| 中文名 | 瑞卡帕布樟脑磺酸盐 |
| 英文名 | RucaparibCamsylate |
| 别名 | 芦卡帕利 瑞卡帕布樟脑磺酸 瑞卡帕布樟脑磺酸盐 PARP抑制剂(RUCAPARIB CAMSYLATE) |
| 英文别名 | RucaparibCamsylate Rucaparibmonocamsylate RucaparibCamphosulfonate 8‐Fluoro‐2‐(4‐methylaminomethyl‐phenyl)‐1,3,4,5‐tetrahydro‐azepino[5,4,3‐cd]indol‐6‐one (S)‐camphorsulfonate Salt 8-fluoro-2-{4-[(methylamino)methyl]phenyl}-1,3,4,5-tetrahydro-6H-azepino[5,4,3-cd]indol-6-one ((1S,4R)-7,7dimethyl-2-oxobicyclo[2.2.1] hept-1-yl) methanesulfonic acid salt |
| CAS | 1859053-21-6 |
| 化学式 | C29H34FN3O5S |
| 分子量 | 555.6607632 |
| 存储条件 | Room Temprature |
| 体外研究 | Rucaparib is the most potent PARP inhibitor in enzyme assays (K i ,1.4 nM), and a possible N-demethylation metabolite of AG14644. Theradio-sensitization by Rucaparib is due to downstream inhibition ofactivation of NF-κB, and is independent of SSB repair inhibition.Rucaparib could target NF-κB activated by DNA damage and overcometoxicity observed with classical NF-κB inhibitors withoutcompromising other vital inflammatory functions. Rucaparib inhibitsPARP-1 activity by 97.1% at a concentration of 1 μM inpermeabilised D283Med cells. |
| 体内研究 | Rucaparib and AG14584 significantly (P < 0.05) increasestemozolomide toxicity. Rucaparib (1 mg/kg) significantly increasestemozolomide-induced body weight loss. Rucaparib (0.1 mg/kg)results in a 50% increase in the temozolomide-induced tumor growthdelay. Rucaparib is not toxic but significantly enhancestemozolomide-induced TGD in the DNA repair protein-competentD384Med xenografts. Pharmacokinetics studies also show thatRucaparib is detected in the brain tissue, which indicates thatRucaparib has potential in intra-cranial malignancy therapy.Rucaparib significantly potentiates the cytotoxicity of topotecanand temozolomide in NB-1691, SH-SY-5Y, and SKNBE (2c) cells.Rucaparib enhances the antitumor activity of temozolomide andindicates complete and sustained tumor regression in NB1691 andSHSY5Y xenografts. |
