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China Factory for Sacubitril Hemicalcium - Niraparib 1038915-60-4 – CPF

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  • China Factory for Sacubitril Hemicalcium - Niraparib 1038915-60-4 – CPF

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China Factory for Sacubitril Hemicalcium - 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

Niraparib 1038915-60-4

2018 GMP-2
原料药GMP证书201811（captopril ,thalidomide etc）
GMP-of-PMDA-in-Chanyoo-平成28年08月03日　Nantong-Chanyoo-Pharmatech-Co
FDA-EIR-Letter-201901

OUR STRENGTH

Quality management1

Proposal 18 Quality Consistency Evaluation projects which have approved 4, and 6 projects are under approving.

Quality management2

Advanced international quality management system has laid solid foundation for sales.

Quality management3

Quality supervision runs through the whole life cycle of the product to ensure the quality and therapeutic effect. 

Quality management4

Professional Regulatory Affairs team supports the quality demands during the application and registration.


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International cooperation
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Domestic cooperation

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China Factory for Sacubitril Hemicalcium - Niraparib 1038915-60-4 – CPF detail pictures

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We are commitment to offer the competitive price ,outstanding products quality, as well as fast delivery for China Factory for Sacubitril Hemicalcium - Niraparib 1038915-60-4 – CPF , The product will supply to all over the world, such as: Cologne, San Diego, Israel, Our products are very popular in the word, like South American, Africa, Asia and so on. Companies to "create first-class products" as the goal, and strive to deliver customers with high quality solutions, present high-quality after-sales service and technical support, and customer mutual benefit, create a better career and future!
This supplier offers high quality but low price products, it is really a nice manufacturer and business partner.
5 Stars By Janet from New Orleans - 2017.04.18 16:45
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.
5 Stars By Sara from Malaysia - 2017.03.08 14:45
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