MK-4827 (Niraparib)1038915-60-4

MK4827 (Niraparib)
分子式：C19H20N4O    分子量：320.39
 
 
產品描述
MK-4827是選擇性PARP1/2抑制劑，IC50為3.8 nM/2.1 nM, 作用于攜帶突變型BRCA-1和BRCA-2的癌細胞，具有強的作用活性。比作用于PARP3, V-PARP 和Tank1選擇性高330倍以上。
靶點
PARP1
PARP2
       
IC50
3.8 nM
2.1 nM
       
體外研究
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.
體內研究
MK-4827 is well tolerated in vivo and demonstrates efficacy as a single agent in a xenograft model of BRCA-1 deficient cancer.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.
溶解性
可溶于DMSO
穩定性
2年 -20°C粉狀，6月-80°C溶于DMSO