Home DNA Damage/DNA Repair PARP inhibitor Rucaparib For research use only.

Rucaparib

Synonyms: AG014699, PF01367338

Rucaparib 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.

Rucaparib Chemical Structure

Rucaparib Chemical Structure

CAS: 283173-50-2

Selleck's Rucaparib has been cited by 38 publications

Purity & Quality Control

Batch: Purity: 99.91%
99.91

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Biological Activity

Description Rucaparib 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.
Targets
PARP1 [1]
(Cell-free assay)
1.4 nM(Ki)
In vitro
In vitro

Rucaparib, the PARP inhibitor, exhibits a synergetic antiproliferative effect by enhancing apoptosis and DNA damage and reducing HR repair in BRCA-proficient GBM when combined with PI3K inhibitor BKM120.[2]
Cell Research Cell lines GBM U251 and U87MG cells
Concentrations 0.1, 1, 10, 100 μM
Incubation Time 4 days
Method

Cell proliferation is measured by MTT assay. The cells are seeded at a density of 5×103 cells/ml in a volume of 200 μl/well in 96-well plates. The next day, cells are treated with DMSO or a series of concentrations of BKM120 or rucaparib. Four days later, 20 μl of MTT (5 mg/ml) is added to each well. After further incubation for 4 h at 37 ℃, the absorbance at 490 nm is measured. Data obtained from the growth inhibitory experiments are analyzed by CalcuSyn software to determine the drug combination effect. Combination indexes (CI) are then calculated.
In Vivo
In vivo

Rucaparib combined with BKM120 enhances the antitumor efficacy in a nude mouse U87MG subcutaneous xenograft model and nude mouse U87MG orthotopic xenograft model.[2]
Animal Research Animal Models U87MG heterotopic nude mouse model, U87MG orthotopic mouse model
Dosages 4 mg/kg, 10 mg/kg
Administration 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

Chemical lnformation & Solubility

Molecular Weight 323.36 Formula

C19H18FN3O
CAS No. 283173-50-2 SDF --
Smiles CNCC1=CC=C(C=C1)C2=C3CCNC(=O)C4=C3C(=CC(=C4)F)[NH]2
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 65 mg/mL ( (201.01 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 32 mg/mL

Water : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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