Home DNA Damage/DNA Repair PARP inhibitor Pamiparib For research use only.

Pamiparib

Synonyms: BGB-290

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 Chemical Structure

Pamiparib Chemical Structure

CAS No. 1446261-44-4

Purity & Quality Control

Pamiparib Related Products

Signaling Pathway

PARP Signaling Pathways

PARP Signaling Pathway

Biological Activity

Description 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.
Targets
PARP2 [1]
(Cell-free assay)		 PARP1 [1]
(Cell-free assay)
0.11 nM 0.83 nM
In vitro
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
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].
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

Chemical Information & Solubility

Molecular Weight 298.31 Formula

C16H15FN4O
CAS No. 1446261-44-4 SDF --
Smiles CC12CCCN1CC3=NNC(=O)C4=C5C3=C2NC5=CC(=C4)F
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 59 mg/mL ( (197.78 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 45 mg/mL

Water : Insoluble


Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.


In vivo Formulation Calculator

Preparing Stock Solutions

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo Formulation Calculator (Clear solution)

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

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% DMSO % % Tween 80 % ddH2O
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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.

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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