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Rucaparib phosphate

別名：AG-014699 phosphate, PF-01367338 phosphate

Rucaparib phosphate is an inhibitor of PARP with Ki of 1.4 nM for PARP1 in a cell-free assay, also showing binding affinity to eight other PARP domains. Phase 3.

Rucaparib phosphate化学構造

CAS No. 459868-92-9

サイズ 価格(税別) 在庫状況
10mM (1mL in DMSO) JPY 29500 国内在庫あり
JPY 22000 国内在庫あり
JPY 31500 国内在庫あり
JPY 100500 国内在庫あり
JPY 250500 国内在庫なし(納期7~10日)

代表番号: 045-509-1970|電子メール：[email protected]
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Rucaparib phosphate関連製品

シグナル伝達経路

PARP Signaling Pathways

PARPシグナル伝達経路

PARP阻害剤の選択性比較

Cell Data

Cell Lines Assay Type Concentration Incubation Time 活性情報 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
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生物活性

製品説明 Rucaparib phosphate is an inhibitor of PARP with Ki of 1.4 nM for PARP1 in a cell-free assay, also showing binding affinity to eight other PARP domains. Phase 3.
特性 The first PARP inhibitor used in clinical trials combined with temozolomide.
Targets
PARP [1]
(Cell-free assay)
1.4 nM(Ki)
In Vitro
In vitro Rucaparib is a potent inhibitor of purified full-length human PARP-1 and shows higher inhibition of cellular PARP in LoVo and SW620 cells. Besides, Rucaparib binds detectably to eight other PARP domains, including PARP2, 3, 4, 10, 15, 16, TNKS1 and TNKS2. [1] [2] The radio-sensitization by Rucaparib is due to downstream inhibition of activation of NF-κB, and is independent of SSB repair inhibition. Rucaparib could target NF-κB activated by DNA damage and overcome toxicity observed with classical NF-κB inhibitors without compromising other vital inflammatory functions. [3] Rucaparib inhibits PARP-1 activity by 97.1% at a concentration of 1 μM in permeabilised D283Med cells. [4]
Kinase Assay Ki Determination
Inhibition of human full-length recombinant PARP-1 by [32P]NAD+ incorporation is measured. The [32P]ADP-ribose incorporated into acid insoluble material is quantified using a PhosphorImager. Ki is calculated by nonlinear regression analysis.
細胞実験 細胞株 D425Med, D283Med and D384Med cells
濃度 0.4 μM
反応時間 3 or 5 days
実験の流れ Medulloblastoma cell lines are seeded in 96-well plates at a density of 1 × 103, 3 × 103 and 3 × 103, respectively. At 24 hours (D384Med) or 48 hours (D283Med and D425Med) after seeding, the cells are exposed to various concentrations of temozolomide in the presence or absence of 0.4 μM Rucaparib. After 3 days (D425Med and D384Med) or 5 days (D283Med) of culture, cell viability is evaluated by a XTT cell proliferation kit assay. Cell growth is expressed as a percentage in relation to DMSO or 0.4 μM Rucaparib-alone controls. The concentration of temozolomide, alone or in combination with Rucaparib that inhibited growth by 50% (GI50) is calculated. The potentiation factor 50 (PF50) is defined as the ratio of the GI50 of temozolomide in the presence of Rucaparib to the GI50 of temozolomide alone.
実験結果図 Methods Biomarkers 結果図 PMID
Western blot PAR BRCA1 27960087
Growth inhibition assay Cell viability 31119062
Immunofluorescence α-tubulin PAR γH2AX 53BP1 30589644
In Vivo
In Vivo Rucaparib is not toxic but significantly enhances temozolomide-induced TGD in the DNA repair protein-competent D384Med xenografts. Pharmacokinetics studies also show that Rucaparib is detected in the brain tissue, which indicates that Rucaparib has potential in intra-cranial malignancy therapy. [4] Rucaparib significantly potentiates the cytotoxicity of topotecan and temozolomide in NB-1691, SH-SY-5Y, and SKNBE (2c) cells. Rucaparib enhances the antitumor activity of temozolomide and indicates complete and sustained tumor regression in NB1691 and SHSY5Y xenografts. [5]
動物実験 動物モデル CD-1 nude mice bearing established D283Med xenografts
投与量 1 mg/kg
投与経路 One or four daily by i.p.
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

化学情報

分子量 421.36 化学式

C19H18FN3O.H3PO4
CAS No. 459868-92-9 SDF Download Rucaparib phosphate SDFをダウンロードする
Smiles CNCC1=CC=C(C=C1)C2=C3CCNC(=O)C4=C3C(=CC(=C4)F)N2.OP(=O)(O)O
保管

In vitro
Batch:

DMSO : 84 mg/mL ( (199.35 mM)； 吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。)

Water : Insoluble

Ethanol : Insoluble

モル濃度計算器

in vivo
Batch:

Add solvents to the product individually and in order.

投与溶液組成計算機

実験計算

モル濃度計算器

質量 濃度 体積 分子量

投与溶液組成計算機(クリア溶液)

ステップ１：実験データを入力してください。（実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します）

mg/kg g μL 匹

ステップ２：投与溶媒の組成を入力してください。（ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください）

% DMSO % % Tween 80 % ddH2O
%DMSO %

計算結果：

投与溶媒濃度： mg/ml;

DMSOストック溶液調製方法： mg 試薬を μL DMSOに溶解する（濃度 mg/mL, 注：濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )

投与溶媒調製方法：Take μL DMSOストック溶液に μL PEG300，を加え、完全溶解後μL Tween 80，を加えて完全溶解させた後 μL ddH2O，を加え完全に溶解させます。

投与溶媒調製方法：μL DMSOストック溶液に μL Corn oil，を加え、完全溶解。

注意：１.ストック溶液に沈殿、混濁などがないことをご確認ください；
２.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。

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