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    MK-8745
    MK-8745

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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 #: V0352
    CAS #: 885325-71-3Purity ≥98%

    Description: MK-8745 is a novel, potent, specific and selective Aurora A inhibitor with potential antitumor activity. It inhibits Aurora A with an IC50 of 0.6 nM, and is 450-fold more selective for Aurora A over Aurora B. It shows potent in vitro antiproliferative activity and high in vivo antitumor efficacy. Exposure of p53 wild-type cells to MK8745 resulted in the induction of p53 phosphorylation (ser15) and an increase in p53 protein expression. p53-dependent apoptosis by MK8745 was further confirmed in HCT 116 p53(-/-) cells transfected with wild-type p53.

    References: Leuk Lymphoma. 2012 Mar;53(3):462-71; Cell Cycle. 2012 Feb 15;11(4):807-17.

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    Molecular Weight (MW)431.91
    FormulaC20H19ClFN5OS
    CAS No.885325-71-3
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 86 mg/mL (199.1 mM)
    Water: <1 mg/mL
    Ethanol: 1 mg/mL (2.3 mM) 
    Other infoChemical Name: (3-chloro-2-fluorophenyl)(4-((6-(thiazol-2-ylamino)pyridin-2-yl)methyl)piperazin-1-yl)methanone.
    InChi Key: YCRFPWKUUNKNDN-UHFFFAOYSA-N
    InChi Code: InChI=1S/C20H19ClFN5OS/c21-16-5-2-4-15(18(16)22)19(28)27-10-8-26(9-11-27)13-14-3-1-6-17(24-14)25-20-23-7-12-29-20/h1-7,12H,8-11,13H2,(H,23,24,25)
    SMILES Code: O=C(C1=CC=CC(Cl)=C1F)N2CCN(CC3=NC(NC4=NC=CS4)=CC=C3)CC2
    SynonymsMK 8745; MK8745; MK-8745


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    In Vitro

    In vitro activity: MK-8745 leads to cell cycle arrest at the G2/M phase with accumulation of tetraploid nuclei followed by cell death in non-Hodgkin lymphoma (NHL) cell lines. Treatment with MK-8745 induces p21(waf1/cip1) and CycB1, indicating cell cycle arrest and an increase in the G2/M phase cell population. Following MK-8745 treatment, Aurora-A substrates (TACC3, Eg5 and TPX2) are rapidly degraded following the reduction of phospho-Aurora-A. MK8745 induces apoptotic cell death in a p53-dependent manner when tested in vitro in cell lines of multiple lineages. Exposure of p53 wild-type cells to MK8745 results in the induction of p53 phosphorylation (ser15) and an increase in p53 protein expression. p53-dependent apoptosis by MK8745 is further confirmed in HCT 116 p53(-/-) cells transfected with wild-type p53.


    Kinase Assay: MK-8745 is a novel, potent and selective Aurora A inhibitor with IC50 of 0.6 nM, 450-fold more selective for Aurora A over Aurora B. 


    Cell Assay: When tested with p53-/+ cell lines, MK-8745 treatment induced apoptotic cell death in a p53-dependent manner through inhibiting Aurora A activity. 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. 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. 

    In VivoNA
    Animal modelNA
    Formulation & Dosage
    ReferencesLeuk Lymphoma. 2012 Mar;53(3):462-71; Cell Cycle. 2012 Feb 15;11(4):807-17.


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

    MK-8745

    MK8745 is a selective inhibitor of Aurora A kinase.  2012 Feb 15;11(4):807-17.

    MK-8745

    Cell cycle effect and induction of apoptosis by MK8745 (5 µM) in isogenic variants of HCT-116 cells (parental, p53−/−, p21−/−). (A) Flow cytometry analysis of the HCT 116 (top) and its isogenic variants; p21−/− (middle) and p53−/− (bottom) upon exposure to MK for different time points (6, 17, 22, 30 and 40 h) and exposure to ABI (100 nM AZD 1152) for 40 h after Propidium Iodide staining.   2012 Feb 15;11(4):807-17.

    MK-8745

    Downregulation of Aurora A recapitulates the effects of MK8745.  2012 Feb 15;11(4):807-17.


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