计算溶液所需的质量、体积或浓度。
概述
Information
Niraparib tosylate (MK-4827, ZEJULA) is a selective inhibitor ofPARP1/PARP2withIC50of 3.8 nM/2.1 nM. Niraparib increases formation of PARP-DNA complexes resulting in DNA damage,apoptosis, and cell death.
In vitro
Micromolar concentrations of niraparib radiosensitizes tumor cell lines derived from lung, breast, and prostate cancers independently of their p53 status but not cell lines derived from normal tissues. Niraparib also sensitizes tumor cells to H2O2 and converts H2O2-induced single strand breaks (SSBs) into DSBs during DNA replication.
In vivo
MK-4827 strongly enhances the effect of radiation on a variety of human tumor xenografts, both p53 wild type and p53 mutant. MK-4827 reduces PAR levels in tumors by 1 h after administration which persisted for up to 24 h. In vivo treatment with MK-4827 and radiation prolonged survival (p<0.01) compared to single modalities. In vivo superiority of MK-4827 plus radiation is further documented by significant elevations of cleaved caspase-3 and γ-H2AX in tumors from the combination group compared to single modality cohorts.
Cell Data
cell lines：
Concentrations：50 nM
Incubation Time：24 h
Powder Purity:≥99%
规格
英文别名
Niraparib tosylate, MK 4827 tosylate, ZEJULA
规格或纯度
10mM in DMSO
英文名称
Niraparib (MK-4827) tosylate
生化机理
Niraparib tosylate（MK-4827，ZEJULA）是 PARP1/PARP2 的选择性抑制剂，IC50 为 3.8 nM/2.1 nM。Niraparib 可增加 PARP-DNA 复合物的形成，导致 DNA 损伤、细胞凋亡和细胞死亡。
储存条件
-80℃储存
运输条件
特低温运输
名称和识别符
分子类型
小分子
Isomeric 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
分子量
492.59
Reaxy-Rn
42083915
Reaxys-RN link address
https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=42083915&ln=
高级数据
化学和物理性质
溶解性
Solubility (25°C) In vitro DMSO: 81 mg/mL (198.8 mM); Water: Insoluble; Ethanol: Insoluble;
质检证书(CoA,COO,BSE/TSE 和分析图谱)
C of A & Other Certificates(BSE/TSE, COO):
输入批号以搜索分析图谱:
溶液计算器
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