| 货号 (SKU) | 包装规格 | 是否现货 | 价格 | 数量 |
|---|---|---|---|---|
| N409261-1ml |
1ml |
现货  |
|
| 别名 | 尼拉帕尼 (MK-4827) |
|---|---|
| 英文别名 | (S)-2-(4-(piperidin-3-yl)phenyl)-2H-indazole-7-carboxamide |
| 规格或纯度 | Moligand™, 10mM in DMSO |
| 英文名称 | Niraparib (MK-4827) |
| 生化机理 | 尼拉帕利（MK-4827）是一种选择性 PARP1/2 抑制剂，IC50 为 3.8 nM/2.1 nM，对突变 BRCA-1 和 BRCA-2 癌细胞具有很强的活性。它对 PARP3、V-PARP 和 Tank1 的选择性大于 330 倍。Niraparib 可形成 PARP-DNA 复合物，导致 DNA 损伤、细胞凋亡和细胞死亡。第 3 阶段 |
| 储存温度 | -80℃储存 |
| 运输条件 | 超低温冰袋运输 |
| 作用类型 | 抑制剂 |
| 作用机制 | 聚[ADP-核糖]聚合酶-1 抑制剂 |
| 产品介绍 |
MK-4827(Niraparib)是高活性PARP1/PARP2抑制剂，IC50分别为3.8 nM/2.1 nM，在BRCA-1和BRCA-2突变型肿瘤细胞中具有很好的活性，比对PARP3，V-PARP和Tank1的抑制性高330倍以上。 Information Niraparib (MK-4827) is a selective inhibitor ofPARP1/2withIC50of 3.8 nM/2.1 nM, with great activity in cancer cells with mutant BRCA-1 and BRCA-2. It is >330-fold selective against PARP3, V-PARP and Tank1. Niraparib can form PARP–DNA complexes resulting i In a whole cell assay, MK-4827 inhibited PARP activity with EC50 = 4 nM and inhibited proliferation of cancer cells with mutant BRCA-1 and BRCA-2 with CC50 in the 10-100 nM range. It was demonstratedto be a potent and selective PARP-1 and PARP-2 inhibitor with IC50=3.8 and 2.1 nM, respectively. Furthermore, it displayed at least a 100-fold selectivity over PARP-3, V-PARP, and tankyrase-1, with IC50 = 1300, 330, and 570 nM, respectively. As well as inhibiting the growth of HeLa cell lacking BRCA-1 because of silencing by RNA interference, MK-4827 is able to inhibit the proliferation of cancer cell lines carrying natural BRCA-1 or BRCA-2 mutations. In MDA-MB-436 human mammary gland adenocarcinoma cells carrying BRCA-1 mutations, MK-4827 displayed CC50 = 18 nM, while in CAPAN-1 human pancreatic adenocarcinoma cells, which are BRCA-2 mutant, MK-4827 displayed CC50 = 90 nM. In contrast, normal human prostate and mammary epithelial cells are resistant to MK-4827, displaying antiproliferative effects in the micromolar range, thereby demonstrating the very high selective cytotoxicity from these PARP inhibitors in BRCA-1 and -2 mutant cancer cells compared to surrounding tissue. In vivo MK-4827, a novel, orally bioavailable, PARP-1 and PARP-2 inhibitor, strongly enhanced the effect of radiation on a variety of human tumor xenografts, both p53 wild type and p53 mutant. It was well tolerated in vivo and demonstrated efficacy as a single agent in a xenograft model of BRCA-1 deficient cancer. cell lines：Adrenocortical tumor cell line NCI-h295 Concentrations：serial dilutions Incubation Time：7 days Powder Purity:≥99% |
| ALogP | 2.2 |
|---|
| 分子类型 | 小分子 |
|---|---|
| Isomeric SMILES | C1C[C@H](CNC1)C2=CC=C(C=C2)N3C=C4C=CC=C(C4=N3)C(=O)N |
| 分子量 | 320.39 |
| Reaxy-Rn | 19395275 |
| Reaxys-RN link address | https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=19395275&ln= |
| 溶解性 | Solubility (25°C) In vitro DMSO: 40 mg/mL (98.22 mM); Ethanol: 3 mg/mL (7.36 mM); Water: Insoluble; |
|---|
| 象形图 | GHS08, GHS07 |
|---|---|
| 信号词 | Danger |
| 危险声明 |
H373: 通过长时间或反复暴露对器官造成损害 H302: 吞食有害 H340: 可能导致遗传缺陷 H361: 怀疑破坏生育力或未出生的孩子 |
| 预防措施声明 |
P280: 戴防护手套/穿防护服/戴防护眼罩/戴防护面具。 P405: 密闭存放 P501: 将内容物/容器处理到。。。 P264: 处理后要彻底洗手。 P260: 不要吸入灰尘/烟雾/气体/雾/蒸汽/喷雾。 P281: 根据需要使用个人防护设备。 P270: 使用本产品时，请勿进食、饮水或吸烟。 P330: 漱口 P203: 使用前，获取、阅读并遵守所有安全说明。 P301+P317: 如果被吞咽：请寻求医疗帮助。 P318: 如果暴露或担心，请就医。 P319: 如果你感到不适，请寻求医疗帮助。 |
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