Chemical Probes logo
ARD-266 | Degrader (PROTAC) of AR
RATINGS:
Cellular Use: (2 reviews)

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

Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
AR
    • DC50, Dmax, IC50:0.53 nM LNCaP, 0.97 nM VCaP, 0.15 nM 22Rv1 (DC50); 90% 10 nM, >95% 100 nM, >99% 1000 nM; 2 nM LNCaP, 6 nM VCaP (IC50)
    Degrader (PROTAC)
    10-100 nM

    Selectivity

    Potency
    Cellular
    In Vitro

    AR

    Mode of Action: Degrader (PROTAC)

    Structure-Activity-Relationship data available? Yes

    DOI Reference: 10.1021/acs.jmedchem.9b01393

    Orthogonal Probes def

    ARCC-4

    Chemical Information

    Molecular Formula C52H59ClN6O7
    SMILEs Cc1cc([C@H](C(=O)N2C[C@H](O)C[C@H]2C(=O)N[C@@H](CC(=O)N2CCC(C#Cc3ccc(C(=O)N[C@H]4C(C)(C)[C@H](Oc5ccc(C#N)c(Cl)c5)C4(C)C)cc3)CC2)c2ccccc2)C(C)C)on1
    InChI InChI=1S/C52H59ClN6O7/c1-31(2)45(43-25-32(3)57-66-43)48(64)59-30-38(60)26-42(59)47(63)55-41(35-11-9-8-10-12-35)28-44(61)58-23-21-34(22-24-58)14-13-33-15-17-36(18-16-33)46(62)56-49-51(4,5)50(52(49,6)7)65-39-20-19-37(29-54)40(53)27-39/h8-12,15-20,25,27,31,34,38,41-42,45,49-50,60H,21-24,26,28,30H2,1-7H3,(H,55,63)(H,56,62)/t38-,41+,42+,45-,49-,50-/m1/s1
    Molecular weight 914.41 Da
    AlogP 7.359400000000009
    HBond acceptors 13
    HBond donors 3
    Atoms 125

    References

    Publications

    Cross References

    canSARChEMBL

    Vendors

    Note: This is not an exhaustive list and does not indicate endorsement by the portal.

    Expert Reviews

    by SERP
    (on 18 Feb 2021 )
    Cellular Use Rating
    ARD-266 potently induces cellular degradation of Androgen receptor at nanomolar concentrations within three hours of treatment in several tested human cell lines. As expected, degradation resulted in...
    by SERP+
    (on 6 Feb 2026 )
    Cellular Use Rating
    This probe demonstrated degradation of AR in LNCaP cells with good DC50 and Dmax values. A western blot assay with a defined time course of five timepoints demonstrated degradation of AR, with clear target...
    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