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Rucaparib (AG-014699) PARP inhibitor

Cat.No.S4948

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.
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Quality Control

Batch: Purity: 99.91%
99.91

Solubility

In vitro
Batch:

DMSO : 65 mg/mL (201.01 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 32 mg/mL

Water : Insoluble

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Mass Concentration Volume Molecular Weight
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In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

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Working concentration: mg/ml;

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.

Chemical Information, Storage & Stability

Molecular Weight 323.36 Formula

C19H18FN3O

Storage (From the date of receipt) 3 years -20°C powder
CAS No. 283173-50-2 -- Storage of Stock Solutions

Synonyms AG014699, PF01367338 SMILES CNCC1=CC=C(C=C1)C2=C3CCNC(=O)C4=C3C(=CC(=C4)F)[NH]2

Read more about storage stability stock solution CAS number SMILES

Mechanism of Action

Targets/IC50/Ki
PARP1
(Cell-free assay)
1.4 nM(Ki)
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.

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.

References

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2026-07-29)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03899155 RECRUITING
Cancer
Bristol-Myers Squibb
2019-08-09 PHASE2
NCT03768063 ACTIVE_NOT_RECRUITING
Cancer
Hoffmann-La Roche
2019-02-28 PHASE3
NCT02925234 RECRUITING
Cancer; Tumors; Neoplasm; Neoplasia
The Netherlands Cancer Institute
2016-08 PHASE2
NCT04455750 ACTIVE_NOT_RECRUITING
Castration-Resistant Prostate Carcinoma; Metastatic Prostate Adenocarcinoma; Stage IV Prostate Cancer AJCC v8; Stage IVA Prostate Cancer AJCC v8; Stage IVB Prostate Cancer AJCC v8
Alliance for Clinical Trials in Oncology
2021-10-14 PHASE3
NCT04253262 ACTIVE_NOT_RECRUITING
Metastatic Castration-resistant Prostate Cancer
Brown University
2020-04-03 PHASE1; PHASE2
NCT04624178 ACTIVE_NOT_RECRUITING
Leiomyosarcoma
Memorial Sloan Kettering Cancer Center
2020-11-05 PHASE2

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