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 44 publications

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
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
DNA binding and RAD51 engagement by the BRCA2 C-terminus orchestrate DNA repair and replication fork preservation [ Nat Commun, 2023, 14(1):432]	PubMed: 36702902
BRCA2 Germline Mutations Identify Gastric Cancers Responsive to PARP Inhibitors [ Cancer Res, 2023, 83(10):1699-1710]	PubMed: 37129948
Thioparib inhibits homologous recombination repair, activates the type I IFN response, and overcomes olaparib resistance [ EMBO Mol Med, 2023, e16235.]	PubMed: 36652375
PARP inhibitor shuts down the global translation of thyroid cancer through promoting Pol II binding to DIMT1 pause [ Int J Biol Sci, 2023, 19(12):3970-3986]	PubMed: 37564214
Geometrical isomerization of arachidonic acid during lipid peroxidation interferes with ferroptosis [ Free Radic Biol Med, 2023, 204:374-384]	PubMed: 37257700
PARP1 mediated PARylation contributes to myogenic progression and glucocorticoid transcriptional response [ Cell Death Discov, 2023, 9(1):133]	PubMed: 37087471

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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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