Home DNA Damage/DNA Repair PARP inhibitor Saruparib (AZD5305) For research use only.

Saruparib (AZD5305)

Saruparib (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).

Saruparib (AZD5305) Chemical Structure

Saruparib (AZD5305) Chemical Structure

CAS No. 2589531-76-8

Purity & Quality Control

Products often used together with Saruparib (AZD5305)

KSQ-4279

AZD5305 and KSQ-4279 combination use exhibits significantly greater and more durable anti-tumor activity, including regressions compared to single agents.

Tobin E, et al. Cancer Res (2023) 83 (7_Supplement): 1581.

Saruparib (AZD5305) Related Products

Signaling Pathway

PARP Signaling Pathways

PARP Signaling Pathway

Biological Activity

Description Saruparib (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
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.

[2]
Cell Research Cell lines DLD-1 cells, BRCA2 (-/-) DLD-1 cells
Concentrations 0.0001-10 μM
Incubation Time 7 days
Method

DLD-1 and BRCA2(-/-) DLD-1 cells are harvested to a density of 5000 cells/mL and 2.5 × 104 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. 
In Vivo
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>
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05797168 Recruiting
Ovarian Cancer|Lung Adenocarcinoma
AstraZeneca
 June 5 2023 Phase 1|Phase 2

Chemical Information & Solubility

Molecular Weight 406.48 Formula

C22H26N6O2
CAS No. 2589531-76-8 SDF --
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 20 mg/mL ( (49.2 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 2 mg/mL

Water : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

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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