Rucaparib

Catalog No.S4948 Batch:S494801

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	32 mg/mL (98.96 mM)
		Water	Insoluble
* <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.)

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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

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

Selleck's Rucaparib has been cited by 60 publications

Discovery of a small-molecule inhibitor that traps Polθ on DNA and synergizes with PARP inhibitors [ Nat Commun, 2024, 15(1):2862]	PubMed: 38580648
DNA-PK participates in pre-rRNA biogenesis independent of DNA double-strand break repair [ Nucleic Acids Res, 2024, gkae316]	PubMed: 38682589
PARP inhibitors suppress tumours via centrosome error-induced senescence independent of DNA damage response [ EBioMedicine, 2024, 103:105129]	PubMed: 38640836
Conjugated fatty acids drive ferroptosis through chaperone-mediated autophagic degradation of GPX4 by targeting mitochondria [ Cell Death Dis, 2024, 15(12):884]	PubMed: 39643606
Minimizing DNA trapping while maintaining activity inhibition via selective PARP1 degrader [ Cell Death Dis, 2024, 15(12):898]	PubMed: 39695097
Identification of differential biological activity and synergy between the PARP inhibitor rucaparib and its major metabolite [ Cell Chem Biol, 2024, S2451-9456(24)00043-6]	PubMed: 38335967
Aggregability of the SQSTM1/p62-based aggresome-like induced structures determines the sensitivity to parthanatos [ Cell Death Discov, 2024, 10(1):74]	PubMed: 38346947
Role of Exogenous Pyruvate in Maintaining Adenosine Triphosphate Production under High-Glucose Conditions through PARP-Dependent Glycolysis and PARP-Independent Tricarboxylic Acid Cycle [ Int J Mol Sci, 2024, 25(20)11089]	PubMed: 39456870
Silencing of Epidermal Growth Factor-like Domain 8 Promotes Proliferation and Cancer Aggressiveness in Human Ovarian Cancer Cells by Activating ERK/MAPK Signaling Cascades [ Int J Mol Sci, 2024, 26(1)274]	PubMed: 39796130
Molecular Basis of XRN2-Deficient Cancer Cell Sensitivity to Poly(ADP-ribose) Polymerase Inhibition [ Cancers (Basel), 2024, 16(3)595]	PubMed: 38339346

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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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