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AZD9574 | AZD9574 : Inhibitor of PARP1
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
PARP1
  • IC50:5.5 nM
  • IC50:1.5 nM
  • IC50:2 nM
  • IC50:4.7 nM
Inhibitor
up to 100 nM

Selectivity

In Vitro Selectivity Assessment
Potency Assay Off-Target:
AZD9574 demonstrated potent binding to PARP1 measured by fluorescence anisotropy, showing significan ...

Potency
Cellular
In Vitro

PARP1

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1158/1078-0432.CCR-23-2094

In Vivo Validations

Mouse
Dose: 0.3, 3.0, 30.0 mg/Kg
Route of delivery: Subcutaneous

DOI Reference: 10.1158/1078-0432.CCR-23-2094

Chemical Information

Molecular Formula C21H22F2N6O2
SMILEs CNC(=O)c1ccc(N2CCN(Cc3ccc4nc(C)c(=O)[nH]c4c3F)CC2)c(F)n1
InChI InChI=1S/C21H22F2N6O2/c1-12-20(30)27-18-14(25-12)4-3-13(17(18)22)11-28-7-9-29(10-8-28)16-6-5-15(21(31)24-2)26-19(16)23/h3-6H,7-11H2,1-2H3,(H,24,31)(H,27,30)
Molecular weight 428.18 Da
AlogP 0.0
HBond acceptors 8
HBond donors 2
Atoms 53

References

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Expert Reviews

by SERP
(on 12 Feb 2024 )
Cellular Use Rating
In Model Organisms
I believe that AZD9574 is one of the best PARP inhibitors to evaluate the PARP1 selective inhibition. In addition, this compound showed acceptable oral bioavailability so it is possible to recommended...
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