research use only

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.
Jump to

Quality Control

Batch: Purity: 99.99%
99.99

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
Dilution Calculator Molecular Weight Calculator

In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

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

mg/kg
g
μL

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)
CAS No. 1446261-44-4 -- Storage of Stock Solutions

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

Read more about storage stability stock solution CAS number SMILES

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

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2026-03-04)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05526924 RECRUITING
Head and Neck Cancer; Head and Neck Squamous Cell Carcinoma; Head and Neck Carcinoma; Head and Neck Cancer Stage IV; Head and Neck Cancers - Throat
University of Chicago
2023-03-07 PHASE1
NCT06692491 NOT_YET_RECRUITING
Rare Tumour
Peking University Shenzhen Hospital
2025-01-01 PHASE2
NCT04796454 WITHDRAWN
Platinum-Sensitive Biliary Tract Cancer
European Organisation for Research and Treatment of Cancer - EORTC
2022-05 PHASE2
NCT04164199 COMPLETED
Advanced Malignancies
BeOne Medicines
2019-12-19 PHASE3
NCT05038839 COMPLETED
Advanced Malignant Solid Neoplasm; Refractory Malignant Solid Neoplasm
M.D. Anderson Cancer Center
2022-02-09 PHASE1
NCT06387056 RECRUITING
Locally Advanced Prostate Cancer; Oligometastatic Prostate Cancer
The First Affiliated Hospital of Xiamen University
2024-04-01 PHASE2

Read more about Clinical Trials

Tech Support

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

Signaling Pathway Map