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
* <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 52 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
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
Molecular Basis of XRN2-Deficient Cancer Cell Sensitivity to Poly(ADP-ribose) Polymerase Inhibition [ Cancers (Basel), 2024, 16(3)595]	PubMed: 38339346
Poly (ADP-ribose) polymerase inhibitor sensitized DNA damage caused by an alkylating pyrrole-imidazole polyamide targeting MYCN in neuroblastoma cells [ Biochem Biophys Res Commun, 2024, 735:150794]	PubMed: 39395371
Polθ is phosphorylated by PLK1 to repair double-strand breaks in mitosis [ Nature, 2023, 621(7978):415-422]	PubMed: 37674080
Polθ is phosphorylated by PLK1 to repair double-strand breaks in mitosis [ Nature, 2023, 621(7978):415-422]	PubMed: 37674080
Repression of LSD1 potentiates homologous recombination-proficient ovarian cancer to PARP inhibitors through down-regulation of BRCA1/2 and RAD51 [ Nat Commun, 2023, 10.1038/s41467-023-42850-x]	PubMed: 37973845

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SHIPPING AND STORAGE
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