Pamiparib (BGB-290)

For research use only.

Catalog No.S8592

3 publications

Pamiparib (BGB-290) Chemical Structure

CAS No. 1446261-44-4

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.

Selleck's Pamiparib (BGB-290) has been cited by 3 publications

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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

Solubility (25°C)

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

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 298.31
Formula

C16H15FN4O

CAS No. 1446261-44-4
Storage powder
in solvent
Synonyms N/A
Smiles CC12CCCN1CC3=NNC(=O)C4=C5C3=C2NC5=CC(=C4)F

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Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
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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 June 18 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

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.

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PARP Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID