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。

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

Pamiparib, an investigational Poly (ADP-ribose) polymerase (PARP) inhibitor in clinical development, demonstrates excellent selectivity for both PARP1 and PARP2, and superb anti-proliferation activities in tumor cell lines with BRCA1/2 mutations or HR pathway deficiency (HRD).?Pamiparib has good bioavailability and is 16-fold more potent than olaparib in an efficacy study using BRCA1 mutated MDA-MB-436 breast cancer xenograft model.?Pamiparib also shows strong anti-tumor synergy with temozolomide (TMZ), a DNA alkylating agent used to treat brain tumors.?Compared to other PARP inhibitors, pamiparib demonstrated improved penetration across the blood brain barrier (BBB) in mice.?Oral administration of pamiparib at a dose as low as 3 mg/kg is sufficient to abrogate PARylation in brain tumor tissues.?In SCLC-derived, TMZ-resistant H209 intracranial xenograft model, combination of pamiparib with TMZ overcomes its resistance and shows significant tumor inhibitory effects and prolonged life span[1].

1446261-44-4

C16H15FN4O

298.321

BGB-290

DMSO:62.5 mg/mL (209.51 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years