Rucaparib phosphate
别名: AG-014699 phosphate, PF-01367338 phosphate 中文名称：瑞卡帕布磷酸盐
Rucaparib phosphate是一种PARP抑制剂，无细胞试验中作用于PARP1的Ki为1.4 nM，对其余8个PARP位点也有结合亲和力。Phase 3。
Rucaparib phosphate Chemical Structure
CAS: 459868-92-9
产品质控
批次：
纯度：
99.87%
99.87
Rucaparib phosphate相关产品
相关信号通路图
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 |
|---|---|---|---|---|---|
| A549 | Growth Inhibition Assay | 400 nM | 24 h | increases cellular radiosensitivity | 24411611 |
| H460 | Growth Inhibition Assay | 400 nM | 24 h | increases cellular radiosensitivity | 24411611 |
| MDA-MB-231 | Growth Inhibition Assay | 10/20/40 μM | 24 h | blocks cell cycle progression in G2/M phase | 24420152 |
| MDA-MB-231 | Apoptosis Assay | 10/20/40 μM | 24 h | induces apoptosis dose dependently | 24420152 |
| MDA-MB-231 | Cell Viability Assay | 0.1-40 μM | 24 h | IC50 = 17.77 μM | 24420152 |
| MDA-MB-231 | Function Assay | 10/20/40 μM | 24 h | increases p-AKT levels in a dose-dependent manner | 24420152 |
| EFM192A | Growth Inhibition Assay | 500 nM | 10–15 d | reduces cell growth in the four lines and significantly | 25128455 |
| AU565 | Growth Inhibition Assay | 500 nM | 10–15 d | reduces cell growth in the four lines and significantly | 25128455 |
| SKBR3 | Growth Inhibition Assay | 500 nM | 10–15 d | reduces cell growth in the four lines and significantly | 25128455 |
| BT474 | Growth Inhibition Assay | 500 nM | 10–15 d | reduces cell growth in the four lines and significantly | 25128455 |
| C4-2 | Growth Inhibition Assay | 0-3 μM | 14 d | decreases colony number dose dependently | 23565244 |
| PC3 | Growth Inhibition Assay | 0-3 μM | 14 d | decreases colony number dose dependently | 23565244 |
| DU145 | Growth Inhibition Assay | 0-3 μM | 14 d | decreases colony number dose dependently | 23565244 |
| VCaP | Growth Inhibition Assay | 0-3 μM | 14 d | decreases colony number dose dependently | 23565244 |
| LNCaP | Growth Inhibition Assay | 0-3 μM | 14 d | decreases colony number dose dependently | 23565244 |
| LoVo | Cytotoxicity assay | 0.4 uM | 5 days | Potentiation of temozolomide-induced cytotoxicity in human LoVo cells assessed as temozolomide GI50 at 0.4 uM after 5 days by Celltiter-Glo assay, GI50 = 0.144 μM. | 26652717 |
| BT-474 | Function Assay | 0.1/1/500/1000 nM | inhibits PARP activity at starting concerntration of 500 nM | 25128455 | |
| TOV112D | Growth Inhibition Assay | 0-3 μM | IC50>15 μM | 23729402 | |
| LoVo | Function assay | 30 mins | Inhibition of PARP in human LoVo cells assessed as inhibition of poly(ADP)-ribose polymerization for 30 mins by fluorescence assay, EC50 = 0.00469 μM. | 26652717 | |
| MDA-MB-436 | Anticancer assay | 96 hrs | Anticancer activity against human BRCA1-deficient MDA-MB-436 cells after 96 hrs by MTT assay, CC50 = 3 μM. | 26342868 | |
| OVCAR3 | Antiproliferative assay | 24 hrs | Antiproliferative activity against human OVCAR3 cells after 24 hrs by MTT assay, IC50 = 3.31 μM. | 29456106 | |
| MCF7 | Anticancer assay | 96 hrs | Anticancer activity against human MCF7 cells after 96 hrs by MTT assay, CC50 = 19.47 μM. | 26342868 | |
| PEO6 | Growth Inhibition Assay | IC50=7.06 ± 0.74 μM | 23729402 | ||
| RMUGS | Growth Inhibition Assay | IC50=7.03 ± 1.83 μM | 23729402 | ||
| KK | Growth Inhibition Assay | IC50=6.15 ± 1.42 μM | 23729402 | ||
| OVISE | Growth Inhibition Assay | IC50=5.68 ± 0.23 μM | 23729402 | ||
| TOV21G | Growth Inhibition Assay | IC50=5.07 ± 1.30 μM | 23729402 | ||
| KURAMOCHIb | Growth Inhibition Assay | IC50=4.34 ± 0.29 μM | 23729402 | ||
