AZD5305

Catalog No.S9875

For research use only.

AZD5305 is a highly selective and potent inhibitor of PARP1 with an IC50 of 3 nM in wild-type A549 lung cancer cells. AZD5305 shows no or minimal growth inhibitory effects in other cells (IC50s >10μM).

AZD5305 Chemical Structure

CAS No. 2589531-76-8

Purity & Quality Control

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Biological Activity

Description AZD5305 is a highly selective and potent inhibitor of PARP1 with an IC50 of 3 nM in wild-type A549 lung cancer cells. AZD5305 shows no or minimal growth inhibitory effects in other cells (IC50s >10μM).
Targets
PARP1 [1]
(in wild-type A549 lung cancer cells)
3 nM
In vitro

AZD5305 is highly selective inhibitor for PARP1 over other PARP family members, with good secondary pharmacology and physicochemical properties and excellent pharmacokinetics in preclinical species. AZD5305 reduces anti-proliferation effects on human bone marrow progenitor cells in vitro.<sup><a class="sref" href="#s_ref">[2]</a></sup>

In vivo

AZD5305 is a potent and selective PARP1 inhibitor and PARP1–DNA trapper with excellent in vivo efficacy in a BRCA mutant HBCx-17 PDX model.<sup><a class="sref" href="#s_ref">[2]</a></sup>

Protocol (from reference)

Cell Research:

<sup><a class="sref" href="#s_ref">[2]</a></sup>

  • Cell lines: DLD-1 cells, BRCA2 (-/-) DLD-1 cells
  • Concentrations: 0.0001-10 μM
  • Incubation Time: 7 days
  • Method:

    DLD-1 and BRCA2<sup>(-/-)</sup> DLD-1 cells are harvested to a density of 5000 cells/mL and 2.5 × 10<sup>4</sup> cells/mL, respectively, in complete media, 40 μL/well seeded into 384-well plates using a Multidrop Combi then incubated at 37 °C, 5% CO2 overnight. The next day (day 1) using a Multidrop Combi, sytox green (5 μL, 2 μM) and saponin (10 μL, 0.25% stock) to a day 0 plate are added, the plate is sealed using a black adhesive lid and incubated for >3 h at rt. Cells are imaged using Cell Insight fitted with a 4× objective. AZD5305 is added using an Echo 555 and placed in an incubator maintained at 37 °C, 5% CO2 and incubated for 7 days. On day 8, sytox green (5 μL, 2 μM) and then saponin (10 μL, 0.25% stock) is added to plates, the plate is sealed using a black adhesive lid and incubated for >3 h at rt. All cells are read on a Cell Insight with 4× Objective. 

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 406.48
Formula

C22H26N6O2

CAS No. 2589531-76-8
Storage 3 years -20°C powder
2 years -80°C in solvent

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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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