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BAVDEGALUTAMIDE | BAVDEGALUTAMIDE : Degrader (PROTAC) of AR
RATINGS:
Cellular Use: (1 reviews)

In Model Organisms: (1 reviews)
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
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Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
AR (Mutant:WT, F877L, T878A, M896V, and H875Y)
    • DC50:1 nM
    • IC50:10 nM
    • IC50:20 nM
    Degrader (PROTAC)
    up to 30 nM

    Selectivity

    In Cell Selectivity Assessment
    Selectivity Assessment Description:
    In the MCF-7 breast cancer cell line, bavdegalutamide treatment (30–300 nmol/L) resulted in the degr ...
    In Cell Selectivity Assessment
    Potency Assay Off-Target:
    Unbiased proteomic screen of nearly 4,000 detectable proteins in VCaP cells showed that treatment wi ...
    In Cell Selectivity Assessment
    Selectivity Assessment Description:
    Treatment of Ramos cells with increasing concentrations of bavdegalutamide did not lead to degradati ...

    Potency
    Cellular
    In Vitro

    AR (Mutant:WT, F877L, T878A, M896V, and H875Y)

    Mode of Action: Degrader (PROTAC)

    Structure-Activity-Relationship data available? Yes

    DOI Reference: 10.1158/1535-7163.MCT-23-0655

    In Vivo Validations

    Mouse
    Dose: 2 mg/Kg
    Route of delivery: Intravenous
    Plasma half life: 11.4 ± 0.51 h
    Systemic clearance: 180.9 ± 30.8 mL/h/Kg
    Cmax: 1263 ± 99 ng/mL
    Tmax: 0.05 h
    Area Under the Curve:: 11304 ± 1964 ng*h/mL
    Volume of Distribution at Steady-State: 2636 ± 402 mL/Kg

    DOI Reference: 10.3390/molecules27061977

    Dose: 5 mg/Kg
    Route of delivery: Oral
    Plasma half life: 14.57 ± 2.479 h
    Cmax: 612.0 ± 88.38 ng/mL
    Tmax: 4.800 ± 1.789 h
    Area Under the Curve:: 10,707 ± 1176 ng∙h/mL
    Bioavailability: 37.89 ± 4.16 %

    DOI Reference: 10.3390/molecules27061977

    Rat
    Dose: 2 mg/Kg
    Route of delivery: Intravenous
    Plasma half life: 13.62 ± 1.43 h
    Systemic clearance: 413.6 ± 31.7 mL/h/Kg
    Cmax: 2525 ± 292 ng/mL
    Tmax: 0.083 ± 0.000 h
    Area Under the Curve:: 4857 ± 381 ng∙h/mL
    Volume of Distribution at Steady-State: 5775 ± 320 mL/Kg

    DOI Reference: 10.3390/molecules27061977

    Dose: 5 mg/Kg
    Route of delivery: Oral
    Plasma half life: 17.67 ± 3.21 h
    Cmax: 110.5 ± 9.2 ng/mL
    Tmax: 5.500 ± 1.915 h
    Area Under the Curve:: 2894 ± 318 ng∙h/mL
    Bioavailability: 23.83 ± 2.62 %

    DOI Reference: 10.3390/molecules27061977

    Chemical Information

    Molecular Formula C41H43ClFN9O6
    SMILEs N#Cc1ccc(O[C@H]2CC[C@H](NC(=O)c3ccc(N4CCC(CN5CCN(c6cc7c(cc6F)C(=O)N(C6CCC(=O)NC6=O)C7=O)CC5)CC4)nn3)CC2)cc1Cl
    InChI InChI=1S/C41H43ClFN9O6/c42-31-19-28(4-1-25(31)22-44)58-27-5-2-26(3-6-27)45-38(54)33-7-9-36(48-47-33)51-13-11-24(12-14-51)23-49-15-17-50(18-16-49)35-21-30-29(20-32(35)43)40(56)52(41(30)57)34-8-10-37(53)46-39(34)55/h1,4,7,9,19-21,24,26-27,34H,2-3,5-6,8,10-18,23H2,(H,45,54)(H,46,53,55)/t26-,27-,34?
    Molecular weight 811.30 Da
    AlogP 3.700580000000002
    HBond acceptors 15
    HBond donors 2
    Atoms 101

    Expert Reviews

    by SERP
    (on 7 Jan 2026 )
    Cellular Use Rating
    In Model Organisms
    ( The reviewer did not leave any comments )
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