Rucaparib，也稱為AG-014699或PF-01367338，是一種聚(ADP核糖)聚合酶(PARP)抑制劑。PARP是一種DNA損傷激活的核酶，在堿基切除修復(fù)途徑中具有關(guān)鍵的信號作用。因此，還發(fā)現(xiàn)rucaparib在DNA修復(fù)缺陷的細(xì)胞中最有效，其中所述缺陷細(xì)胞是由暴露于基因毒性劑引起的，例如輻射產(chǎn)生DNA損傷，并且當(dāng)DNA修復(fù)受損時其毒性增強(qiáng)。通過γ-H2AX和p53BP1病灶確定，rucaparib存在時放射敏感性增加與持續(xù)DNA斷裂相關(guān)。Rucaparib放射增敏前列腺癌細(xì)胞，最有效的是那些PTEN缺陷和表達(dá)ETS基因融合蛋白的細(xì)胞，其抑制NHEJ DNA修復(fù)。

產(chǎn)品性質(zhì)：

Cas No.：459868-92-9

別名：瑞卡帕布磷酸鹽; AG-014699 phosphate; PF-01367338 phosphate

化學(xué)名：8-fluoro-2-(4-((methylamino)methyl)phenyl)-4,5-dihydro-1H-azepino[5,4,3-cd]indol-6(3H)-one phosphate

Canonical SMILES：OP(O)(O)=O.FC1=CC2=C3C(CCNC2=O)=C(C4=CC=C(CNC)C=C4)NC3=C1

分子式：C19H18FN3O.H3PO4

分子量：421.36

溶解度：≥ 21.1 mg/mL in DMSO

儲存條件：Store at -20°C

注意事項：

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References

[1].Ruth Plummer, Paul Lorigan, Neil Steven, Lucy Scott, Mark R. Middleton, Richard H. Wilson, Evan Mulligan, Nicola Curtin, Diane Wang, Raz Dewji, Antonello Abbattista, Jorge Gallo, Hilary Calvert. A phase II study of the potent PARP inhibitor, Rucaparib (PF-01367338, AG014699), with temozolomide in patients with metastatic melanoma demonstrating evidence of chemopotentiation.

[2].Payel Chatterjee, Gaurav Choudhary, Warren D. Heston, Eric A. Klein, Alex Almasan. The PARP inhibitor rucaparib radiosensitizes prostate cancer cells, most effectively those that are PTEN-deficient and are expressing ETS gene fusion proteins, which inhibit NHEJ DNA repair. Cancer Research. 2012. 72: B27.