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Niraparib

产品编号 T3231Cas号 1038915-60-4
别名 尼拉帕尼, MK-4827

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。

Niraparib

Niraparib

纯度: 99.91%
产品编号 T3231 别名 尼拉帕尼, MK-4827Cas号 1038915-60-4

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。

规格价格库存数量
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 x 10 mM (in DMSO)¥ 563现货
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纯度:99.91%
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产品介绍

生物活性
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
PARP1:3.8 nM, PARP2:2.1 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
化学信息
分子量320.39
分子式C19H20N4O
CAS No.1038915-60-4
储存&溶解度
存储Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
溶解度信息
Ethanol: 60 mg/mL (187.3 mM)
H2O: < 1 mg/mL (insoluble or slightly soluble)
10% DMSO+40% PEG300+5% Tween 80+45% Saline: 6 mg/mL (18.73 mM), Please add co-solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately.
DMSO: 16.67 mg/mL (52.02 mM), Sonication is recommended.
溶液配制表
10% DMSO+40% PEG300+5% Tween 80+45% Saline/DMSO/Ethanol
1mg5mg10mg50mg
1 mM3.1212 mL15.6060 mL31.2120 mL156.0598 mL
5 mM0.6242 mL3.1212 mL6.2424 mL31.2120 mL
10 mM0.3121 mL1.5606 mL3.1212 mL15.6060 mL
DMSO/Ethanol
1mg5mg10mg50mg
20 mM0.1561 mL0.7803 mL1.5606 mL7.8030 mL
50 mM0.0624 mL0.3121 mL0.6242 mL3.1212 mL
Ethanol
1mg5mg10mg50mg
100 mM0.0312 mL0.1561 mL0.3121 mL1.5606 mL

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TargetMol | Animal experiments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 μLTargetMol | Animal experiments 一共给药动物 10 只 ,您使用的配方为 5% TargetMol | reagent DMSO+ 30%PEG300+ 5%Tween 80 + 60% ddH2O. 那么您的工作液浓度为 2 mg/mL
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体内配方的制备方法:50μLDMSOTargetMol | reagent 母液,添加 300 μLPEG300TargetMol | reagent 混匀澄清,再加 50μLTween 80, 混匀澄清,再加 600μLddH2OTargetMol | reagent 混匀澄清

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