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Product name : MK-4827 (Synonyms: Niraparib)
Item : c2314
Price : 200mg, $459;500mg, $850; 1g, $1195; 2g, $1795
contact : Send inquiry to: info@acesobio.com
CAS : 1038915-60-4 (free base)
Molecular Weight : 320.396
Formula : C19H20N4O
Storage : at -20°C
Additional information : Send inquiry to: info@acesobio.com
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Details:
Description of:MK-4827 (Synonyms: Niraparib)
Niraparib(CAS:1038915-60-4 ), also known as MK4827, is an orally active, potent and selective poly(ADP-Ribose) polymerase (PARP) inhibitor that radiosensitizes human lung and breast cancer cells.MK-4827 (Niraparib) 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 MK-4827 (Niraparib) 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 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.

Quality control data:
Quality control by 1H-NMR, 13C-NMR, HPLC and LCMS.
Product will be shipped with supporting analytical data. 

REFERENCES

1: Ledermann JA. PARP inhibitors in ovarian cancer. Ann Oncol. 2016 Apr;27 Suppl 1:i40-i44. doi: 10.1093/annonc/mdw094. PubMed PMID: 27141070.

2: Kaye SB. Progress in the treatment of ovarian cancer-lessons from homologous recombination deficiency-the first 10 years. Ann Oncol. 2016 Apr;27 Suppl 1:i1-i3. doi: 10.1093/annonc/mdw082. PubMed PMID: 27141062; PubMed Central PMCID: PMC4852273.

3: Jenner ZB, Sood AK, Coleman RL. Evaluation of rucaparib and companion diagnostics in the PARP inhibitor landscape for recurrent ovarian cancer therapy. Future Oncol. 2016 Jun;12(12):1439-56. doi: 10.2217/fon-2016-0002. Epub 2016 Apr 18. PubMed PMID: 27087632.

4: Liu JF, Matulonis UA. What Is the Place of PARP Inhibitors in Ovarian Cancer Treatment? Curr Oncol Rep. 2016 May;18(5):29. doi: 10.1007/s11912-016-0515-z. Review. PubMed PMID: 26984416.

5: Alotaibi M, Sharma K, Saleh T, Povirk LF, Hendrickson EA, Gewirtz DA. Radiosensitization by PARP Inhibition in DNA Repair Proficient and Deficient Tumor Cells: Proliferative Recovery in Senescent Cells. Radiat Res. 2016 Mar;185(3):229-45. doi: 10.1667/RR14202.1. Epub 2016 Mar 2. PubMed PMID: 26934368; PubMed Central PMCID: PMC4821451.

6: Ekblad T, Schüler H. Sirtuins are Unaffected by PARP Inhibitors Containing Planar Nicotinamide Bioisosteres. Chem Biol Drug Des. 2016 Mar;87(3):478-82. doi: 10.1111/cbdd.12680. Epub 2015 Nov 26. PubMed PMID: 26518726.

7: McGonigle S, Chen Z, Wu J, Chang P, Kolber-Simonds D, Ackermann K, Twine NC, Shie JL, Miu JT, Huang KC, Moniz GA, Nomoto K. E7449: A dual inhibitor of PARP1/2 and tankyrase1/2 inhibits growth of DNA repair deficient tumors and antagonizes Wnt signaling. Oncotarget. 2015 Dec 1;6(38):41307-23. doi: 10.18632/oncotarget.5846. PubMed PMID: 26513298; PubMed Central PMCID: PMC4747407.

8: Engert F, Schneider C, Weiβ LM, Probst M, Fulda S. PARP Inhibitors Sensitize Ewing Sarcoma Cells to Temozolomide-Induced Apoptosis via the Mitochondrial Pathway. Mol Cancer Ther. 2015 Dec;14(12):2818-30. doi: 10.1158/1535-7163.MCT-15-0587. Epub 2015 Oct 5. PubMed PMID: 26438158.



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