Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Niraparib (MK-4827) 是一种 PARP 抑制剂,可以抑制 PARP1 和 PARP2 (IC50=3.8/2.1 nM),具有选择性。Niraparib 具有抗肿瘤活性,可以抑制 DNA 损伤修复、诱导细胞凋亡。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 223 | 现货 | ||
5 mg | ¥ 513 | 现货 | ||
10 mg | ¥ 739 | 现货 | ||
25 mg | ¥ 1,130 | 现货 | ||
50 mg | ¥ 1,580 | 现货 | ||
100 mg | ¥ 2,350 | 现货 | ||
200 mg | ¥ 3,480 | 现货 | ||
500 mg | ¥ 5,290 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 563 | 现货 |
产品描述 | Niraparib (MK-4827) is a PARP inhibitor that selectively inhibits PARP1 and PARP2 (IC50=3.8/2.1 nM). Niraparib has antitumor activity, inhibits DNA damage repair, and induces apoptosis. |
靶点活性 | PARP2:2.1 nM, PARP1:3.8 nM |
体外活性 |
方法:PDAC 细胞系 MIA-PaCa-2、PANC-1、Capan-1 和 OvCa 细胞系 OVCAR8、PEO1 用 Niraparib (0.1-200 µM) 处理 48 h,使用 CellTiter-Glo Luminescent Cell Viability Assay 检测细胞活力。 结果:Niraparib 对 MIA-PaCa-2、PANC-1、Capan-1、OVCAR8、PEO1 细胞的 IC50 分别为 26 µm、50 µm、15 µM、20 µM 和 28 µM。[1] 方法:卵巢癌细胞 SKOV3 和 UWB1.289 用 Niraparib (0.5-15 µM) 处理 48 h,使用 Western Blot 方法检测靶点蛋白表达水平。 结果:Niraparib 上调了 SKOV3 和 UWB1.289 细胞中 PD-L1 的表达。[2] |
体内活性 |
方法:为检测体内抗肿瘤活性,将 Niraparib (25 mg/kg,口服给药,每周四次) 和 PD-L1 (10mg/kg,腹腔注射,每周两次) 给药给携带卵巢癌肿瘤 ID8 的 C57BL/6 小鼠,持续八周。 结果:Niraparib 在体内上调卵巢肿瘤的 PD-L1 表达,并与 PD-L1 阻断具有协同作用。[2] 方法:为检测体内抗肿瘤活性,将 Niraparib (50 mg/kg,0.5% methylcellulose) 灌胃给药给携带颅内人源性 TNBC 细胞系 SUM149、MDA-MB-231Br 或 MDA-MB-436 的 C57BL/6 小鼠,每天一次,持续两周。 结果:在 BRCA 突变型 MDA-MB-436 模型中,Niraparib 增加中位生存期和减少肿瘤负荷。但在 BRCA 突变型 SUM149 或 BRCA 野生型 MDA-MB-231Br 模型中不增加,尽管颅内肿瘤中存在高浓度。[3] |
激酶实验 | Enzyme assay is conducted in buffer containing 25 mM Tris, pH 8.0, 1 mM DTT, 1 mM spermine, 50 mM KCl, 0.01% Nonidet P-40, and 1 mM MgCl2. PARP reaction contains 0.1 μCi [3H]NAD+ (200?000 DPM), 1.5 μM NAD+, 150 nM biotinylated NAD+, 1 μg/mL activated calf thymus, and 1?5 nM PARP-1. Autoreactions utilizing SPA bead-based detection are carried out in 50 μL volumes in white 96-well plates. Compounds (e.g., MK-4827) are prepared in 11-point serial dilution in 96-well plate, 5 μL/well in 5% DMSO/Water (10× concentrated). Reactions are initiated by adding first 35 μL of PARP-1 enzyme in buffer and incubating for 5 min at room temperature and then 10 μL of NAD+ and DNA substrate mixture. After 3 h at room temperature, these reactions are terminated by the addition of 50 μL of streptavidin-SPA beads (2.5 mg/mL in 200 mM EDTA, pH 8). After 5 min, they are counted using a TopCount microplate scintillation counter. IC50 data is determined from inhibition curves at various substrate concentrations[1]. |
细胞实验 | Proliferation assays were conducted in 96-well black viewplates, and 300 cells/well (250 cell/well for BRCA-1 wt) in culture medium, 190 μL/well (DMEM containing 10% FCS, 0.1 mg/mL penicillin-streptomycin, and 2 mM L-glutamine), were plated and incubated for 4 h at 37℃ under 5% CO2 atmosphere. Inhibitors were then added with serial dilutions, 10 μL/well to obtain the desired final compound concentration in 0.5% DMSO. The cells were then incubated for 7 days at 37℃ in 5% CO2 after which time viability was assessed. Briefly, with CellTiter-Blue solution prediluted 1:10 in medium, 100 μL/well was added and the cells left for 45 min at 37℃ under 5% CO2 and then a further 15 min at room temperature in the dark. The number of living cells was determined by reading the plate at fluorimeter, excitation at 550 nm and emission at 590 nm. Cell growth was expressed as the percentage growth with respect to vehicle treated cells. The concentration required to inhibit cell growth by 50% (CC50) was determined.(Only for Reference) |
别名 | 尼拉帕尼, MK-4827 |
分子量 | 320.39 |
分子式 | C19H20N4O |
CAS No. | 1038915-60-4 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Ethanol: 60 mg/mL (187.3 mM)
H2O: < 1 mg/mL (insoluble or slightly soluble)
DMSO: 60 mg/mL (187.3 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
Ethanol / DMSO | 1 mM | 3.1212 mL | 15.606 mL | 31.212 mL | 78.0299 mL |
5 mM | 0.6242 mL | 3.1212 mL | 6.2424 mL | 15.606 mL | |
10 mM | 0.3121 mL | 1.5606 mL | 3.1212 mL | 7.803 mL | |
20 mM | 0.1561 mL | 0.7803 mL | 1.5606 mL | 3.9015 mL | |
50 mM | 0.0624 mL | 0.3121 mL | 0.6242 mL | 1.5606 mL | |
100 mM | 0.0312 mL | 0.1561 mL | 0.3121 mL | 0.7803 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。
Niraparib 1038915-60-4 Apoptosis Chromatin/Epigenetic DNA Damage/DNA Repair Others PARP breast 尼拉帕尼 DNA damage inhibit cancer anti-tumor poly ADP ribose polymerase bioavailable MK-4827 orally Inhibitor lung ovarian MK4827 MK 4827 inhibitor