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Pamiparib PARP inhibitor

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.
Pamiparib PARP inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 298.31

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Quality Control

Chemical Information, Storage & Stability

Molecular Weight 298.31 Formula

C16H15FN4O

 Storage (From the date of receipt)
CAS No. 1446261-44-4 -- Storage of Stock Solutions

Synonyms BGB-290 Smiles CC12CCCN1CC3=NNC(=O)C4=C5C3=C2NC5=CC(=C4)F

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

In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

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%
% Tween 80
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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
PARP2 [1]
(Cell-free assay)
0.11 nM
PARP1 [1]
(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[1].
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[1].

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[2].
References

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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