瑞卡帕布樟脑磺酸盐CAS: 1859053-21-6原料供应发货可做商检可出口备案
更新时间：2024-05-19 07:00:00
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详细介绍
| 中文名 | 瑞卡帕布樟脑磺酸盐 |
| 英文名 | Rucaparib Camsylate |
| 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 | Rucaparib Camsylate Rucaparib monocamsylate Rucaparib Camphosulfonate 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. 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. |
| 体内研究 | Rucaparib and AG14584 significantly (P < 0.05) increases temozolomide toxicity. Rucaparib (1 mg/kg) significantly increases temozolomide-induced body weight loss. Rucaparib (0.1 mg/kg) results in a 50% increase in the temozolomide-induced tumor growth delay. 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. |
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