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Synonyms | AG014699, PF01367338 | Storage (From the date of receipt) |
3 years -20°C powder | |
化学式 | C19H18FN3O |
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分子量 | 323.36 | CAS No. | 283173-50-2 | |
Solubility (25°C)* | 体外 | 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. |
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. |
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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] |
細胞アッセイ | 細胞株 | GBM U251 and U87MG cells |
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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. |
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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. |
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Discovery of a small-molecule inhibitor that traps Polθ on DNA and synergizes with PARP inhibitors [ Nat Commun, 2024, 15(1):2862] | PubMed: 38580648 |
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 |
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 |
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。
各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。