TAK960

- Overview
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    Background
    
    IC50: 8.4 to 46.9 nmol/L for multiple cancer cell linesPolo-like kinase 1 (PLK1) is a serine/threonine protein kinase involved in key mitosis processes. Human PLK1 has been shown to be overexpressed in various human cancers. Elevated levels of PLK1 have been associated with poor prognosis, making it an attractive target for anticancer therapy. TAK-960 is a novel, investigational, orally bioavailable, potent, and selective PLK1 inhibitor.In vitro: TAK-960 treatment caused accumulation of G2–M cells, aberrant polo mitosis morphology, and increased the phosphorylation of histone H3. TAK-960 inhibited proliferation of multiple cancer cell lines, with mean EC50 ranging from 8.4 to 46.9 nmol/L, but not in nondividing normal cells [1]. In vivo: 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. Once daily treatment TAK-960 exhibited significant efficacy against multiple tumor xenografts, including an adriamycin/paclitaxel-resistant xenograft model and a disseminated leukemia model [1]. Clinical trial: TAK-960 is currently undergoing Phase I evaluation in adult patients with advanced non-hematologic malignancies.
    
    [1] Hikichi Y, Honda K, Hikami K, Miyashita H, Kaieda I, Murai S, Uchiyama N, Hasegawa M, Kawamoto T, Sato T, Ichikawa T, Cao S, Nie Z, Zhang L, Yang J, Kuida K, Kupperman E. TAK-960, a novel, orally available, selective inhibitor of polo-like kinase 1, shows broad-spectrum preclinical antitumor activity in multiple dosing regimens. Mol Cancer Ther. 2012 Mar;11(3):700-9.
- Properties
  - Alternative 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
    
    CAS Number
    
    1137868-52-0
    
    Molecular Formula
    
    C27H34F3N7O3
    
    Molecular Weight
    
    561.6
    
    Appearance
    
    A solid
    
    Purity
    
    98.06%
    
    Solubility
    
    ≥28.05 mg/mL in DMSO; insoluble in H2O; ≥12.3 mg/mL in EtOH
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only

TAK960

Background

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