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
体内 （毎回新しく調製した物を用意してください）
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
* <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.

参考

  • https://pubmed.ncbi.nlm.nih.gov/17363489/
  • https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8150626/

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：

Combining Multiplexed CRISPR/Cas9-Nickase and PARP Inhibitors Efficiently and Precisely Targets Cancer Cells [ Cancer Res, 2025, 10.1158/0008-5472.CAN-24-2938] PubMed: 40327605
ZNF251 haploinsufficiency confers PARP inhibitors resistance in BRCA1-mutated cancer cells through activation of homologous recombination [ Cancer Lett, 2025, 613:217505] PubMed: 39892701
PARP inhibition augments immunomodulatory function of mesenchymal stem/stromal cells by promoting STAT1 phosphorylation [ Stem Cell Res Ther, 2025, 16(1):548] PubMed: 41063195
PARP inhibitors elicit distinct transcriptional programs in homologous recombination competent castration-resistant prostate cancer [ Mol Oncol, 2025, 10.1002/1878-0261.70098] PubMed: 40915979
Homologous Repair-Deficient Pancreatic Cancer: Refined Targeting of DNA Damage Response is an Effective Therapeutic Strategy [ United Eur Gastroent, 2025, 13(7):1328-1342] PubMed: 40823818
ATR Inhibition Synergizes With Alkylating PI Polyamide Targeting MYCN by Suppressing DNA Repair in MYCN-Amplified Neuroblastoma [ Cancer Sci, 2025, 10.1111/cas.70043] PubMed: 40052411
The clinically applied PARP inhibitor talazoparib ameliorates imiquimod-induced psoriasis in mice without reducing skin inflammation [ Front Pharmacol, 2025, 16:1519066] PubMed: 40046735
Targeting Latent HIV Reservoirs: Effectiveness of Combination Therapy with HDAC and PARP Inhibitors [ Viruses, 2025, 17(3)400] PubMed: 40143326
Lack of synergy between AR targeted therapies and PARP inhibitors in homologous recombination-proficient prostate cancer [ bioRxiv, 2025, 2025.06.02.657429] PubMed: 40501631
PARP inhibitor response is enhanced in prostate cancer when XRCC1 expression is reduced [ NAR Cancer, 2025, 7(2):zcaf015] PubMed: 40271221

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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