Niraparib, Free Base

Niraparib, also known as MK-4827, is a poly(ADP-ribose)polymerase (PARP) inhibitor.  Niraparib displayed excellent PARP 1 and 2 inhibition with IC50 values of 3.8 and 2.1 nM, respectively, and in a whole cell assay, it inhibited PARP activity with an IC50 of 4 nM, and inhibited proliferation of cancer cells with mutant BRCA-1 and BRCA-2, with IC50 values of 10-100 nM.  Niraparib was well tolerated in vivo and showed antitumor activity as a single agent in a xenograft model of BRCA-1 deficient cancer.  Jones P., et al. Discovery of 2-{4-[(3S)-piperidin-3-yl]phenyl}-2H-indazole-7-carboxamide (MK-4827): a novel oral poly(ADP-ribose)polymerase (PARP) inhibitor efficacious in BRCA-1 and -2 mutant tumors." J. Med. Chem. 52: 7170-7185 (2009)."

• Supplier: LC Laboratories
• Product #: N-5665
• Sku #: N-5665_500mg