Niraparib tosylate
别名: MK 4827 tosylate 中文名称：尼拉帕尼甲苯磺酸盐
Niraparib tosylate是PARP1/PARP2的选择性抑制剂，IC50分别为3.8 nM和2.1 nM。Niraparib可增加PARP-DNA复合体的形成，并导致DNA损伤、凋亡和细胞死亡。
Niraparib tosylate Chemical Structure
CAS: 1038915-73-9
客户使用Selleck的Niraparib tosylate发表文献37篇
产品质控
Niraparib tosylate相关产品
| 相关靶点 | PARP1 PARP2 PARP3 Tankyrase-1 Tankyrase-2 PARP14 PARP7 TNKS1 TNKS2 | 点击展开 |
|---|---|---|
| 相关化合物库 | FDA药物库 天然产物库 凋亡分子化合物库 DNA损伤/ DNA修复化合物库 细胞周期化合物库 | 点击展开 |
相关信号通路图
PARP抑制剂选择性比较
细胞实验数据示例
| 细胞系 | 实验类型 | 给药浓度 | 孵育时间 | 活性描述 | 文献信息 |
|---|---|---|---|---|---|
| MDA-MB-436 | Antitumor assay | 50 mg/kg | 33 days | Antitumor activity against human MDA-MB-436 cells expressing BRCA1 5396 + 1G>A mutant xenografted in CD1 mouse assessed as tumor regression at 50 mg/kg, po bid for 33 days | 19873981 |
| MDA-MB-436 | Antitumor assay | 100 mg/kg | 33 days | Antitumor activity against human MDA-MB-436 cells expressing BRCA1 5396 + 1G>A mutant xenografted in CD1 mouse assessed as tumor regression at 100 mg/kg, po qd for 33 days | 19873981 |
| MDA-MB-436 | Antitumor assay | 80 mg/kg | 1 to 2 weeks | Antitumor activity against human MDA-MB-436 cells harboring BRCA1 mutant xenografted in immunocompromised mouse assessed as tumor growth inhibition at 80 mg/kg, po qd for 1 to 2 weeks | 25761096 |
| MDA-MB-436 | Antitumor assay | 80 mg/kg | 4 weeks | Antitumor activity against human MDA-MB-436 cells harboring BRCA1 mutant xenografted in immunocompromised mouse assessed as complete and sustained tumor regression at 80 mg/kg, po qd for 4 weeks | 25761096 |
| MDA-MB-436 | Antitumor assay | 80 mg/kg | 3 weeks | Antitumor activity against human MDA-MB-436 cells harboring BRCA1 mutant xenografted in immunocompromised mouse assessed as tumor shrinkage at 80 mg/kg, po qd for 3 weeks | 25761096 |
| MDA-MB-436 | Antitumor assay | 50 mg/kg | Antitumor activity against human MDA-MB-436 cells harboring BRCA1 mutant xenografted in immunocompromised mouse assessed as tumor growth inhibition at 50 mg/kg, po administered daily | 25761096 | |
| HeLa | Antiproliferative assay | 7 days | Antiproliferative activity against human HeLa cells expressing wild type BRCA1 after 7 days by cell titer-blue assay, CC50 = 0.86 μM. | 19873981 | |
| Capan1 | Antiproliferative assay | 13 days | Antiproliferative activity against human Capan1 cells expressing BRCA2 6174delT mutation and loss of wild-type allele after 13 days by cell titer-blue assay, CC50 = 0.09 μM. | 19873981 | |
| HeLa | Antiproliferative assay | 7 days | Antiproliferative activity against BRCA1 deficient human HeLa cells after 7 days by cell titer-blue assay, CC50 = 0.033 μM. | 19873981 | |
| MDA-MB-436 | Antiproliferative assay | 6 days | Antiproliferative activity against human MDA-MB-436 cells expressing BRCA1 5396 + 1G>A mutant after 6 days by cell titer-blue assay, CC50 = 0.018 μM. | 19873981 | |
| Jurkat | Function assay | 96 hrs | Inhibition of PARP1 in human Jurkat cells assessed as reduction of cell viability after 96 hrs by MTS assay in presence of 100 uM of temozolomide, EC50 = 0.2 μM. | 23850199 | |
| Jurkat | Function assay | 96 hrs | Inhibition of PARP1 in human Jurkat cells assessed as reduction of cell viability after 96 hrs by MTS assay, EC50 = 31 μM. | 23850199 | |
| A549 | Cytotoxicity assay | 5 to 7 days | Cytotoxicity against human A549 cells transfected with BRCA2 shRNA assessed as inhibition of cell proliferation after 5 to 7 days by CellTiter-Blue assay, CC50 = 0.011 μM. | 25761096 | |
