Rucaparib

製品コードS4948 バッチS494803

印刷

化学情報

Chemical Structure Synonyms AG014699, PF01367338 Storage
(From the date of receipt)		 3 years -20°C powder
化学式

C19H18FN3O
分子量 323.36 CAS No. 283173-50-2
Solubility (25°C)* 体外 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.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 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.
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]

プロトコル(参考用のみ)

細胞アッセイ 細胞株 GBM U251 and U87MG cells
濃度 0.1, 1, 10, 100 μM
反応時間 4 days
実験の流れ

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.
動物実験 動物モデル U87MG heterotopic nude mouse model, U87MG orthotopic mouse model
投薬量 4 mg/kg, 10 mg/kg
投与方法 i.p.

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

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

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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