Original Factory Doxycycline Mono 100mg Cap - Niraparib 1038915-60-4 – CPF
Original Factory Doxycycline Mono 100mg Cap - Niraparib 1038915-60-4 – CPF Detail:
Description
Niraparib (MK-4827) is a highly potent and orally bioavailable PARP1 and PARP2 inhibitor with IC50s of 3.8 and 2.1 nM, respectively. Niraparib leads to inhibition of repair of DNA damage, activates apoptosis and shows anti-tumor activity.
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[1]. 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.
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 (Vdss=6.9 L/kg), long terminal half-life (t1/2=3.4 h), and excellent bioavailability, F=65%[1]. 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].
Storage
Powder |
-20°C |
3 years |
4°C |
2 years | |
In solvent |
-80°C |
6 months |
-20°C |
1 month |
Chemical structure
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Quality supervision runs through the whole life cycle of the product to ensure the quality and therapeutic effect.
Professional Regulatory Affairs team supports the quality demands during the application and registration.
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In order to give you convenience and enlarge our business, we also have inspectors in QC Team and assure you our best service and product for Original Factory Doxycycline Mono 100mg Cap - Niraparib 1038915-60-4 – CPF , The product will supply to all over the world, such as: Russia, Saudi Arabia, European, Qualified R&D engineer will be there for your consultation service and we will try our best to meet your requirements. So please feel free to contact us for inquiries. You'll be able to send us emails or call us for small business. Also you are able to come to our business by yourself to get further knowing of us. And we will surely give you the best quotation and after-sale service. We're ready to build stable and friendly relations with our merchants. To achieve mutual success, we will make our best efforts to build a solid co-operation and transparent communication work with our companions. Above all, we are here to welcome your inquiries for any of our goods and service.
By Amy from Cancun - 2017.06.16 18:23
The company account manager has a wealth of industry knowledge and experience, he could provide appropriate program according our needs and speak English fluently.
By Elsie from Gambia - 2018.10.01 14:14