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    CYC116
    CYC116

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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 #: V0364
    CAS #: 693228-63-6Purity ≥98%

    Description: CYC116 is a novel, potent, orally bioavailable inhibitor of Aurora A/B/C kinases with potential antitumor activity. It inhibits Aurora A/B/C with IC50s of 44 nM, 19 nM and 65 nM respectively. CYC116 is less potent against VEGFR2 (Ki of 44 nM), with 50-fold greater potency than CDKs, and is not active against PKA, Akt/PKB, PKC, GSK-3α/β, CK2, Plk1 and SAPK2A.  

    ReferencesJ Med Chem. 2010 Jun 10;53(11):4367-78.

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    Molecular Weight (MW)368.46
    FormulaC18H20N6OS
    CAS No.693228-63-6
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 24 mg/mL (65.1 mM)
    Water: <1 mg/mL
    Ethanol: <1 mg/mL
    Solubility (In vivo)1% DMSO+30% polyethylene glycol+1% Tween 80: 30 mg/mL
    Synonyms

    Synonym: CYC 116; CYC-116; CYC116.

    Chemical Name: 4-methyl-5-(2-(4-morpholinophenylamino)pyrimidin-4-yl)thiazol-2-amine

    InChi Key: GPSZYOIFQZPWEJ-UHFFFAOYSA-N

    InChi Code: InChI=1S/C18H20N6OS/c1-12-16(26-17(19)21-12)15-6-7-20-18(23-15)22-13-2-4-14(5-3-13)24-8-10-25-11-9-24/h2-7H,8-11H2,1H3,(H2,19,21)(H,20,22,23)

    SMILES Code: NC1=NC(C)=C(C2=NC(NC3=CC=C(N4CCOCC4)C=C3)=NC=C2)S1


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    In Vitro

    In vitro activity: The most Aurora-selective CYC116 shows inhibitory effect on Aurora A and B kinases 50-fold more potently than any of the CDKs assayed. CYC116 is initially screened against a panel of human leukemia and solid tumor cell lines using an MTT antiproliferative assay. The results show that CYC116 has broad-spectrum antitumor activity and shows specific cytotoxicity against the acute myelogenous leukemia cell line MV4-11 with IC50 of 34 nM. In addition, anti-proliferative activity of CYC116 is found to be associated with Aurora A and B modulation such as, inhibition of Aurora autophosphorylation, reduction of histone H3 phosphorylation, polyploidy, followed by cell death, resulting from a failure in cytokinesis.


    Kinase Assay: Aurora A kinase assays are performed using a 25 μL reaction volume (25 mM β-glycerophosphate, 20 mM Tris/HCl, pH 7.5, 5 mM EGTA, 1 mM DTT, 1 mM Na3VO4, 10 μg of kemptide (peptide substrate)). Recombinant Aurora A kinase is diluted in 20 mM Tris/HCl, pH 8, containing 0.5 mg/mL BSA, 2.5% glycerol, and 0.006% Brij-35. Reactions are started by the addition of 5 μL Mg/ATP mix (15 mM MgCl2, 100 μM ATP, with 18.5 kBq γ-32P-ATP per well) and incubated at 30°C for 30 minutes before termination with 25 μL of 75 mM H3PO4. Aurora B kinase assays are performed like Aurora A except that prior to use, Aurora B is activated in a separate reaction at 30°C for 60 minutes with inner centromere protein.


    Cell Assay: Standard MTT assays are performed. In short, cells (HeLa, MCF7, MV4-11 and A2780 cells) are seeded into 96-well plates according to doubling time and incubated overnight at 37°C. Test compounds are made up in DMSO, a 3-fold dilution series is prepared in 100 μL of cell medium, added to cells (in triplicates) and incubated for 72 or 96 hours at 37°C. MTT is made up as a stock of 5 mg/mL in cell medium, and the solution is filter-sterilized. Medium is removed from the cells followed by a wash with PBS. MTT solution is then added at 20 μL/well and incubated in the dark at 37°C for 4 hours. MTT solution is removed and cells are again washed with 200 μL of PBS. MTT dye is solubilized with 200 μL/well of DMSO by agitation. Absorbance is read at 540 nm and data analyzed using curve-fitting software to determine IC50 values.

    In VivoMice bearing subcutaneous NCI-H460 xenografts are given CYC116 orally for 5 days, at dose levels of 75 and 100 mg/kg q.d. It leads to tumor growth delays of 2.3 and 5.8 days, which translated into specific growth delays of 0.32 and 0.81, respectively.
    Animal modelNCI-H460 cells are implanted intraperitoneally into the mice
    Formulation & DosageDissolved in DMSO and then diluted in water; 75, 100 mg/kg;  Oral gavage
    References

    J Med Chem. 2010 Jun 10;53(11):4367-78


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

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