Pamiparib

Catalog No.S8592 Batch:S859201

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Technical Data

Formula

C16H15FN4O
Molecular Weight 298.31 CAS No. 1446261-44-4
Solubility (25°C)* In vitro DMSO 59 mg/mL (197.78 mM)
Ethanol 45 mg/mL (150.84 mM)
Water Insoluble
In vivo (Add solvents to the product individually and in order)
5% DMSO 95% Corn oil
0.7mg/ml
5%DMSO 40%PEG300 5%Tween80 50%ddH2O
3.0mg/ml
* <1 mg/ml means slightly soluble or 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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

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

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)

Selleck's Pamiparib has been cited by 10 publications

Aggregability of the SQSTM1/p62-based aggresome-like induced structures determines the sensitivity to parthanatos [ Cell Death Discov, 2024, 10(1):74] PubMed: 38346947
Zinc Finger MYND-Type Containing 8 (ZMYND8) Is Epigenetically Regulated in Mutant Isocitrate Dehydrogenase 1 (IDH1) Glioma to Promote Radioresistance [ Clin Cancer Res, 2023, 29(9):1763-1782] PubMed: 36692427
Class I HDAC inhibition reduces DNA damage repair capacity of MYC-amplified medulloblastoma cells [ J Neurooncol, 2023, 164(3):617-632] PubMed: 37783879
Class I HDAC inhibition reduces DNA damage repair capacity of MYC-amplified medulloblastoma cells [ J Neurooncol, 2023, 164(3):617-632] PubMed: 37783879
PARP-mediated PARylation of MGMT is critical to promote repair of temozolomide-induced O6-methylguanine DNA damage in glioblastoma [ Neuro Oncol, 2021, 23(6):920-931] PubMed: 33433610
A pan-cancer organoid platform for precision medicine [ Cell Rep, 2021, 36(4):109429] PubMed: 34320344
Pharmacological Poly (ADP-Ribose) Polymerase Inhibitors Decrease Mycobacterium tuberculosis Survival in Human Macrophages [ Front Immunol, 2021, 12:712021] PubMed: 34899683
Pharmacological Poly (ADP-Ribose) Polymerase Inhibitors Decrease Mycobacterium tuberculosis Survival in Human Macrophages [ Front Immunol, 2021, 12:712021] PubMed: 34899683
EGFR Amplification Induces Increased DNA Damage Response and Renders Selective Sensitivity to Talazoparib (PARP Inhibitor) in Glioblastoma [ Clin Cancer Res, 2020, 26(6):1395-1407] PubMed: 31852834
EGFR amplification induces increased DNA damage response and renders selective sensitivity to Talazoparib (PARP inhibitor) in glioblastoma. [ Clin Cancer Res, 2019, 10.1158/1078-0432.CCR-19-2549] PubMed: 31852834

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.