Low MOQ for Doxycycline Hyclate Capsules - Niraparib 1038915-60-4 – CPF
Low MOQ for Doxycycline Hyclate Capsules - 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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Our company since its inception, constantly regards product or service high quality as business life, continually improve creation technology, make improvements to product high-quality and consistently strengthen business total high-quality management, in strict accordance together with the national standard ISO 9001:2000 for Low MOQ for Doxycycline Hyclate Capsules - Niraparib 1038915-60-4 – CPF , The product will supply to all over the world, such as: Belgium, Spain, Mexico, After 13 years of researching and developing products, our brand can represent wide range of products with outstanding quality in world market. We have completed big contracts from many countries such as Germany, Israel, Ukraine, United Kingdom, Italy, Argentina, France, Brazil, and so on. You probably feel secure and satisfy when copperate with us.
By Elsa from Saudi Arabia - 2017.11.11 11:41
Good quality and fast delivery, it's very nice. Some products have a little bit problem, but the supplier replaced timely, overall, we are satisfied.
By Joanne from Rome - 2017.11.01 17:04