| OVTOKO | Growth Inhibition Assay | IC50=4.14 ± 1.53 μM | 23729402 | ||
| A2780 | Growth Inhibition Assay | IC50=3.94 ± 0.25 μM | 23729402 | ||
| PEO14 | Growth Inhibition Assay | IC50=3.84 ± 0.76 μM | 23729402 | ||
| OVCAR3 | Growth Inhibition Assay | IC50=3.74 ± 0.40 μM | 23729402 | ||
| OVKATE | Growth Inhibition Assay | IC50=3.64 ± 1.79 μM | 23729402 | ||
| OVSAHO | Growth Inhibition Assay | IC50=3.64 ± 0.33 μM | 23729402 | ||
| OAW28 | Growth Inhibition Assay | IC50=3.61 ± 0.28 μM | 23729402 | ||
| OV177 | Growth Inhibition Assay | IC50=2.78 ± 0.71 μM | 23729402 | ||
| OVMANAb | Growth Inhibition Assay | IC50=2.58 ± 0.38 μM | 23729402 | ||
| COLO704 | Growth Inhibition Assay | IC50=2.52 ± 0.67 μM | 23729402 | ||
| DU145 | Growth Inhibition Assay | IC50=18 nM | 24356813 | ||
| DT40 | Growth Inhibition Assay | IC50=21 nM | 24356813 | ||
| OVCA429 | Growth Inhibition Assay | IC50=8.29 ± 1.64 μM | 23729402 | ||
| OV167 | Growth Inhibition Assay | IC50=8.33 ± 1.18 μM | 23729402 | ||
| RMG1 | Growth Inhibition Assay | IC50=9.32 ± 2.36 μM | 23729402 | ||
| OVCAR5 | Growth Inhibition Assay | IC50=9.50 ± 2.59 μM | 23729402 | ||
| EFO21 | Growth Inhibition Assay | IC50=9.92 ± 1.87 μM | 23729402 | ||
| ES2 | Growth Inhibition Assay | IC50=10.12 ± 1.23 μM | 23729402 | ||
| Tyk-nu | Growth Inhibition Assay | IC50=10.20 ± 1.12 μM | 23729402 | ||
| CAOV3 | Growth Inhibition Assay | IC50=10.37 ± 0.87 μM | 23729402 | ||
| OV207 | Growth Inhibition Assay | IC50=12.27 ± 0.32 μM | 23729402 | ||
| HEY | Growth Inhibition Assay | IC50=13.01 ± 0.75 μM | 23729402 | ||
| DOV13 | Growth Inhibition Assay | IC50>15 μM | 23729402 | ||
| EFO27 | Growth Inhibition Assay | IC50>15 μM | 23729402 | ||
| HEY C2 | Growth Inhibition Assay | IC50>15 μM | 23729402 | ||
| KOC-7cc | Growth Inhibition Assay | IC50>15 μM | 23729402 | ||
| MCASb | Growth Inhibition Assay | IC50>15 μM | 23729402 | ||
| OAW42 | Growth Inhibition Assay | IC50>15 μM | 23729402 | ||
| OV2008 | Growth Inhibition Assay | IC50>15 μM | 23729402 | ||
| OV90 | Growth Inhibition Assay | IC50>15 μM | 23729402 | ||
| OVCA420b | Growth Inhibition Assay | IC50>15 μM | 23729402 | ||
| OVCA432 | Growth Inhibition Assay | IC50>15 μM | 23729402 | ||
| PEA2 | Growth Inhibition Assay | IC50>15 μM | 23729402 | ||
| SKOV3 | Growth Inhibition Assay | IC50>15 μM | 23729402 | ||
| MDA-MB-468 | Cell Viability Assay | IC50=9.7 μM | 22678161 | ||
| MDA-MB-231 | Cell Viability Assay | IC50=13 μM | 22678161 | ||
| Cal-51 | Cell Viability Assay | IC50=8.6 μM | 22678161 | ||
| MX1 | Cytotoxicity assay | Cytotoxicity against BRCA1-deficient human MX1 cells, EC50 = 0.0053 μM. | 26652717 | ||
| Rosetta2 (DE3) | Function assay | Inhibition of human N-terminal 6xhis-tagged ARTD6 (873 to 1161) expressed in Escherichia coli Rosetta2 (DE3) cells using NAD+ as substrate by fluorescence assay, IC50 = 0.014 μM. | 24900770 | ||
| Rosetta2 (DE3) | Function assay | Inhibition of human 6xhis-tagged ARTD5 (1030 to 1317) expressed in Escherichia coli Rosetta2 (DE3) cells using NAD+ as substrate by fluorescence assay, IC50 = 0.025 μM. | 24900770 | ||
| Capan1 | Cytotoxicity assay | Cytotoxicity against BRCA2-deficient human Capan1 cells, EC50 = 0.609 μM. | 26652717 | ||
| MRC5 | Cytotoxicity assay | Cytotoxicity against human MRC5 cells, EC50 = 8.53 μM. | 26652717 | ||
| A673 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells | 29435139 | ||
| A673 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for A673 cells) | 29435139 | ||
