New Arrival China Sofosbuvir Tablets 400 Mg - Niraparib 1038915-60-4 – CPF
New Arrival China Sofosbuvir Tablets 400 Mg - 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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With advanced technologies and facilities, strict high-quality handle, reasonable rate, superior services and close co-operation with prospects, we are devoted to furnishing the best price for our customers for New Arrival China Sofosbuvir Tablets 400 Mg - Niraparib 1038915-60-4 – CPF , The product will supply to all over the world, such as: Cyprus, Mozambique, Korea, Our well-equipped facilities and excellent quality control throughout all stages of production enable us to guarantee total customer satisfaction. If you are interested in any of our products or would like to discuss a custom order, please feel free to contact me. We are looking forward to forming successful business relationship with new clients around the world.
By Diego from India - 2017.06.22 12:49
Factory equipment is advanced in the industry and the product is fine workmanship, moreover the price is very cheap, value for money!
By Laura from British - 2017.03.28 16:34