PdtDtShtProduct Data SheetProduct Name:CAS No.: Cat. No.:MWt:Formula:Purity :MK-4827 tosylate1038915-73-9HY-10619B492.59C26H28N4O4S>98%Solubility:DMSOMechanisms: Pathways:Cell Cycle/DNA Damage; Target:PARP Biological Activity:()yMK-4827(Niraparib) tosylate is a selective inhibitor of PARP1/PARP2 with IC50 of 3.8 nM/2.1 nM;with great activity in cancer cells with mutant BRCA-1 and BRCA-2; >330-fold selective againstPARP3, V-PARP and Tank1. IC50 value: 3.8 nM/2.1 nM( PARP1/2) [1] Target: PARP1/2 in vitro: MK-4827 displays excellent PARP 1 and 2 inhibition with IC(50) = 3.8 and 2.1 nM,respectively, and in a whole cell assay, it inhibits PARP activity with EC(50) = 4 nM and inhibitsproliferation of cancer cells with mutant BRCA-1 and BRCA-2 with CC(50) in the 10-100 nM range[1]. iiin vivo: MK-4827 is well tolerated in vivo and demonstrates efficacy as a single agent in a xenograftMK4827illtltdiiddttffiiltiftmodel of BRCA-1 deficient cancer [1]. In addition, MK-4827 strongly enhances the effect of radiationon a variety of human tumor xenografts, both p53 wild type and p53 mutant. The enhancement ofradiation response ...References:[1]. 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 -2mutanttumorsJMedChem2009Nov26;52(22):717085 mutant tumors. J Med Chem. 2009 Nov 26;52(22):7170-85.[2]. Wang L, et al. MK-4827, a PARP-1/-2 inhibitor, strongly enhances response of human lung andbreast cancer xenografts to radiation. Invest New Drugs. 2012 Dec;30(6):2113-20. Caution: Not fully tested. For research purposes onlyMedchemexpress LLCwww.medchemexpress.com18Wilkinson Way, Princeton, NJ 08540,USAess.com Web: www.medchemexpress.comEmail: info@medchemexpr