中文名:Rucaparib (AG-014699) phosphate
英文名:Rucaparib (AG-014699) phosphate
英文别名:PF-01367338;8-fluoro-5-(4-((methylamino)methyl)phenyl)-3,4-dihydro-2H-azepino[5,4,3-cd]indol-1(6H)-one phosphoric acid
纯度:10mM in DMSO
货号:R407993
包装:1ml
Cas号:459868-92-9
存储温度:-80℃储存
产品介绍:
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%
查看阿拉丁官网此产品相关对应页面:https://www.aladdin-e.com/zh_cn/R407993.html
![](https://www.aladdin-e.com/media/about/about_1.jpg)
![](https://www.aladdin-e.com/media/about/about_2.jpg)
![](https://www.aladdin-e.com/media/about/about_3.jpg)
![](https://www.aladdin-e.com/media/about/about_4.jpg)
关键字: 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((股票代码:688179),专注于科研试剂的研发、生产和销售,已陆续建立多个工厂和研发中心。作为领军企业,阿拉丁始终坚持质量第一,连续13年被评为“最受欢迎试剂品牌”。
阿拉丁目前常备库存试剂产品品种超过7万种,SKU总数超过46万,产品线涵盖了化学试剂、生化试剂、药靶配体、蛋白质和抗体等多个领域,是国内少数化学试剂到生物试剂全面发展的国产试剂品牌,产品同步发布在我们国内外电商平台。