Pamiparib

Pamiparib (BGB-290) is an orally active, potent, highly selective PARP inhibitor, with IC50 values of 0.9 nM and 0.5 nM for PARP1 and PARP2, respectively. Pamiparib has potent PARP trapping, and capability to penetrate the brain, and can be used for the research of various cancers including the solid tumor[1][2].

Product Specifications

CAS Number

[1446261-44-4]

Product Name Alternative

BGB-290

UNSPSC

12352005

Hazard Statement

H315, H319, H320

Target

PARP

Type

Reference compound

Related Pathways

Cell Cycle/DNA Damage; Epigenetics

Applications

Cancer-programmed cell death

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/Pamiparib.html

Purity

99.96

Solubility

DMSO : 50 mg/mL (ultrasonic)

Smiles

O=C1NN=C2CN(CCC3)[C@@]3(C)C(N4)=C2C5=C4C=C(F)C=C51

Molecular Formula

C16H15FN4O

Molecular Weight

298.32

Precautions

H315, H319, H320

References & Citations

[1]Changyou Zhou, et al. Fused tetra or penta-cyclic dihydrodiazepinocarbazolones as parp inhibitors. WO 2013097225 A1.|[2]Friedlander M, et al. Pamiparib in combination with tislelizumab in patients with advanced solid tumours: results from the dose-escalation stage of a multicentre, open-label, phase 1a/b trial. Lancet Oncol. 2019 Sep;20 (9) :1306-1315.|[3]Zhiyu Tang, et al. Abstract 1653: BGB-290: A highly potent and specific PARP1/2 inhibitor potentiates anti-tumor activity of chemotherapeutics in patient biopsy derived SCLC models. Cancer Research. August 2015, Volume 75, Issue 15.|[4]Shiv K. Gupta, et al. Abstract 3505: Inhibition of PARP activity by BGB-290 potentiates efficacy of NSC 362856 in patient derived xenografts of glioblastoma multiforme. Cancer Research. August 2015, Volume 75, Issue 15