My cart
In the shopping cart is not goods, to choose and buy!
  • Product Name
  • Size
  • Quantity
  • Amount
    Selected items : 0 pieces Total : CHECK OUT()

    Market Price:

    This product is for research use only, not for human use. We do not sell to patients.
    Number: - + Pieces(InventoryPieces)
    InvivoChem Cat #: V4581
    CAS #: 1137868-52-0Purity ≥98%

    Description: TAK-960 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 : 1137868-52-0; 1137868-96-2 (HCl salt)

    Customer Validation
    Official Supplier of
    • VE
    • OF
    • YALE
    • hhmi
    • 香港大学
    Related Products
    Publications Citing InvivoChem Products
    • Physicochemical and Storage Information
    • Protocol
    • Quality Control Documentation
    • Related Biological Data
    • Customer Review


    Name: TAK-960
    CAS#: 1137868-52-0
    Chemical Formula: C27H34F3N7O3
    Exact Mass: 561.26752
    Molecular Weight: 561.59917
    Elemental Analysis: C, 57.74; H, 6.10; F, 10.15; N, 17.46; O, 8.55
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Technical InformationSynonym: TAK960, TAK-960, TAK 960
    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
    InChi Code: InChI=1S/C27H34F3N7O3/c1-35-10-8-16(9-11-35)32-24(38)18-12-22(40-3)20(13-19(18)28)33-26-31-14-21-23(34-26)37(17-6-4-5-7-17)15-27(29,30)25(39)36(21)2/h12-14,16-17H,4-11,15H2,1-3H3,(H,32,38)(H,31,33,34)

    • Molarity Calculator
    • Dilution Calculator
    • The molarity calculator equation

      Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

      • Mass
      • Concentration
      • Volume
      • Molecular Weight *
      • =
      • ×
      • ×
    • The dilution calculator equation

      Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

      This equation is commonly abbreviated as: C1V1 = C2V2

      • Concentration (start)
      • ×
      • Volume (start)
      • =
      • Concentration (final)
      • ×
      • Volume (final)
      • ×
      • =
      • ×
      • C1
      • V1
      • C2
      • V2

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


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


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


    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.


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


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


      Home Prev Next Last page / pices


      Your information is safe with us. * Required Fields.
      Products are for research use only;  We do not sell to patients
      Tel: 1-708-310-1919
      Fax: 1-708-557-7486
      Subscribe to our E-newsletter
      • Name*
      • *
      • E-mail*
      • *
      • instructions:
      • *
      Copyright 2020 InvivoChem LLC | All Rights Reserved
      Do you confirm the receipt?