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CP-10 | CP-10 : Degrader (PROTAC) of CDK6
RATINGS:
Cellular Use: (3 reviews)

In Model Organisms: (0 reviews)
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
Vendors
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Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
CDK6
    • DC50, IC50, Dmax:2.1 nM (DC50); 10 nM MM.aS, 8 nM Mino; 72% @ 10 nM, 89% @ 100 nM
    Degrader (PROTAC)
    100 nM

    Selectivity

    In Cell Selectivity Assessment
    Selectivity Assessment Description:
    >50 fold selective over CDK4. Outside target family: Quantitative proteomic analysis confirmed ...

    Potency
    Cellular
    In Vitro

    CDK6

    Mode of Action: Degrader (PROTAC)

    Structure-Activity-Relationship data available? No

    DOI Reference: 10.1021/acs.jmedchem.9b00871

    Negative Control Compounds

    CP-23

    Orthogonal Probes def

    BSJ-03-123

    Chemical Information

    Molecular Formula C44H49N13O7
    SMILEs CC(=O)c1c(C)c2cnc(Nc3ccc(N4CCN(Cc5cn(CCOCCNc6cccc7c6C(=O)N(C6CCC(=O)NC6=O)C7=O)nn5)CC4)cn3)nc2n(C2CCCC2)c1=O
    InChI InChI=1S/C44H49N13O7/c1-26-32-23-47-44(50-39(32)56(29-6-3-4-7-29)42(62)37(26)27(2)58)48-35-12-10-30(22-46-35)54-17-15-53(16-18-54)24-28-25-55(52-51-28)19-21-64-20-14-45-33-9-5-8-31-38(33)43(63)57(41(31)61)34-11-13-36(59)49-40(34)60/h5,8-10,12,22-23,25,29,34,45H,3-4,6-7,11,13-21,24H2,1-2H3,(H,49,59,60)(H,46,47,48,50)
    Molecular weight 871.39 Da
    AlogP 2.9998200000000015
    HBond acceptors 20
    HBond donors 3
    Atoms 113

    References

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    Expert Reviews

    by SERP
    (on 9 Feb 2021 )
    Cellular Use Rating
    This molecule should have good selectivity for CDK6 based on the selectivity of the parent compound Palbociclib used to generate the PROTAC. However, the kinome or cellular selectivity have not actually...
    by SERP
    (on 9 Feb 2021 )
    Cellular Use Rating
    CP-10 is a selective CDK6 degrader comprising Palbociclib linked to Pomalidomide. Used alongside the structurally matched negative controls CP-9 and CP-23, CP-10 can be a useful cell-based probe to...
    by SERP+
    (on 31 Oct 2024 )
    Cellular Use Rating
    the compound seems a good degrader but also degrades CDK4. More selective degraders i.e, BSJ-03-123 exist, which also based on palbociclib.
    Note: The Chemical Probes Portal only endorses compounds as chemical probes for use as specific and selective modulators of the proposed target if they receive three or more (3-4) stars. Read more about our evaluation criteria