Pamiparib (BGB-290)

Catalog No.S8592

For research use only.

Pamiparib (BGB-290) 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 (BGB-290) Chemical Structure

CAS No. 1446261-44-4

Selleck's Pamiparib (BGB-290) has been cited by 4 Publications

Purity & Quality Control

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Biological Activity

Description Pamiparib (BGB-290) 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

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].

Protocol (from reference)

Solubility (25°C)

In vitro

DMSO 59 mg/mL
(197.78 mM)
Ethanol 45 mg/mL
(150.84 mM)
Water Insoluble

Chemical Information

Molecular Weight 298.31
Formula

C16H15FN4O

CAS No. 1446261-44-4
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC12CCCN1CC3=NNC(=O)C4=C5C3=C2NC5=CC(=C4)F

In vivo Formulation Calculator (Clear solution)

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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.

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.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04985721 Not yet recruiting Drug: Pamiparib|Drug: Tislelizumab Cancer Peter MacCallum Cancer Centre Australia August 1 2021 Phase 2
NCT03991494 Completed Drug: [14C]-pamiparib Advanced Solid Tumors BeiGene May 29 2019 Phase 1
NCT03427814 Active not recruiting Drug: pamiparib|Drug: Placebo Advanced or Inoperable Gastric Cancer BeiGene July 23 2018 Phase 2
NCT03150862 Completed Drug: Pamiparib|Drug: TMZ|Radiation: Radiation Brain and Central Nervous System Tumors BeiGene USA Inc.|BeiGene August 1 2017 Phase 1|Phase 2
NCT03150810 Recruiting Drug: Pamiparib|Drug: Temozolomide Locally Advanced or Metastatic Solid Tumors BeiGene|Myriad Genetics Inc. June 28 2017 Phase 1|Phase 2

(data from https://clinicaltrials.gov, updated on 2022-01-17)

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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