Niraparib tosylate NEW
| Price | $38 | $61 | $85 |
| Package | 2mg | 5mg | 10mg |
| Min. Order: | |
| Supply Ability: | 10g |
| Update Time: | 2024-11-17 |
Product Details
| Product Name: Niraparib tosylate | CAS No.: 1038915-73-9 |
| Purity: 99.87% | Supply Ability: 10g |
| Release date: 2024/11/17 |
Product Introduction
Bioactivity
| 名稱 | Niraparib tosylate |
| 描述 | Niraparib tosylate (MK-4827 (tosylate))(with IC50 of 3.8 nM/2.1 nM) is a selective PARP1/PARP2 inhibitor. |
| 細(xì)胞實(shí)驗(yàn) | 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) |
| 激酶實(shí)驗(yàn) | 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]. |
| 體外活性 | Micromolar concentrations of niraparib radiosensitizes tumor cell lines derived from lung, breast, and prostate cancers independently of their p53 status but not cell lines derived from normal tissues. Niraparib also sensitizes tumor cells to Water2 and converts Water2-induced single strand breaks (SSBs) into DSBs during DNA replication[5]. |
| 體內(nèi)活性 | Niraparib tosylate strongly enhances the effect of radiation on a variety of human tumor xenografts, both p53 wild type and p53 mutant. Niraparib tosylate reduces PAR levels in tumors by 1 h after administration which persisted for up to 24 h[1]. In vivo treatment with Niraparib tosylate and radiation prolonged survival (p<0.01) compared to single modalities. In vivo superiority of Niraparib tosylate plus radiation is further documented by significant elevations of cleaved caspase-3 and γ-H2AX in tumors from the combination group compared to single modality cohorts[4]. |
| 存儲(chǔ)條件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 溶解度 | Ethanol : < 1 mg/mL (insoluble or slightly soluble) DMSO : 91 mg/mL (184.7 mM) H2O : < 1 mg/mL (insoluble or slightly soluble) |
| 關(guān)鍵字 | PARP | Niraparib tosylate | Apoptosis | inhibit | MK-4827 Tosylate | MK4827 | Niraparib Tosylate | bioavailable | cancer | damage | poly ADP ribose polymerase | breast | MK 4827 Tosylate | Inhibitor | MK-4827 | anti-tumor | orally | ovarian | MK4827 Tosylate | MK 4827 | lung | Niraparib | DNA | Niraparib (MK-4827) Tosylate |
| 相關(guān)產(chǎn)品 | Stavudine | 5-Fluorouracil | Acetylcysteine | Myricetin | Sodium 4-phenylbutyrate | L-Ascorbic acid | Dextran sulfate sodium salt (MW 4500-5500) | Metronidazole | Sorafenib | Tributyrin |
| 相關(guān)庫 | 經(jīng)典已知活性庫 | 抗癌臨床化合物庫 | 藥物功能重定位化合物庫 | 抑制劑庫 | FDA 上市藥物庫 | 抗癌上市藥物庫 | 抗衰老化合物庫 | 已知活性化合物庫 | 抗癌活性化合物庫 | 抗癌藥物庫 |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
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United States- Since: 2011-01-07
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