Factory wholesale Captopril Manufacturer - Niraparib 1038915-60-4 – CPF
Factory wholesale Captopril Manufacturer - 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
Proposal 18 Quality Consistency Evaluation projects which have approved 4, and 6 projects are under approving.
Advanced international quality management system has laid solid foundation for sales.
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.
VIEW MORE
VIEW MORE
International cooperation
Domestic cooperation
Product detail pictures:
Related Product Guide:
Sticking for the belief of "Creating items of top of the range and creating buddies with people today from all over the world", we normally put the interest of shoppers in the first place for Factory wholesale Captopril Manufacturer - Niraparib 1038915-60-4 – CPF , The product will supply to all over the world, such as: Atlanta, Uruguay, Morocco, We will not only continuously introduce technical guidance of experts from both home and abroad, but also develop the new and advanced products constantly to satisfactorily meet the needs of our clients all over the world.
By King from Oslo - 2018.09.23 17:37
Company director has very rich management experience and strict attitude, sales staff are warm and cheerful, technical staff are professional and responsible,so we have no worry about product,a nice manufacturer.
By Andrew Forrest from USA - 2018.10.31 10:02