化合物BGB-290 T5058

Product Introduction
Bioactivity


英文名: Pamiparib

描述: 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。

体内活性: 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].

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 62.5 mg/mL (209.51 mM)


关键字: inhibit | PARP | Inhibitor | poly ADP ribose polymerase | Pamiparib | BGB 290 | BGB290

相关产品: PARP1-IN-14 | PARP1-IN-15 | Lupiwighteone | Fucosterol | PARP-1-IN-3 | Lerzeparib | Furanodiene | Niraparib hydrochloride | Verbascoside | Zingiberen newsaponin

相关库: Drug Repurposing Compound Library | Approved Drug Library | Anti-Cancer Drug Library | Clinical Compound Library | Bioactive Compounds Library Max | Anti-Cancer Clinical Compound Library | Inhibitor Library | Anti-Cancer Active Compound Library | Highly Selective Inhibitor Library | Anti-Cancer Approved Drug Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途