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- qPCR
- 2x SYBR Green qPCR Master Mix
- 2x SYBR Green qPCR Master Mix(Low ROX)
- 2x SYBR Green qPCR Master Mix(High ROX)
- 蛋白實驗
- Protein A/G免疫沉淀磁珠
- Anti-DYKDDDDK Tag免疫磁珠
- Anti-DYKDDDDK Tag親和凝膠
- Anti-Myc免疫磁珠
- Anti-HA免疫磁珠
- 磁力架
- Poly DYKDDDDK Tag多肽
- 細胞核與細胞漿蛋白抽提試劑盒
- 免疫磁珠
- 蛋白酶抑制劑Cocktail
- 蛋白酶抑制劑Cocktail(DMSO儲液)
- 磷酸酶抑制劑Cocktail
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Rucaparib phosphate
別名: AG-014699 phosphate, PF-01367338 phosphate 中文名稱：瑞卡帕布磷酸鹽
Rucaparib phosphate是一種PARP抑制劑，無細胞試驗中作用于PARP1的Ki為1.4 nM，對其余8個PARP位點也有結(jié)合親和力。Phase 3。
Rucaparib phosphate Chemical Structure
CAS: 459868-92-9
產(chǎn)品質(zhì)控
批次：
純度：
99.87%
99.87
Rucaparib phosphate相關(guān)產(chǎn)品
| 相關(guān)靶點 | PARP1 PARP2 PARP3 Tankyrase-1 Tankyrase-2 PARP14 PARP7 TNKS1 TNKS2 | 點擊展開 |
|---|---|---|
| 相關(guān)產(chǎn)品 | XAV-939 Veliparib (ABT-888) PJ34 HCl AG-14361 Iniparib (BSI-201) A-966492 G007-LK UPF 1069 AZD2461 Pamiparib 3-Aminobenzamide ME0328 NMS-P118 Stenoparib (E7449) NVP-TNKS656 WIKI4 Benzamide NU1025 BGP-15 2HCl Picolinamide BYK204165 Fluzoparib (SHR-3162) | 點擊展開 |
| 相關(guān)化合物庫 | FDA藥物庫 天然產(chǎn)物庫 凋亡分子化合物庫 DNA損傷/ DNA修復(fù)化合物庫 細胞周期化合物庫 | 點擊展開 |
相關(guān)信號通路圖
細胞實驗數(shù)據(jù)示例
| 細胞系 | 實驗類型 | 給藥濃度 | 孵育時間 | 活性描述 | 文獻信息(PMID) |
|---|---|---|---|---|---|
| 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 | ||
| 點擊查看更多細胞系數(shù)據(jù) | |||||
生物活性
| 產(chǎn)品描述 | Rucaparib phosphate是一種PARP抑制劑，無細胞試驗中作用于PARP1的Ki為1.4 nM，對其余8個PARP位點也有結(jié)合親和力。Phase 3。 | ||
|---|---|---|---|
| 特性 | AG-014699是第一個用于人類癌癥療法的PARP 抑制劑。 | ||
| 靶點 |
|
| 體外研究(In Vitro) | ||||
| 體外研究活性 | AG-014699有效抑制純化的全長人類PARP-1，作用于LoVo和SW620細胞顯示出強PARP抑制效果。AG-014699是AG14447的磷酸鹽形式，且是第一個和temozolomide聯(lián)用用于臨床實驗的PARP抑制劑。[1] AG-014699的輻射增敏性是由于下游NF-κB激活的抑制，及SSB修復(fù)抑制。AG-014699可以作用于DNA損傷激活的NF-κB，且克服傳統(tǒng)NF-κB抑制劑的毒性，不會損害其他重要的炎癥反應(yīng)。[2]1μM AG-014699作用于D283Med細胞時抑制PARP-1活性達97.1%。[3]在NB-1691, SH-SY-5Y, 和SKNBE(2c)細胞中AG-014699明顯增強Topotecan和Temozolomide的細胞毒性。[4] | |||
|---|---|---|---|---|
| 激酶實驗 | 激酶實驗 | |||
