MCE 的所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务。

Niraparib

CAS No. : 1038915-60-4

MCE 国际站：Niraparib

产品活性：Niraparib (MK-4827) 是高效的，具有生物口服利用度的 PARP1 和 PARP2 抑制剂，IC₅₀ 分别为 3.8 nM 和 2.1 nM。Niraparib 抑制 DNA 损伤修复，诱导凋亡 (apoptosis) 并具有抗肿瘤活性。

研究领域：Cell Cycle/DNA Damage  |  Epigenetics  |  Apoptosis

作用靶点：PARP  |  Apoptosis

In Vitro: Niraparib (MK-4827) inhibits PARP activity with EC₅₀=4 nM and EC₉₀=45 nM in a whole cell assay. MK-4827 inhibits proliferation of cancer cells with mutant BRCA-1 and BRCA-2 with CC₅₀ in the 10-100 nM range. MK-4827 displays excellent PARP 1 and 2 inhibition with IC₅₀=3.8 and 2.1 nM, respectively, and in a whole cell assay. To validate that Niraparib (MK-4827) inhibits PARP in these cell lines, A549 and H1299 cells are treated with 1 μM MK-4827 for various times and measured PARP enzymatic activity using a chemiluminescent assay. The results show that Niraparib (MK-4827) inhibits PARP within 15 minutes of treatment reaching about 85% inhibition in the A549 cells at 1 h and about 55% inhibition at 1 h for the H1299 cells.

In Vivo: Niraparib (MK-4827) is well tolerated and demonstrates efficacy as a single agent in a xenograft model of BRCA-1 deficient cancer. Niraparib (MK-4827) is well tolerated in vivo and demonstrates efficacy as a single agent in a xenograft model of BRCA-1 deficient cancer. Niraparib (MK-4827) is characterized by acceptable pharmacokinetics in rats with plasma clearance of 28 (mL/min)/kg, very high volume of distribution (Vd_ss=6.9 L/kg), long terminal half-life (t_1/2=3.4 h), and excellent bioavailability, F=65%. Niraparib (MK-4827) enhances radiation response of p53 mutant Calu-6 tumor in both cases, with the single daily dose of 50 mg/kg being more effective than 25 mg/kg given twice daily.

相关产品：Drug Repurposing Compound Library Plus  |  FDA-Approved Drug Library Plus  |  FDA-Approved Drug Library Mini  |  Bioactive Compound Library Plus  |  Apoptosis Compound Library  |  Cell Cycle/DNA Damage Compound Library  |  Epigenetics Compound Library  |  FDA-Approved Drug Library  |  Anti-Cancer Compound Library  |  Anti-Aging Compound Library  |  Drug Repurposing Compound Library  |  Anti-COVID-19 Compound Library  |  Orally Active Compound Library  |  Chemical Probe Library  |  FDA Approved & Pharmacopeial Drug Library  |  Anti-Breast Cancer Compound Library  |  Drug-Induced Liver Injury (DILI) Compound Library  |  Anti-Pancreatic Cancer Compound Library  |  Targeted Therapy Drug Library   |  Rare Diseases Drug Library  |  Children’s Drug Library  |  EMA-Approved Drug Library  |  FDA-Approved Anticancer Drug Library  |  Anti-Prostate Cancer Compound Library  |  Heterocyclic Compound Library  |  Cell Death Library  |  Anti-Ovarian Cancer Compound Library  |  Multi-Target Compound Library  |  Bioactive Compound Library Max  |  MG-132  |  Doxorubicin hydrochloride  |  Bafilomycin A1  |  Tamoxifen  |  Olaparib  |  Y-27632  |  Paclitaxel  |  Z-VAD-FMK  |  LY294002  |  2-Deoxy-D-glucose  |  Angiotensin II human  |  Acetylcysteine  |  Staurosporine  |  Actinomycin D  |  SB-431542  |  5-Fluorouracil  |  Bortezomib  |  Oxaliplatin  |  Deferoxamine mesylate  |  Sorafenib  |  Trametinib  |  Gemcitabine  |  Temozolomide  |  Etoposide  |  Rotenone  |  Mdivi-1  |  Monomethyl auristatin E  |  Decitabine  |  Ruxolitinib  |  Elesclomol

热门产品线：重组蛋白  |  药物筛选  |  天然产物  |  荧光染料  |  PROTAC  |  同位素标记物

Trending products：Recombinant Proteins  |  Bioactive Screening Libraries  |  Natural Products  |  Dye Reagents  |  PROTAC  |  Isotope-Labeled Compounds

品牌介绍:
•   MCE (MedChemExpress) 拥有200 多种全球独家化合物库，我们致力于为全球科研客户提供前沿最全的高品质小分子活性化合物；
•   50,000 多种高选择性抑制剂、激动剂涉及各热门信号通路及疾病领域；
•   产品种类涵盖各种重组蛋白，多肽，常用试剂盒 ，更有 PROTAC、ADC 等特色产品，广泛应用于新药研发、生命科学等科研项目；
•   提供虚拟筛选，离子通道筛选，代谢组学分析检测分析，药物筛选等专业技术服务；
•   设有专业的实验中心和严格的质控、验证体系；
•   提供 LC/MS、NMR、HPLC、手性分析、元素分析等各项质检报告，确保产品的高纯度、高品质；
•   产品的生物活性多经各国客户实验验证；
•   Nature, Cell, Science 等多种顶级期刊及制药专利收录了MCE客户的科研成果；
•   专业团队跟踪最新的制药及生命科学研究进展，为您提供全球最新的活性化合物；
•   与世界各大制药公司及知名科研机构建立了长期的合作。