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dCDK9-202 | dCDK9-202 : Degrader (PROTAC) of CDK9
RATINGS:
Cellular Use: (3 reviews)

In Model Organisms: (3 reviews)
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
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Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
CDK9
    • DC50:3.5 ± 0.7 nM
    • IC50:8.5 ± 0.2 nM
    Degrader (PROTAC)
    10 nM, up to 25 nM

    Selectivity

    In Cell Selectivity Assessment
    Potency Assay Off-Target:
    dCDK9-202 was evaluated for its target selectivity in the TC-71 cell line. Among CDKs, compound dCDK ...
    In Cell Selectivity Assessment
    Potency Assay Off-Target:
    dCDK9-202 was highly potent and effective in the inhibition of multiple cancer cell lines and achiev ...

    Potency
    Cellular
    In Vitro

    CDK9

    Mode of Action: Degrader (PROTAC)

    Structure-Activity-Relationship data available? Yes

    DOI Reference: 10.1021/acs.jmedchem.5c01111

    In Vivo Validations

    Mouse
    Dose: 2 mg/Kg
    Route of delivery: Intravenous
    Plasma half life: 0.3 h
    Systemic clearance: 312 mL/min/Kg
    Cmax: 280 ng/mL
    Area Under the Curve:: 116 h*ng/mL
    Volume of Distribution at Steady-State: 7.1 L/Kg

    DOI Reference: 10.1021/acs.jmedchem.5c01111

    Negative Control Compounds

    canSAR7437559
    Notes: dCDK9-202Me was not able to degrade CDK9 with a Dmax of only 5% and IC50 >1000 nM in cell growth inhibition assay

    Chemical Information

    Molecular Formula C40H49N7O7S2
    SMILEs CC(C)(C)c1cnc(CSc2cnc(NC(=O)C3CCN(C(=O)CCCCCCCN4Cc5cc6c(cc5C4)C(=O)N(C4CCC(=O)NC4=O)C6=O)CC3)s2)o1
    InChI InChI=1S/C40H49N7O7S2/c1-40(2,3)30-19-41-32(54-30)23-55-34-20-42-39(56-34)44-35(50)24-12-15-46(16-13-24)33(49)9-7-5-4-6-8-14-45-21-25-17-27-28(18-26(25)22-45)38(53)47(37(27)52)29-10-11-31(48)43-36(29)51/h17-20,24,29H,4-16,21-23H2,1-3H3,(H,42,44,50)(H,43,48,51)
    Molecular weight 803.31 Da
    AlogP 5.655600000000006
    HBond acceptors 14
    HBond donors 2
    Atoms 105

    References

    Publications

    Cross References

    Expert Reviews

    by SERP
    (on 25 Nov 2025 )
    Cellular Use Rating
    In Model Organisms
    dCDK9-202 is a potent CDK9 degrader, CRBN and proteasome dependent. In comparison with the earlier degrader THAL-SNS-032 (based on the same inhibitor), the authors report improved cellular potency and...
    by SERP
    (on 27 Nov 2025 )
    Cellular Use Rating
    In Model Organisms
    ( The reviewer did not leave any comments )
    by SERP
    (on 6 Feb 2026 )
    Cellular Use Rating
    In Model Organisms
    This is a potent and selective CDK9 degrader and currently the best probe available. Data suggests that there is selectivity to CDK9 over other CDKs, but a full proteomics assessment is not provided....
    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