bgb-290

Pamiparib (BGB-290) 是一种具有口服活性、强效、高选择性的 PARP 抑制剂，对PARP1和PARP2的IC50值分别为 0.9 nM 和 0.5 nM。它具有强大的 PARP 捕获能力，具有穿透大脑的能力，可用于研究癌症。

Pamiparib is a highly potent and selective PARP inhibitor. BGB-290 selectively binds to PARP and prevents PARP-mediated repair of single-strand DNA breaks via the base-excision repair (BER) pathway. This enhances the accumulation of DNA strand breaks, pro

4-Fluorophenibut (developmental code name CGP-11130; also known as β-(4-fluorophenyl)-γ-aminobutyric acid or β-(4-fluorophenyl)-GABA) is a GABAB receptor agonist which was never marketed. It is selective for the GABAB receptor over the GABAA receptor (IC50 = 1.70 μM and > 100 μM, respectively). The drug is a GABA analogue and is closely related to baclofen (β-(4-chlorophenyl)-GABA), tolibut (β-(4-methylphenyl)-GABA), and phenibut (β-phenyl-GABA). It is less potent as a GABAB receptor agonist than baclofen but more potent than phenibut.

Pamiparib, also known as BGB-290, is a highly potent and selective PARP inhibitor with favorable drug metabolism and pharmacokinetic properties. BGB-290 selectively binds to PARP and prevents PARP-mediated repair of single-strand DNA breaks via the base-excision repair (BER) pathway. This enhances the accumulation of DNA strand breaks, promotes genomic instability, and eventually leads to apoptosis. BGB-290 may both potentiate the cytotoxicity of DNA-damaging agents and reverse tumor cell chemo- and radioresistance.