China Wholesale Rosuvastatin Calcium 20 Mg Suppliers - Niraparib 1038915-60-4 – CPF
China Wholesale Rosuvastatin Calcium 20 Mg Suppliers - 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.
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International cooperation
Domestic cooperation
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"Sincerity, Innovation, Rigorousness, and Efficiency" is definitely the persistent conception of our corporation to the long-term to establish alongside one another with customers for mutual reciprocity and mutual profit for China Wholesale Rosuvastatin Calcium 20 Mg Suppliers - Niraparib 1038915-60-4 – CPF , The product will supply to all over the world, such as: Montreal, Portland, Nicaragua, We have developed large markets in many countries, such as Europe and the United States, Eastern Europe and Eastern Asia. Meanwhile with the powerful predominance in persons with ability, strict production management and business concept.we constantly carry on self-innovation, technological innovation, managing innovation and business concept innovation. To follow the world markets fashion, new products are kept on researching and providing to guarantee our competitive advantage in styles, quality, price and service.
By Heloise from Georgia - 2017.08.28 16:02
This company has the idea of "better quality, lower processing costs, prices are more reasonable", so they have competitive product quality and price, that's the main reason we chose to cooperate.
By Anna from Florence - 2017.08.16 13:39