niraparib-tosylate-hydrate

Description: Niraparibtosylate hydrate (also known as MK-4827) is a potent, orally bioavailable and selectiveinhibitor of PARP1/2 with IC50 of 3.8 nM and 2.1nM for PARP 1 and 2respectively. Niraparib is approved by the US FDA on 27 March 2017 forthe maintenance treatment of adult patients with recurrent epithelialovarian, fallopian tube, or primary peritoneal cancer who are incomplete or partial response to platinum-based chemotherapy. Niraparibdemonstrated high activity in cancer cells with mutant BRCA-1 and BRCA-2with IC50 in the 10?100 nM range. It is > 330-fold selective againstPARP3, V-PARP and Tank1. In a whole cell assay, MK-4827 inhibited PARPactivity with EC50 of 4 nM. MK-4827 also inhibited proliferation ofcancer cells with mutant BRCA-1 and BRCA-2 with CC50 in the 10-100 nMrange. MK-4827 strongly enhanced the effect of radiation on a variety ofhuman tumor xenografts, both p53 wild type and p53 mutant.

References: Invest New Drugs. 2012 Dec; 30(6):2113-20; J Med Chem. 2009 Nov 26; 52(22):7170-85.

Related CAS #: 1038915-73-9(tosylate); 1038915-64-8 (HCl); 1613220-15-7 (tosylate hydrate); 1476777-06-6 (Niraparib metabolite M1); 1038915-58-0 (NiraparibR-enantiomer)