitaxel-resistant xenograft model and a disseminated leukemia model. TAK-960 has entered clinical evaluation in patients with advanced cancers.

    References 2012 Mar;11(3):700-9. 

    Related CAS : 1137868-96-2 (HCl salt); 1137868-52-0 (free base)

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    TAK-960 dihydrochloride

    Name: TAK-960 dihydrochloride
    CAS#: 1137868-52-0
    Chemical Formula: C₂₇H₃₆Cl₂F₃N₇O₃
    Exact Mass: 634.52

    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Technical InformationSynonym: TAK960, TAK-960 dihydrochloride, TAK 960 dihydrochloride
    IUPAC/Chemical Name: 4-((9-cyclopentyl-7,7-difluoro-5-methyl-6-oxo-6,7,8,9-tetrahydro-5H-pyrimido[4,5-b][1,4]diazepin-2-yl)amino)-2-fluoro-5-methoxy-N-(1-methylpiperidin-4-yl)benzamide dihydrochloride
    SMILES Code: CN1C2=C(N=C(NC3=CC(F)=C(C(NC4CCN(C)CC4)=O)C=C3OC)N=C2)N(C5CCCC5)CC(F)(F)C1=O.Cl.Cl

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     TAK-960 dihydrochloride

    TAK-960 is a potent and selective inhibitor of PLK1. Mol Cancer Ther. 2012 Mar;11(3):700-9.

     TAK-960 dihydrochloride

    TAK-960 induces accumulation of aberrant mitotic cells in HT-29 cells. Mol Cancer Ther. 2012 Mar;11(3):700-9.

     TAK-960 dihydrochloride

    PK/PD and antitumor activity analysis for TAK-960 in mice bearing HT-29 colorectal cancer cells. Mol Cancer Ther. 2012 Mar;11(3):700-9.

    TAK-960 dihydrochloride

    Single-agent efficacy of TAK-960 in various tumor xenograft models using human cancer cell lines. Mol Cancer Ther. 2012 Mar;11(3):700-9.

     TAK-960 dihydrochloride

    TAK-960 inhibits proliferation of human cancer cell lines regardless of TP53 and KRASmutation and MDR1 expression status.

     TAK-960 dihydrochloride

    TAK-960 shows PD activity in paclitaxel-resistant model.  Mol Cancer Ther. 2012 Mar;11(3):700-9.


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