| SUM1315MO2 | Cytotoxicity assay | 12 days | Cytotoxicity against human SUM1315MO2 cells carrying BRCA1 mutant assessed as inhibition of cell proliferation after 12 days by CellTiter-Blue assay, CC50 = 0.02 μM. | 25761096 | |
| DoTc2-4510 | Cytotoxicity assay | 5 to 7 days | Cytotoxicity against human DoTc2-4510 cells carrying BRCA2 mutant assessed as inhibition of cell proliferation after 5 to 7 days by CellTiter-Blue assay, CC50 = 0.023 μM. | 25761096 | |
| SUM149PT | Cytotoxicity assay | 5 to 7 days | Cytotoxicity against human SUM149PT cells carrying BRCA1 mutant assessed as inhibition of cell proliferation after 5 to 7 days by CellTiter-Blue assay, CC50 = 0.024 μM. | 25761096 | |
| HeLa | Cytotoxicity assay | 5 to 7 days | Cytotoxicity against human HeLa cells transfected with BRCA1 shRNA assessed as reduction of cell viability after 5 to 7 days by CellTiter-Blue assay, CC50 = 0.034 μM. | 25761096 | |
| UWB1.289 | Cytotoxicity assay | 5 to 7 days | Cytotoxicity against human UWB1.289 cells carrying BRCA1 mutant assessed as inhibition of cell proliferation after 5 to 7 days by CellTiter-Blue assay, CC50 = 0.056 μM. | 25761096 | |
| HeLa | Cytotoxicity assay | 5 to 7 days | Cytotoxicity against wild type human HeLa cells assessed as inhibition of cell proliferation after 5 to 7 days by CellTiter-Blue assay, CC50 = 0.852 μM. | 25761096 | |
| UWB1.289 | Cytotoxicity assay | 5 to 7 days | Cytotoxicity against human UWB1.289 cells expressing BRCA1 assessed as inhibition of cell proliferation after 5 to 7 days by CellTiter-Blue assay, CC50 = 0.975 μM. | 25761096 | |
| A549 | Cytotoxicity assay | 5 to 7 days | Cytotoxicity against wild type human A549 cells assessed as inhibition of cell proliferation after 5 to 7 days by CellTiter-Blue assay, CC50 = 1.76 μM. | 25761096 | |
| BT20 | Cytotoxicity assay | 5 to 7 days | Cytotoxicity against human BT20 cells assessed as inhibition of cell proliferation after 5 to 7 days by CellTiter-Blue assay, CC50 = 2.2 μM. | 25761096 | |
| HeLa | Function assay | Inhibition of PARP in hydrogen peroxide-induced human HeLa cells assessed as inhibition DNA-damage-induced PARylation, EC90 = 0.045 μM. | 19873981 | ||
| HeLa | Function assay | Inhibition of PARP in hydrogen peroxide-induced human HeLa cells assessed as inhibition DNA-damage-induced PARylation, EC50 = 0.004 μM. | 19873981 | ||
| CAPAN-1 | Function assay | Inhibition of PARP in BRCA2-deficient human CAPAN-1 cells assessed as inhibition of hydrogen peroxide-induced PARylation by cell-based assay, IC50 = 0.0035 μM. | 25761096 | ||
| HeLa | Function assay | Inhibition of PARP in human HeLa cells assessed as inhibition of hydrogen peroxide-induced PARylation by cell-based assay, EC50 = 0.004 μM. | 25761096 | ||
| A2780 | Function assay | Inhibition of PARP in human A2780 cells assessed as inhibition of hydrogen peroxide-induced PARylation by cell-based assay, IC50 = 0.004 μM. | 25761096 | ||
| MDA-MB-436 | Cytotoxicity assay | Cytotoxicity against human MDA-MB-436 cells carrying BRCA1 mutant assessed as inhibition of cell proliferation, CC50 = 0.018 μM. | 25761096 | ||
| HeLa | Function assay | Inhibition of PARP in human HeLa cells assessed as inhibition of hydrogen peroxide-induced PARylation by cell-based assay, IC90 = 0.046 μM. | 25761096 | ||
| CAPAN-1 | Function assay | Inhibition of PARP in BRCA2-deficient human CAPAN-1 cells assessed as inhibition of hydrogen peroxide-induced PARylation by cell-based assay, IC90 = 0.05 μM. | 25761096 | ||
| A2780 | Function assay | Inhibition of PARP in human A2780 cells assessed as inhibition of hydrogen peroxide-induced PARylation by cell-based assay, IC90 = 0.052 μM. | 25761096 | ||
