Name: MK-8745
Price: 196.00 USD

- Overview
  - Please contact us at for specific academic pricing.
    
    Background
    
    MK-8745 is a novel and selective inhibitor of Aurora A with IC50 value of 0.6 nM [1].
    Aurora A kinase is a member of mitotic serine/threonine kinases and plays an important role in cellular division by controlling chromatid segregation. It has been reported that abnormal expression of Aurora A is correlated with the high occurrence of cancer and its expression determines cell sensitivity to MK-8745 treatment [1].
    MK-8745 is a potent Aurora A inhibitor. When tested with p53-/+ cell lines, MK-8745 treatment induced apoptotic cell death in a p53-dependent manner through inhibiting Aurora A activity [1]. In non-Hodgkin lymphoma (NHL) cell lines, MK-8745 treatment arrested cell cycle in G2/M phase and induced cell death via inhibiting Aurora A kinase [2]. In HCT 116 Puma (-), HCT116 p21 (-), HCT116 Bax(-) and HCT116 Chk2(-) cell lines, MK-8745 treatment induced cell apoptosis with the percent of 25%, 22%, 25%, and 22%, respectively [3].
    In female athymic nude mice model subcutaneous xenografted with HCT116 Puma (-), HCT116 p21 (-), HCT116 Bax(-) and HCT116 Chk2(-) cells, administration of MK-8745 significantly inhibited tumor growth [3].
    
    [1]. Nair, J.S., A.L. Ho, and G.K. Schwartz, The induction of polyploidy or apoptosis by the Aurora A kinase inhibitor MK8745 is p53-dependent. Cell Cycle, 2012. 11(4): p. 807-17.
    [2]. Chowdhury, A., S. Chowdhury, and M.Y. Tsai, A novel Aurora kinase A inhibitor MK-8745 predicts TPX2 as a therapeutic biomarker in non-Hodgkin lymphoma cell lines. Leuk Lymphoma, 2012. 53(3): p. 462-71.
    [3]. Shionome, Y., et al., Integrity of p53 associated pathways determines induction of apoptosis of tumor cells resistant to Aurora-A kinase inhibitors. PLoS One, 2013. 8(1): p. e55457.
- Properties
  - Alternative Name
    
    (3-chloro-2-fluorophenyl)(4-((6-(thiazol-2-ylamino)pyridin-2-yl)methyl)piperazin-1-yl)methanone
    
    CAS Number
    
    885325-71-3
    
    Molecular Formula
    
    C20H19ClFN5OS
    
    Molecular Weight
    
    431.91
    
    Appearance
    
    A solid
    
    Purity
    
    99.81%
    
    Solubility
    
    ≥21.6 mg/mL in DMSO; insoluble in H2O; ≥2.28 mg/mL in EtOH with gentle warming and ultrasonic
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only

MK-8745

MK-8745

Background

We Also Recommend

ME0328

UNC669

Vorapaxar