| Rh41 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh41 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 | Rucaparib phosphate是一种PARP抑制剂，无细胞试验中作用于PARP1的Ki为1.4 nM，对其余8个PARP位点也有结合亲和力。Phase 3。 | ||
|---|---|---|---|
| 特性 | AG-014699是第一个用于人类癌症疗法的PARP 抑制剂。 | ||
| 靶点 |
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| 体外研究(In Vitro) | ||||
| 体外研究活性 | AG-014699有效抑制纯化的全长人类PARP-1，作用于LoVo和SW620细胞显示出强PARP抑制效果。AG-014699是AG14447的磷酸盐形式，且是第一个和temozolomide联用用于临床实验的PARP抑制剂。[1] AG-014699的辐射增敏性是由于下游NF-κB激活的抑制，及SSB修复抑制。AG-014699可以作用于DNA损伤激活的NF-κB，且克服传统NF-κB抑制剂的毒性，不会损害其他重要的炎症反应。[2]1μM AG-014699作用于D283Med细胞时抑制PARP-1活性达97.1%。[3]在NB-1691, SH-SY-5Y, 和SKNBE(2c)细胞中AG-014699明显增强Topotecan和Temozolomide的细胞毒性。[4] | |||
|---|---|---|---|---|
| 激酶实验 | 激酶实验 | |||
| 不同浓度(0到1μ)AG-014699作用于5×103D283Med 细胞，与只用DMSO处理5×103D283Med细胞相比，来测定PARP活性抑制率。参考GCLP验证试验的PAR标准曲线，在和NAD+及寡核苷酸(底物和激活剂)温育的6分钟期间，使用10H PAR抗体，通过PAR形成量的免疫检测，在细胞样本中测量最大程度刺激的PARP活性。 | ||||
| 细胞实验 | 细胞系 | D425Med, D283Med和D384Med细胞 | ||
| 浓度 | 0.4 μM | |||
| 孵育时间 | 3或5天 | |||
| 方法 | 髓母细胞瘤细胞系包含D425Med, D283Med，和D384Med细胞，分别按1×103, 3×103，和3×103密度接种在96孔板上。接种24小时(D384Med细胞)或48小时(D283Med和D425Med细胞)后，细胞用不同浓度temozolomide处理。培养3天(D425Med和D384Med细胞)或5天(D283Med细胞)后，通过XTT细胞增殖检测试剂盒检测细胞活力。用DMSO处理的对照组和0.4μ AG-014699处理的实验组的百分比表示细胞生长。计算temozolomide单独使用或者和AG-014699联用时的GI50值。Temozolomide单独使用时的GI50值和与AG-014699联用时的GI50值之比就是趋化因子50（PF50）值。 | |||
| 实验图片 | 检测方法 | 检测指标 | 实验图片 | PMID |
| Western blot | PAR BRCA1 |
|
27960087 | |
| Growth inhibition assay | Cell viability |
|
31119062 | |
| Immunofluorescence | α-tubulin PAR γH2AX 53BP1 |
|
30589644 | |
| 体内研究(In Vivo) | ||
| 体内研究活性 | AG-014699无毒，明显增强D384Med移植瘤DNA修复功能蛋白中temozolomide诱导的TGD。药物动力学研究显示在脑组织中也检测到AG-014699，说明AG-014699用于治疗颅内恶性肿瘤具有潜在可能。[3]活体模型(NB1691和SHSY5Y移植瘤)研究显示AG-014699增强temozolomide的抗癌活性，产生彻底且持久的肿瘤衰退现象。[4] | |
|---|---|---|
| 动物实验 | Animal Models | 携带D283Med移植瘤的CD-1裸鼠 |
| Dosages | 1 mg/kg | |
| Administration | 腹腔注射，每天1次或4次 | |
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT04539327 | Completed | Epithelial Ovarian Cancer|Fallopian Tube Cancer|Primary Peritoneal Cancer |
Grupo Español de Investigación en Cáncer de Ovario|Clovis Oncology Inc. |
July 29 2020 | -- |
| NCT04209595 | Active not recruiting | Small Cell Lung Cancer|Extra-Pulmonary Small Cell Carcinomas |
National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) |
April 8 2020 | Phase 1|Phase 2 |
| NCT04179396 | Completed | Metastatic Castration Resistant Prostate Cancer |
pharmaand GmbH |
December 5 2019 | Phase 1 |
| NCT03824704 | Terminated | Epithelial Ovarian Cancer|Fallopian Tube Cancer|Primary Peritoneal Carcinoma|High Grade Serous Carcinoma|Endometrioid Adenocarcinoma |
pharmaand GmbH|Bristol-Myers Squibb|Foundation Medicine |
August 23 2019 | Phase 2 |
| NCT03840200 | Completed | Breast Cancer|Prostate Cancer|Ovarian Cancer |
Hoffmann-La Roche |
June 12 2019 | Phase 1 |
化学信息&溶解度
| 分子量 | 421.36 | 分子式 | C19H18FN3O.H3PO4 |
| CAS号 | 459868-92-9 | SDF | Download Rucaparib phosphate SDF |
| Smiles | CNCC1=CC=C(C=C1)C2=C3CCNC(=O)C4=C3C(=CC(=C4)F)N2.OP(=O)(O)O | ||
| 储存条件(自收到货起) | |||
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体外溶解度 |
DMSO : 84 mg/mL ( (199.35 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 |
|
体内溶解配方 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）
mg/kg
g
μL
只
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）
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
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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