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PLK4-IN-25 | PLK4-IN-25 : Inhibitor of PLK4
RATINGS:
Cellular Use: (2 reviews)

In Model Organisms: (2 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
  • IC50:7.9 ± 4.0 nM
  • EC50:59 ± 2.5 nM
  • EC50:88 ± 37 nM
Inhibitor
up to 500 nM

Selectivity

In Vitro Selectivity Assessment
Potency Assay Off-Target:
Eurofins KinaseProfile Selectivity Panel Data for Compound 25 at 1 µM
Selectivity Assessment Description:
A Eurofins KinaseProfiler selectivity panel containing 435 kinases was conducted to gain additional ...
In Vitro Selectivity Assessment
Potency Assay Off-Target:
Biochemical assays with recombinant AURKB (ADP-Glo IC50 653 nM) and KDR (HTRF IC50 1600 nM ) confirm ...

Potency
Cellular
In Vitro

PLK4

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1021/acs.jmedchem.5c02200

In Vivo Validations

Mouse
Dose: 30 mg/Kg
Route of delivery: Oral
Cmax: 5.1 uM
Tmax: 0.5 h
Area Under the Curve:: 28 μM h

DOI Reference: 10.1021/acs.jmedchem.5c02200

Dose: 100 mg/Kg
Route of delivery: Oral
Cmax: 11 uM
Tmax: 10 h
Area Under the Curve:: 80 μM h

DOI Reference: 10.1021/acs.jmedchem.5c02200

Chemical Information

Molecular Formula C20H19F6N7O2
SMILEs O=C(Nc1c[nH]nc1-c1cc2c(cn1)cnn2CC(F)(F)F)N1CC[C@](O)(C(F)(F)F)CC12CC2
InChI InChI=1S/C20H19F6N7O2/c21-19(22,23)10-33-14-5-12(27-6-11(14)7-29-33)15-13(8-28-31-15)30-16(34)32-4-3-18(35,20(24,25)26)9-17(32)1-2-17/h5-8,35H,1-4,9-10H2,(H,28,31)(H,30,34)/t18-/m1/s1
Molecular weight 503.15 Da
AlogP 3.8374000000000024
HBond acceptors 9
HBond donors 3
Atoms 54

References

Publications

Cross References

Expert Reviews

by SERP
(on 17 Dec 2025 )
Cellular Use Rating
In Model Organisms
A good and pretty selective PLK4 inhibitor. The Eurofins Kinome selectivity panel showed 50% inhibition or higher for 8.5% of kinome at 1 micromolar concentration. These potential off targets were not...
by SERP
(on 9 Feb 2026 )
Cellular Use Rating
In Model Organisms
This is a reasonable PLK4 probe with a recommended maximum in vitro concentration of 100 nM, corresponding to ~1.7× EC50 (NanoBRET). This concentration provides solid engagement while still staying well...
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