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    K03861 (AUZ 454)
    K03861 (AUZ 454)

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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 #: V1536
    CAS #: 853299-07-7Purity ≥98%

    Description: K03861 (K0 3861; AUZ-454; K-03861; AUZ 454), an aminopyrimidine-phenyl urea analog, is novel and potent type II cyclin-dependent kinase-CDK2 inhibitor with potential anticancer activity. It inhibits CDK2(WT), CDK2(C118L), CDK2(A144C), and CDK2(C118L/A144C) with Kd of 50 nM, 18.6 nM, 15.4 nM, and 9.7 nM respectlvely. The cocrystal structure of CDK2 in complex with K03861 revealed a canonical type II binding mode. K03861 acts by competing with the binding of cyclins.  

    References: ACS Chem Biol. 2015 Sep 18;10(9):2116-25.

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    Molecular Weight (MW)501.50
    FormulaC24H26F3N7O2
    CAS No.853299-07-7
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 100 mg/mL (199.4 mM)
    Water: <1 mg/mL 
    Ethanol: 15 mg/mL (29.9 mM)
    Other info

    Chemical Name: 1-(4-((2-aminopyrimidin-4-yl)oxy)phenyl)-3-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)urea

    InChi Key: PWDLXPJQFNVTNL-UHFFFAOYSA-N

    InChi Code: InChI=1S/C24H26F3N7O2/c1-33-10-12-34(13-11-33)15-16-2-3-18(14-20(16)24(25,26)27)31-23(35)30-17-4-6-19(7-5-17)36-21-8-9-29-22(28)32-21/h2-9,14H,10-13,15H2,1H3,(H2,28,29,32)(H2,30,31,35)

    SMILES Code: O=C(NC1=CC=C(CN2CCN(C)CC2)C(C(F)(F)F)=C1)NC3=CC=C(OC4=NC(N)=NC=C4)C=C3

    Synonyms

    K03861; AUZ454; K-03861; AUZ 454; K 03861; AUZ-454


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    In Vitro

    In vitro activity: K03861 is an aminopyrimidine-phenyl urea inhibitor of CDK2. The type II inhibitor CDK2 cocrystal structure of CDK2 with the inhibitor K03861 revealed a canonical type II binding mode. The type II inhibitors could compete with the binding of cyclins. The residues important for the type II inhibitors may be distant to the ATP binding pockets. The crystal structure of this complex may provide a foundation for the cyclin-competitive CDK2 inhibitors 


    Kinase Assay: K03861 is a type II CDK2 inhibitor with Kd of 8.2 nM. AUZ 454 (K03861) inhibits CDK2 activity by competing with binding of activating cyclins.

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    References

    ACS Chem Biol. 2015 Sep 18;10(9):2116-25.


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

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