尼拉帕尼|T3231

Niraparib
1038915-60-4

￥223 1mg 起订

￥513 5mg 起订

￥739 10mg 起订

上海更新日期：2024-12-02

TargetMol中国（陶术生物）

VIP12年

联系人：邵小姐

电话：021-021-33632979拨打

手机：15002134094 拨打

邮箱：marketing@targetmol.com

产品详情:

中文名称：: 尼拉帕尼

英文名称：: Niraparib

CAS号：: 1038915-60-4

品牌：: TargetMol

产地：: 美国

保存条件：: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

纯度规格：: 99.91%

产品类别：: 抑制剂

货号：: T3231

Product Introduction

Bioactivity

名称	Niraparib
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.
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)
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].
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]
存储条件	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice.
溶解度	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.
关键字	breast \| DNA \| damage \| inhibit \| cancer \| anti-tumor \| poly ADP ribose polymerase \| bioavailable \| Niraparib \| PARP \| orally \| Apoptosis \| Inhibitor \| lung \| ovarian \| MK4827 \| MK 4827
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尼拉帕尼|||MK-4827|TargetMol

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成立日期	(12年)
注册资本	566.2651万人民币
员工人数	100-500人
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经营模式	贸易,试剂,定制,服务
主营行业	化学试剂,生物活性小分子