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 No. 283173-50-2

Purity & Quality Control

Rucaparib Related Products

Signaling Pathway

PARP Signaling Pathways

PARP Signaling Pathway

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 Information & 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


Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.


In vivo Formulation Calculator

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In vivo Formulation Calculator (Clear solution)

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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.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

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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