aladdin 阿拉丁 P414075 帕米帕里布（BGB-290） 1446261-44-4 99%

中文名：帕米帕里布（BGB-290）

英文名：Pamiparib (BGB-290)

纯度：Moligand™，≥99%

货号：P414075

Cas号：1446261-44-4

存储温度：-20°C储存

运输条件：超低温运输

产品介绍：

Information

Pamiparib (BGB-290) is a potent and selective inhibitor ofPARP1andPARP2with IC50 values of 0.83 and 0.11 nM, respectively in biochemical assays. It shows high selectivity over other PARP enzymes.

Targets

PARP2 (Cell-free assay); PARP1 (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.

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.

Product Application：

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.

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