中文名：Rucaparib (AG-014699) phosphate
英文名：Rucaparib (AG-014699) phosphate
英文別名：PF-01367338;8-fluoro-5-(4-((methylamino)methyl)phenyl)-3,4-dihydro-2H-azepino[5,4,3-cd]indol-1(6H)-one phosphoric acid
純度：10mM in DMSO
貨號：R407993
包裝：1ml
Cas號：459868-92-9
存儲溫度：-80℃儲存
產(chǎn)品介紹：
Information
Rucaparib (AG-014699) phosphate Rucaparib (AG-014699, PF-01367338) is an inhibitor of PARP with K i of 1.4 nM for PARP1 in a cell-free assay, also showing binding affinity to eight other PARP domains. Phase 3.
In?vitro
Rucaparib is a potent inhibitor of purified full-length human PARP-1 and shows higher inhibition of cellular PARP in LoVo and SW620 cells. Besides, Rucaparib binds detectably to eight other PARP domains, including PARP2, 3, 4, 10, 15, 16, TNKS1 and TNKS2. The radio-sensitization by Rucaparib is due to downstream inhibition of activation of NF-κB, and is independent of SSB repair inhibition. Rucaparib could target NF-κB activated by DNA damage and overcome toxicity observed with classical NF-κB inhibitors without compromising other vital inflammatory functions. Rucaparib inhibits PARP-1 activity by 97.1% at a concentration of 1 μM in permeabilised D283Med cells.
In?vivo
Rucaparib is not toxic but significantly enhances temozolomide-induced TGD in the DNA repair protein-competent D384Med xenografts. Pharmacokinetics studies also show that Rucaparib is detected in the brain tissue, which indicates that Rucaparib has potential in intra-cranial malignancy therapy. Rucaparib significantly potentiates the cytotoxicity of topotecan and temozolomide in NB-1691, SH-SY-5Y, and SKNBE (2c) cells. Rucaparib enhances the antitumor activity of temozolomide and indicates complete and sustained tumor regression in NB1691 and SHSY5Y xenografts.
Cell?Data
cell?lines：
Concentrations：0.4 μM
Incubation?Time：3 or 5 days
Powder?Purity:≥99%
查看阿拉丁官網(wǎng)此產(chǎn)品相關(guān)對應(yīng)頁面：https://www.aladdin-e.com/zh_cn/R407993.html
關(guān)鍵字： PF-01367338;8-fluoro-5-(4-((methylamino)methyl)phenyl)-3,4-dihydro-2H-azepino[5,4,3-cd]indol-1(6H)-one phosphoric acid
上海阿拉丁生化科技股份有限公司是A股上市公司（（股票代碼：688179），專注于科研試劑的研發(fā)、生產(chǎn)和銷售，已陸續(xù)建立多個工廠和研發(fā)中心。作為領(lǐng)軍企業(yè)，阿拉丁始終堅持質(zhì)量第一，連續(xù)13年被評為“最受歡迎試劑品牌”。
阿拉丁目前常備庫存試劑產(chǎn)品品種超過7萬種，SKU總數(shù)超過46萬，產(chǎn)品線涵蓋了化學(xué)試劑、生化試劑、藥靶配體、蛋白質(zhì)和抗體等多個領(lǐng)域，是國內(nèi)少數(shù)化學(xué)試劑到生物試劑全面發(fā)展的國產(chǎn)試劑品牌，產(chǎn)品同步發(fā)布在我們國內(nèi)外電商平臺。