| Capan1 | Cytotoxicity assay | Cytotoxicity against BRCA2-deficient human Capan1 cells, CC50 = 0.09 μM. | 25761096 | ||
| Capan1 | Cytotoxicity assay | Cytotoxicity against BRCA2-deficient human Capan1 cells, EC50 = 0.65 μM. | 26652717 | ||
| TC32 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells | 29435139 | ||
| A673 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells | 29435139 | ||
| NB1643 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells | 29435139 | ||
| A673 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for A673 cells) | 29435139 | ||
| BT-37 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-37 cells | 29435139 | ||
| SK-N-MC | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells | 29435139 | ||
| NB-EBc1 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells | 29435139 | ||
| LAN-5 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells | 29435139 | ||
| SK-N-MC | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-MC cells | 29435139 | ||
| TC32 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for TC32 cells | 29435139 | ||
| 点击查看更多细胞系数据 | |||||
生物活性
| 产品描述 | Niraparib tosylate是PARP1/PARP2的选择性抑制剂，IC50分别为3.8 nM和2.1 nM。Niraparib可增加PARP-DNA复合体的形成，并导致DNA损伤、凋亡和细胞死亡。 | ||||
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| 靶点 |
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| 体外研究(In Vitro) | ||||
| 体外研究活性 | 微摩尔级浓度的niraparib使来自于肺癌、乳腺癌以及前列腺癌的肿瘤细胞对放射线敏感（不依赖于它们的p53状态），而对来自于正常组织的细胞没有此作用。Niraparib同样还可以使肿瘤细胞对过氧化氢敏感、在DNA复制时，将过氧化氢诱导的单链断裂转变为双链断裂[5]。 |
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| 细胞实验 | 细胞系 | V-C8细胞 | ||
| 浓度 | 50 nM | |||
| 孵育时间 | 24 h | |||
| 方法 | 用PARP抑制剂MK-4827对中国仓鼠细胞V-C8（BRCA2-negative）进行处理，24小时后，洗涤并将细胞孵育在不含此化合物的培养基中5-7天，直到形成克隆。 |
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| 实验图片 | 检测方法 | 检测指标 | 实验图片 | PMID |
| Western blot | c-PARP /c-caspase 3 / γ-H2AX |
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29158830 | |
| Immunofluorescence | Rad51 / Geminin |
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27614696 | |
| 体内研究(In Vivo) | ||
| 体内研究活性 |
MK-4827可以增强放射线对多种人类肿瘤异种移植的作用，无论是在p53野生型或是p53突变体。MK-4827在给药后1小时降低肿瘤中PAR水平并持续效果24小时[1]。MK-4827体内给药能延长放射线处理后的动物寿命。MK-4827和放射治疗结合，显著提高肿瘤中裂解的caspase-3和γ-H2AX的水平[4]。 |
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|---|---|---|
| 动物实验 | Animal Models | 雌性裸鼠(Ncr Nu/Nu) |
| Dosages | 25或50 mg/kg | |
| Administration | 口服 | |
化学信息&溶解度
| 分子量 | 492.59 | 分子式 | C19H20N4O.C7H8O3S |
| CAS号 | 1038915-73-9 | SDF | Download Niraparib tosylate SDF |
| Smiles | CC1=CC=C(C=C1)S(=O)(=O)O.C1CC(CNC1)C2=CC=C(C=C2)N3C=C4C=CC=C(C4=N3)C(=O)N | ||
| 储存条件(自收到货起) | |||
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体外溶解度 |
DMSO : 99 mg/mL ( (200.97 mM)； DMSO吸湿会降低化合物溶解度，请使用新开封DMSO) Water : Insoluble Ethanol : Insoluble |
摩尔浓度计算器 |
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体内溶解度 现配现用，请按从左到右的顺序依次添加，澄清后再加入下一溶剂 |
动物体内配方计算器 | ||||
实验计算
动物体内配方计算器（澄清溶液）
第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）
第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系Selleck为您提供正确的澄清溶液配方）
计算结果：
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于μL DMSO溶液（母液浓度mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系Selleck）；
体内配方配制方法：取μL DMSO母液，加入μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入μL ddH2O，混匀澄清。
体内配方配制方法：取μL DMSO母液，加入μL Corn oil，混匀澄清。
注意：1. 首先保证母液是澄清的；
2.一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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