Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 336 | 现货 | ||
2 mg | ¥ 478 | 现货 | ||
5 mg | ¥ 729 | 现货 | ||
10 mg | ¥ 1,230 | 现货 | ||
25 mg | ¥ 1,980 | 现货 | ||
50 mg | ¥ 3,730 | 现货 | ||
100 mg | ¥ 5,380 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 821 | 现货 |
产品描述 | Pamiparib (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 |
靶点活性 | PARP2:0.5 nM, PARP1:0.9 nM |
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]. |
别名 | BGB-290 |
分子量 | 298.31 |
分子式 | C16H15FN4O |
CAS No. | 1446261-44-4 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 62.5 mg/mL (209.51 mM), Sonication is recommended.
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 3.3522 mL | 16.7611 mL | 33.5222 mL | 83.8054 mL |
5 mM | 0.6704 mL | 3.3522 mL | 6.7044 mL | 16.7611 mL | |
10 mM | 0.3352 mL | 1.6761 mL | 3.3522 mL | 8.3805 mL | |
20 mM | 0.1676 mL | 0.8381 mL | 1.6761 mL | 4.1903 mL | |
50 mM | 0.067 mL | 0.3352 mL | 0.6704 mL | 1.6761 mL | |
100 mM | 0.0335 mL | 0.1676 mL | 0.3352 mL | 0.8381 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
Pamiparib 1446261-44-4 Chromatin/Epigenetic DNA Damage/DNA Repair PARP inhibit Inhibitor BGB-290 poly ADP ribose polymerase BGB 290 BGB290 inhibitor