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Niraparib

CAS No. : 1038915-60-4

MCE 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  |  FDA Approved & Pharmacopeial Drug Library  |  Anti-Breast Cancer Compound Library  |  Anti-Pancreatic Cancer Compound Library  |  Targeted Therapy Drug Library   |  MG-132  |  LY294002  |  Doxorubicin hydrochloride  |  Bafilomycin A1  |  Paclitaxel  |  Y-27632 dihydrochloride  |  Acetylcysteine  |  Angiotensin II human  |  SP600125  |  5-Fluorouracil  |  Staurosporine  |  Bortezomib  |  Tamoxifen  |  2-Deoxy-D-glucose  |  Gemcitabine  |  Verteporfin  |  Decitabine  |  Actinomycin D  |  Temozolomide  |  BAY 11-7082  |  Etoposide  |  Mitomycin C  |  CCCP  |  DAPT  |  Rote  |  Etomoxir  |  Stattic  |  Docetaxel  |  Fulvestrant

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