Niraparib(MK-4827) tosylate

产品编号: DC9576 Featured
Niraparib(MK-4827) tosylate
结构式
1038915-73-9
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中国地区超过5000个高品质化合物库存
应用领域
Niraparib tosylate (MK-4827 tosylate) 是一种高效的,具有生物口服利用度的 PARP1 和 PARP2 抑制剂,IC50 分别为 3.8 和 2.1 nM。Niraparib tosylate (MK-4827 tosylate) 抑制 DNA 损伤修复,诱导凋亡 (apoptosis) 并具有抗肿瘤活性。
Cas No.: 1038915-73-9
名称:
别名: Niraparib tosylate;MK 4827 tosylate;MK4827 tosylate
SMILES: CC1=CC=C(C=C1)S(=O)(=O)O.C1C[C@H](CNC1)C2=CC=C(C=C2)N3C=C4C=CC=C(C4=N3)C(=O)N
分子式: C26H28N4O4S
分子量: 492.5899
纯度:
保存条件: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description:
In Vivo:
In Vitro:
References: MK-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 against PARP3, V-PARP and Tank1. 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. 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.
Kinase Assay:
Cell Assay:
Animal Administration:
References:
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
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