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RP-1664 | RP-1664 : Inhibitor of PLK4
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
PLK4
    • EC50:51 nM
    • IC50:3 nM
    • IC50:130 nM
    Inhibitor
    up to 100 nM

    Selectivity

    In Cell Selectivity Assessment
    Potency Assay Off-Target:
    RP-11664 showed high selectivity across the kinome with significant binding observed with only six o ...
    Selectivity Assessment Description:
    Kinase binding selectivity was performed at ActivX Biosciences using the Kinativ kinase profiling pl ...

    Potency
    Cellular
    In Vitro

    PLK4

    Mode of Action: Inhibitor

    Structure-Activity-Relationship data available? No

    DOI Reference: 10.1021/acs.jmedchem.5c00529

    In Vivo Validations

    Mouse
    Dose: 1 mg/Kg IV, 5 mg/Kg PO
    Route of delivery: Intravenous, Oral
    Systemic clearance: 11 mL/min/Kg IV
    Bioavailability: 113% PO

    DOI Reference: 10.1021/acs.jmedchem.5c00529

    Rat
    Dose: 1.0 mg/Kg IV, 2.5 mg/Kg PO
    Route of delivery: Intravenous, Oral
    Systemic clearance: 5.9 mL/min/Kg IV
    Bioavailability: 28% PO

    DOI Reference: 10.1021/acs.jmedchem.5c00529

    Dog
    Dose: 0.5 mg/Kg IV, 1.15 mg/Kg PO
    Route of delivery: Intravenous, Oral
    Systemic clearance: 30 mL/min/Kg IV
    Bioavailability: 98% PO

    DOI Reference: 10.1021/acs.jmedchem.5c00529

    Monkey (Cynomolgus)
    Dose: o.5 mg/Kg IV, 1.25 mg/Kg PO
    Route of delivery: Intravenous, Oral
    Systemic clearance: 14 mL/min/Kg IV
    Bioavailability: 96% PO

    DOI Reference: 10.1021/acs.jmedchem.5c00529

    Chemical Information

    Molecular Formula C23H24F2N8O2S
    SMILEs Cc1cc(Nc2nc(N(C)c3c(F)cc(S(C)(=O)=O)cc3F)nc(-c3cn(C)cn3)c2C2CC2)n[nH]1
    InChI InChI=1S/C23H24F2N8O2S/c1-12-7-18(31-30-12)27-22-19(13-5-6-13)20(17-10-32(2)11-26-17)28-23(29-22)33(3)21-15(24)8-14(9-16(21)25)36(4,34)35/h7-11,13H,5-6H2,1-4H3,(H2,27,28,29,30,31)
    Molecular weight 514.17 Da
    AlogP 3.9792200000000024
    HBond acceptors 10
    HBond donors 2
    Atoms 60

    Expert Reviews

    by SERP
    (on 28 May 2025 )
    Cellular Use Rating
    In Model Organisms
    I do agree with cellular concentrations 2 and 3 however not with cellular concentration 1. 51nM EC50 should be titrated higher than 100nM
    by SERP
    (on 5 Jun 2025 )
    Cellular Use Rating
    In Model Organisms
    The compound appears to be selective vs Plk4 and therefore should be suitable for dosing above 100 nM, which only represents 2x above it's cellular IC50. I would anticipate dosing up to at least IC90 /...
    by SERP
    (on 5 Jun 2025 )
    Cellular Use Rating
    In Model Organisms
    ( The reviewer did not leave any comments )
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