research use only

Saruparib (AZD5305) PARP inhibitor

Name: Saruparib (AZD5305)
Brand: Selleck Chemicals
SKU: S9875
Availability: InStock
Rating: 5 (4 reviews)

Cat.No.S9875

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

Chemical Structure

Molecular Weight: 406.48

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: Purity: 99.79%

99.79

Products Often Used Together with Saruparib (AZD5305)

KSQ-4279

The combination of this compound and KSQ-4279 exhibits significantly greater and more durable anti-tumor activity, including regressions compared to single agents.

Related Targets	DNA/RNA Synthesis HDAC Topoisomerase PPAR Sirtuin ATM/ATR Casein Kinase eIF MDM2/MDMX DNA-PK DNA alkylator DHFR Telomerase Nucleoside Analog/Antimetabolite Thymidylate Synthase CRISPR/Cas9 RAD51 BMI-1 LIM kinase RNR NUDIX High-mobility Group OGG1 Alkylating Agent MTH1 G-quadruplex SMN FENs WRN Pax
Related Products	XAV-939 Veliparib (ABT-888) PJ34 HCl AG-14361 Iniparib (BSI-201) A-966492 G007-LK UPF 1069 AZD2461 Pamiparib ME0328 3-Aminobenzamide NMS-P118 Stenoparib (E7449) NVP-TNKS656 WIKI4 Benzamide BGP-15 2HCl NU1025 BYK204165 Fluzoparib (SHR-3162) Picolinamide

Chemical Information, Storage & Stability

Molecular Weight	406.48	Formula	C₂₂H₂₆N₆O₂	Storage (From the date of receipt)	3 years -20°C powder
CAS No.	2589531-76-8	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent

Solubility

In vitro
Batch:

DMSO : 16 mg/mL ( (39.36 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 10 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.800mg/ml (1.97mM)	Taking the 1 mL working solution as an example, add 50 μL of 16 mg/ml clarified DMSO stock solution to 400 μL PEG300, mix evenly to clarify it; add 50 μL Tween-80 to the above system, mix evenly to clarify it; then continue to add 500 μL ddH2O Dilute to 1 mL. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

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.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC₅₀/Ki	PARP1 ^[1] (in wild-type A549 lung cancer cells) 3 nM
In vitro	Saruparib (AZD5305) is a highly selective inhibitor for PARP1 over other PARP family members, with good secondary pharmacology and physicochemical properties and excellent pharmacokinetics in preclinical species. It reduces anti-proliferation effects on human bone marrow progenitor cells in vitro. ^[2]
In vivo	Saruparib (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.^[2]
References	https://pubmed.ncbi.nlm.nih.gov/34904816/ https://pubmed.ncbi.nlm.nih.gov/34570508/ https://pubmed.ncbi.nlm.nih.gov/35929986/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT05797168	Recruiting	Ovarian Cancer\|Lung Adenocarcinoma	AstraZeneca	June 5 2023	Phase 1\|Phase 2

Tech Support

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):