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Pamiparib PARP inhibitor

Name: Pamiparib
Brand: Selleck Chemicals
SKU: S8592
Availability: InStock
Rating: 5 (10 reviews)

Cat.No.S8592

Pamiparib is a potent and selective inhibitor of PARP1 and PARP2 with IC50 values of 0.83 and 0.11 nM, respectively in biochemical assays. It shows high selectivity over other PARP enzymes.

Chemical Structure

Molecular Weight: 298.31

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Quality Control

Batch: Purity: 99.99%

99.99

Related Targets	HDAC ATM/ATR DNA-PK WRN DNA/RNA Synthesis Topoisomerase PPAR Sirtuin Casein Kinase eIF
Other PARP Inhibitors	XAV-939 AZD5305 (Saruparib) Veliparib (ABT-888) PJ34 HCl AG-14361 Iniparib (BSI-201) G007-LK UPF 1069 A-966492 Stenoparib (E7449)

Solubility

In vitro
Batch:

DMSO : 59 mg/mL (197.78 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 45 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection 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.
	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.	3.000mg/ml (10.06mM)
	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.700mg/ml (2.35mM)
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.

Chemical Information, Storage & Stability

Molecular Weight	298.31	Formula	C₁₆H₁₅FN₄O	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	1446261-44-4	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	BGB-290			Smiles	CC12CCCN1CC3=NNC(=O)C4=C5C3=C2NC5=CC(=C4)F

Mechanism of Action

Targets/IC₅₀/Ki	PARP2 (Cell-free assay) 0.11 nM PARP1 (Cell-free assay) 0.83 nM
In vitro	BGB-290 shows potent DNA-trapping activity with IC50 of 13 nM. In the cellular assays, BGB-290 inhibits intracellular PAR formation with an IC50 of 0.24 nM.
In vivo	Oral administration of BGB-290 results in time-dependent and dose-dependent inhibition of PARylation in MDA-MB-436 (BRCA1 mutant) breast cancer xenograft, correlating well with the tumor drug concentrations. BGB-290 has also demonstrated good combination activity with chemotherapeutics in patient biopsy derived SCLC models. BGB-290 has significant brain penetration in C57 mice. The drug exposure in brain vs. that in plasma was close to 20% after oral administration of BGB-290.
References	[1] http://cancerres.aacrjournals.org/content/75/15_Supplement/1653 [2] http://cancerres.aacrjournals.org/content/75/15_Supplement/1651 [3] https://aacrjournals.org/cancerres/article-split/75/15_Supplement/3505/602723/Abstract-3505-Inhibition-of-PARP-activity-by-BGB

Clinical Trial Information

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

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT05376722	Recruiting	Neoadjuvant Therapy	Hongqian Guo\|First Affiliated Hospital of Zhejiang University\|The First Affiliated Hospital of Soochow University\|Nanjing First Hospital Nanjing Medical University\|The Affiliated Nanjing Drum Tower Hospital of Nanjing University Medical School	February 22 2022	Phase 2
NCT04985721	Recruiting	Cancer	Peter MacCallum Cancer Centre Australia	February 24 2022	Phase 2
NCT03991494	Completed	Advanced Solid Tumors	BeiGene	May 29 2019	Phase 1

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