Rucaparib

Catalog No.S4948 Batch:S494803

Technical Data

Formula

C₁₉H₁₈FN₃O

Molecular Weight

323.36

CAS No.

283173-50-2

Solubility (25°C)*

In vitro

DMSO

65 mg/mL (201.01 mM)

Ethanol

5 mg/mL (15.46 mM)

Water

Insoluble

In vivo (Add solvents to the product individually and in order)

Homogeneous suspension

CMC-NA

≥5mg/ml

Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

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

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]

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]

Protocol (from reference)

Cell Assay:^{^[2]}	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.
Animal Study:^{^[2]}	Animal Models U87MG heterotopic nude mouse model, U87MG orthotopic mouse model Dosages 4 mg/kg, 10 mg/kg Administration i.p.

Cell Assay:^{^[2]}

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.

Animal Study:^{^[2]}

Animal Models
U87MG heterotopic nude mouse model, U87MG orthotopic mouse model
Dosages
4 mg/kg, 10 mg/kg
Administration
i.p.

References

https://pubmed.ncbi.nlm.nih.gov/17363489/
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8150626/

Selleck's Rucaparib Has Been Cited by 72 Publications

Combining Multiplexed CRISPR/Cas9-Nickase and PARP Inhibitors Efficiently and Precisely Targets Cancer Cells [ Cancer Res, 2025, 10.1158/0008-5472.CAN-24-2938]	PubMed: 40327605
ZNF251 haploinsufficiency confers PARP inhibitors resistance in BRCA1-mutated cancer cells through activation of homologous recombination [ Cancer Lett, 2025, 613:217505]	PubMed: 39892701
PARP inhibition augments immunomodulatory function of mesenchymal stem/stromal cells by promoting STAT1 phosphorylation [ Stem Cell Res Ther, 2025, 16(1):548]	PubMed: 41063195
PARP inhibitors elicit distinct transcriptional programs in homologous recombination competent castration-resistant prostate cancer [ Mol Oncol, 2025, 10.1002/1878-0261.70098]	PubMed: 40915979
Homologous Repair-Deficient Pancreatic Cancer: Refined Targeting of DNA Damage Response is an Effective Therapeutic Strategy [ United Eur Gastroent, 2025, 13(7):1328-1342]	PubMed: 40823818
ATR Inhibition Synergizes With Alkylating PI Polyamide Targeting MYCN by Suppressing DNA Repair in MYCN-Amplified Neuroblastoma [ Cancer Sci, 2025, 10.1111/cas.70043]	PubMed: 40052411
The clinically applied PARP inhibitor talazoparib ameliorates imiquimod-induced psoriasis in mice without reducing skin inflammation [ Front Pharmacol, 2025, 16:1519066]	PubMed: 40046735
Targeting Latent HIV Reservoirs: Effectiveness of Combination Therapy with HDAC and PARP Inhibitors [ Viruses, 2025, 17(3)400]	PubMed: 40143326
Lack of synergy between AR targeted therapies and PARP inhibitors in homologous recombination-proficient prostate cancer [ bioRxiv, 2025, 2025.06.02.657429]	PubMed: 40501631
PARP inhibitor response is enhanced in prostate cancer when XRCC1 expression is reduced [ NAR Cancer, 2025, 7(2):zcaf015]	PubMed: 40271221

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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