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- CAS号：
1038915-73-9
- 规格：
1mLx10mM(inDMSO)/1mg/5mg/10mg/25mg/50mg/100mg
| 规格： | 1mLx10mM(inDMSO) | 产品价格： | ￥444.0 |
|---|---|---|---|
| 规格： | 1mg | 产品价格： | ￥191.0 |
| 规格： | 5mg | 产品价格： | ￥397.0 |
| 规格： | 10mg | 产品价格： | ￥586.0 |
| 规格： | 25mg | 产品价格： | ￥896.0 |
| 规格： | 50mg | 产品价格： | ￥1256.0 |
| 规格： | 100mg | 产品价格： | ￥1864.0 |
Product Introduction
Bioactivity
| 名称 | Niraparib tosylate |
| 描述 | Niraparib tosylate (MK-4827 (tosylate))(with IC50 of 3.8 nM/2.1 nM) is a selective PARP1/PARP2 inhibitor. |
| 细胞实验 | V-C8 (BRCA2-negative) Chinese hamster cells are treated with the PARP inhibitor MK-4827 for 24 h, washed and incubated in drug-free medium for 5-7 days until colonies formed. (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 | 微摩尔浓度的Niraparib（尼拉帕利）对来源于肺癌、乳腺癌和前列腺癌的肿瘤细胞系进行放射增敏，其作用与p53状态无关，但对来源于正常组织的细胞系无效。Niraparib还能使肿瘤细胞对Water2敏感，并在DNA复制过程中将Water2引起的单链断裂（SSBs）转化为双链断裂（DSBs）[5]。 |
| 体内活性 | Niraparib tosylate显著增强了放射线对各种人类肿瘤异种移植物（包括p53野生型和p53突变型）的作用效果。Niraparib tosylate在给药后1小时内降低了肿瘤中的PAR水平，并且这种效果持续了至多24小时[1]。与单一疗法相比，联合使用Niraparib tosylate和放射线治疗能显著延长存活时间（p<0.01）。通过与单一疗法组相比，联合治疗组肿瘤中裂解的caspase-3和γ-H2AX显著升高，进一步证明了Niraparib tosylate加放射线治疗的体内优势[4]。 |
| 存储条件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. |
| 溶解度 | Ethanol : < 1 mg/mL (insoluble or slightly soluble) DMSO : 91 mg/mL (184.74 mM), Sonication is recommended. H2O : < 1 mg/mL (insoluble or slightly soluble) |
| 关键字 | poly ADP ribose polymerase | PARP2 | PARP1 | PARP | ovarian | orally | Niraparib tosylate | Niraparib (MK-4827) Tosylate | Niraparib | MK-4827 Tosylate | MK4827 Tosylate | MK-4827 | MK4827 | MK 4827 Tosylate | MK 4827 | lung | Inhibitor | inhibit | DNA | damage | cancer | breast | bioavailable | Apoptosis | anti-tumor |
| 相关产品 | Formamide | Urea | Sodium Molybdate | Dimethyl phthalate | Aceglutamide | Alginic acid | Cysteamine hydrochloride | Metronidazole | Sildenafil citrate | Citric Acid Triammonium | Stavudine | Tamoxifen |
| 相关库 | Inhibitor Library | Bioactive Compound Library | Anti-Cancer Active Compound Library | Anti-Cancer Approved Drug Library | Bioactive Compounds Library Max | Anti-Pancreatic Cancer Compound Library | EMA Approved Drug Library | Anti-Aging Compound Library | FDA-Approved Drug Library | Drug Repurposing Compound Library | Anti-Cancer Clinical Compound Library | Anti-Cancer Drug Library |
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尼拉帕尼对苯甲磺酸盐【1038915-73-9】
￥191 - 1864