| 不同濃度(0到1μ)AG-014699作用于5×103D283Med 細胞，與只用DMSO處理5×103D283Med細胞相比，來測定PARP活性抑制率。參考GCLP驗證試驗的PAR標準曲線，在和NAD+及寡核苷酸(底物和激活劑)溫育的6分鐘期間，使用10H PAR抗體，通過PAR形成量的免疫檢測，在細胞樣本中測量最大程度刺激的PARP活性。 | ||||
| 細胞實驗 | 細胞系 | D425Med, D283Med和D384Med細胞 | ||
| 濃度 | 0.4 μM | |||
| 孵育時間 | 3或5天 | |||
| 方法 | 髓母細胞瘤細胞系包含D425Med, D283Med，和D384Med細胞，分別按1×103, 3×103，和3×103密度接種在96孔板上。接種24小時(D384Med細胞)或48小時(D283Med和D425Med細胞)后，細胞用不同濃度temozolomide處理。培養(yǎng)3天(D425Med和D384Med細胞)或5天(D283Med細胞)后，通過XTT細胞增殖檢測試劑盒檢測細胞活力。用DMSO處理的對照組和0.4μ AG-014699處理的實驗組的百分比表示細胞生長。計算temozolomide單獨使用或者和AG-014699聯(lián)用時的GI50值。Temozolomide單獨使用時的GI50值和與AG-014699聯(lián)用時的GI50值之比就是趨化因子50（PF50）值。 | |||
| 實驗圖片 | 檢測方法 | 檢測指標 | 實驗圖片 | PMID |
| Western blot | PAR BRCA1 |
|
27960087 | |
| Growth inhibition assay | Cell viability |
|
31119062 | |
| Immunofluorescence | α-tubulin PAR γH2AX 53BP1 |
|
30589644 | |
| 體內(nèi)研究(In Vivo) | ||
| 體內(nèi)研究活性 | AG-014699無毒，明顯增強D384Med移植瘤DNA修復(fù)功能蛋白中temozolomide誘導(dǎo)的TGD。藥物動力學(xué)研究顯示在腦組織中也檢測到AG-014699，說明AG-014699用于治療顱內(nèi)惡性腫瘤具有潛在可能。[3]活體模型(NB1691和SHSY5Y移植瘤)研究顯示AG-014699增強temozolomide的抗癌活性，產(chǎn)生徹底且持久的腫瘤衰退現(xiàn)象。[4] | |
|---|---|---|
| 動物實驗 | Animal Models | 攜帶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 Espa?ol 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 |
|
化學(xué)信息&溶解度
| 分子量 | 421.36 | 分子式 | C19H18FN3O.H3PO4 |
| CAS號 | 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 | ||
| 儲存條件(自收到貨起) | |||
|
體外溶解度 |
DMSO : 84 mg/mL ( (199.35 mM) ；DMSO吸濕會降低化合物溶解度，請使用新開封DMSO) Water : Insoluble Ethanol : Insoluble |
摩爾濃度計算器 |
|
體內(nèi)溶解配方 現(xiàn)配現(xiàn)用，請按從左到右的順序依次添加，澄清后再加入下一溶劑 |
動物體內(nèi)配方計算器 | |||||
實驗計算
動物體內(nèi)配方計算器（澄清溶液）
第一步：請輸入基本實驗信息（考慮到實驗過程中的損耗，建議多配一只動物的藥量）
mg/kg
g
μL
只
第二步：請輸入動物體內(nèi)配方組成（配方適用于不溶于水的藥物；不同批次藥物配方比例不同，請聯(lián)系Selleck為您提供正確的澄清溶液配方）
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
計算結(jié)果：
工作液濃度： mg/ml；
DMSO母液配制方法： mg 藥物溶于μL DMSO溶液（母液濃度mg/mL，注：如該濃度超過該批次藥物DMSO溶解度，請先聯(lián)系Selleck）；
體內(nèi)配方配制方法：取μL DMSO母液，加入μL PEG300，混勻澄清后加入μL Tween 80，混勻澄清后加入μL ddH2O，混勻澄清。
體內(nèi)配方配制方法：取μL DMSO母液，加入μL Corn oil，混勻澄清。
注意：1. 首先保證母液是澄清的；
2.一定要按照順序依次將溶劑加入，進行下一步操作之前必須保證上一步操作得到的是澄清的溶液，可采用渦旋、超聲或水浴加熱等物理方法助溶。
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