Niraparib tosylate

CAS No.	1038915-73-9	Cat. No.	BCP16472
Name	Niraparib tosylate
Synonyms	MK 4827 tosylate;MK4827 tosylate;MK-4827 tosylate;
Formula	C26H28N4O4S	M. Wt	492.59

Description	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 inhibits proliferation of cancer cells with mutant BRCA-1 and BRCA-2 with CC(50) in the 10-100 nM range. in vivo: MK-4827 is well tolerated in vivo and demonstrates efficacy as a single agent in a xenograft model of BRCA-1 deficient cancer [1]. In addition, MK-4827 strongly enhances the effect of radiation on a variety of human tumor xenografts, both p53 wild type and p53 mutant. The enhancement of radiation response is observed in clinically relevant radiation-dose fractionation schedules. The therapeutic window during which time MK-4827 interacts with radiation lasts for several hours. These biological attributes make translation of this therapeutic combination treatment feasible for translation to the treatment of a variety of human cancers.
Pathways	Cell Cycle/DNA Damage Epigenetics
Targets	PARP

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