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    CAY10603
    CAY10603

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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 #: V0267
    CAS #: 1045792-66-2Purity ≥98%

    Description: CAY10603 is a novel, potent and selective HDAC6 (Histone deacetylase) inhibitor with potential anticancer activity and a potential to treat neurodegenerative diseases. It inhibits HDAC6 with an IC50 of 2 pM, it displayed >200-fold selectivity over other HDACs. CAY10603 has IC50 of 271 nM, 252 nM, 0.42 nM, 6851 nM, and 90.7 nM for HDAC1, 2, 3, 8, and 10, respectively. CAY10603 has potent antiproliferative activity against pancreatic cancer cell lines with IC50 of<1 μM. It could be useful chemical probe to study HDAC biology. The inhibition of HDAC6 by CAY10603 inhibited the proliferation of lung adenocarcinoma cells and induced apoptosis. CAY10603 downregulated the levels of EGFR protein, which in turn inhibited activation of the EGFR signaling pathway. Moreover, CAY10603 synergized with gefitinib to induce apoptosis of the lung adenocarcinoma cell lines via the destabilization of EGFR. Taken together, our results suggest that the inhibition of HDAC6 may be a promising strategy for the treatment of lung adenocarcinoma.

    ReferencesJ Med Chem. 2008 Aug 14;51(15):4370-3;  2016 Jul;36(1):589-97. 

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    Molecular Weight (MW)446.5
    FormulaC22H30N4O6
    CAS No.1045792-66-2
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 89 mg/mL (199.3 mM)
    Water: <1 mg/mL
    Ethanol: 5 mg/mL (11.2 mM)
    Solubility (In vivo)5% DMSO+50% PEG 300+ddH2O: 9 mg/mL
    Synonyms

    CAY-10603; CAY10603; CAY 10603

    Chemical Name: tert-butyl (4-(3-((7-(hydroxyamino)-7-oxoheptyl)carbamoyl)isoxazol-5-yl)phenyl)carbamate

    SMILES Code: O=C(OC(C)(C)C)NC1=CC=C(C2=CC(C(NCCCCCCC(NO)=O)=O)=NO2)C=C1


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    In Vitro

    In vitro activity: CAY10603, via inhibition of HDAC6, shows potent antiproliferative activity against pancreatic cancer cell lines with IC50 of<1 μM, which can be used as a new molecular probe in exploring HDAC biology


    Kinase Assay: Purified HDACs are incubated with 1 mM carboxyfluorescein (FAM)-labeled acetylated peptide substrate and test compound for 17 h at 25 °C in HDAC assay buffer containing 100 mM HEPES (pH 7.5), 25 mM KCl, 0.1% BSA, and 0.01% Triton X-100. Reactions are terminated by the addition of buffer containing 0.078% SDS for a final SDS concentration of 0.05%. Substrate and product are separated electrophoretically using a Caliper LabChip 3000 system with blue laser excitation and green fluorescence detection (CCD2). The fluorescence intensity in the substrate and product peaks is determined using the Well Analyzer software on the Caliper system. The reactions are performed in duplicate for each sample. IC50 values are automatically calculated using the IDBS XLFit version 4.2.1 plug-in for Microsoft Excel and the XLFit 4-Parameter Logistic Model: ((A+((B_A)/1+((C/x)D)))), in which x is compound concentration, A and B are respectively the estimated minimum and maximum of percent inhibition, C is the inflection point, and D is the Hill slope of the sigmoidal curve. The standard errors of the IC50 values are automatically calculated using the IDBS XLFit version 4.2.1 plug-in for Microsoft Excel and the formula xf4_FitResultStdError.


    Cell Assay: The pancreatic cancer cell lines BxPc-3, HupT3, Mia Paca-2, Panc 04.03, and SU 86.86 are grown in medium (DMEM or RPMI) containing 10% fetal calf serum and l-glutamine. Pancreatic cancer cells are plated out in duplicate into 6 wells of a 96-well microtiter plate. Four hours post plating, individual wells are treated with diluent (DMSO) or varying concentrations of SAHA or the indicated HDACIs from a concentration of 1 nM to 50 mM. Cytotoxicity is measured at time “0”, and 72 h post treatment using the colorimetric MTT assay according to the manufacturer’s suggestions. The IC50 values are calculated using XLfit.

    In VivoNA
    Animal modelNA
    Formulation & DosageNA
    References

    J Med Chem. 2008 Aug 14;51(15):4370-3.


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

     

    CAY10603

    Comparison of IC50 (nM) Values of Compounds 1–11 (compound 7 is CAY10603) and SAHA against Class I and Class II HDACs. J Med Chem. 2008 Aug 14;51(15):4370-3.
     

    CAY10603

    General structural features of compounds 1–11. J Med Chem.2008 Aug 14;51(15):4370-3. 
     

    CAY10603

    Compound 7 (CAY10603) docked into the binding site of the current HDAC6 homology model. J Med Chem. 2008 Aug 14;51(15):4370-3. 


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