瑞卡帕布樟脑磺酸盐
中文名称 | 瑞卡帕布樟脑磺酸盐 |
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中文同义词 | 瑞卡帕布樟脑磺酸盐;芦卡帕利;英文同义词: RUCAPARIB CAMSYLATE;PARP抑制剂(RUCAPARIB CAMSYLATE);瑞卡帕布樟脑磺酸;瑞卡帕布樟脑磺酸盐|||RUCAPARIB CAMSYLATE;8-氟-5-(4-((甲氨基)甲基)苯基)-2,3,4,6-四氢-1H-氮杂卓并[5,4,3-CD]吲哚-1-酮 ((1S,4R)-7,7-二甲基-2-氧代双环[2.2.1]庚烷-1-基)甲磺酸盐 |
英文名称 | Rucaparib Camsylate |
英文同义词 | Rucaparib Camsylate;8‐Fluoro‐2‐(4‐methylaminomethyl‐phenyl)‐1,3,4,5‐tetrahydro‐azepino[5,4,3‐cd] indol‐6‐one (S)‐camphorsulfonate Salt;Rucaparib Camphosulfonate;Bicyclo[2.2.1]heptane-1-methanesulfonic acid, 7,7-dimethyl-2-oxo-, (1S,4R)-, compd. with 8-fluoro-1,3,4,5-tetrahydro-2-[4-[(methylamino)methyl]phenyl]-6H-pyrrolo[4,3,2-ef][2]benzazepin-6-one (1:1);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;Rucaparib monocamsylate;Asciminib Impurity 1;8-Fluoro-5-(4-((methylamino)methyl)phenyl)-2,3,4,6-tetrahydro-1H-azepino[5,4,3-cd]indol-1-one ((1S,4R)-7,7-dimethyl-2-oxobicyclo[2.2.1]heptan-1-yl)methanesulfonate |
CAS号 | 1859053-21-6 |
分子式 | C29H34FN3O5S |
分子量 | 555.67 |
EINECS号 | |
相关类别 | 细胞生物学试剂;医药原料 |
Mol文件 | 1859053-21-6.mol |
结构式 |
瑞卡帕布樟脑磺酸盐 性质
储存条件 | Store at -20°C |
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溶解度 | DMSO:79.63(最大浓度 mg/mL);143.31(最大浓度 mM) |
形态 | 固体 |
颜色 | 浅黄至灰色 |
PARP-1 1.4 nM (Ki) |
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.
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.
安全信息
更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
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2024/08/19 | HY-102003 | 瑞卡帕布樟脑磺酸盐 Rucaparib monocamsylate | 1859053-21-6 | 5 mg | 700元 |
2024/08/19 | HY-102003 | 瑞卡帕布樟脑磺酸盐 Rucaparib monocamsylate | 1859053-21-6 | 10 mM * 1 mLin DMSO | 855元 |