AZD9574

AZD9574 : Inhibitor of PARP1

Structure

SERP Rating

In Cells

(1 ratings)

In Model Organisms

(1 ratings)

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Probe AZD9574 is in the process of SERP review.

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Information

PARP1

Inhibitor

up to 100 nM

Probe Availability:

In Vitro Validations

Uniprot ID: P09874

Target Class: Other post-translational modification

Target SubClass: PARP

Potency: IC50

Potency Value: 5.5 nM

Potency Assay: fluorescence anisotropy assay

PDB ID for probe-target interaction (3D structure): --

Target aliases:

Poly [ADP-ribose] polymerase 1, PPOL, ADPRT, PARP1 ...

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

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Potency assay (off target): AZD9574 demonstrated potent binding to PARP1 measured by fluorescence anisotropy, showing significantly greater selectivity over PARP2 (>8000-fold) and other PARPs (>18000-fold).

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SERP ratings and comments

SERP Ratings

In Cell Rating

In Model Organisms

SERP Comments:

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 to use it not only for subcutaneous injection but also for oral administration.

(last updated: 12 Feb 2024 )