Rucaparib
产品说明书
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同义名 : | AG014699; PF-01367338; AG-014447 |
| CAS号 : | 283173-50-2 | |
| 货号 : | A115210 | |
| 分子式 : | C19H18FN3O | |
| 纯度 : | 98% | |
| 分子量 : | 323.36 | |
| MDL号 : | MFCD11977252 | |
| 存储条件： |
Pure form Keep in dark place, sealed in dry, 2-8°C In solvent -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : |
DMSO: 25 mg/mL(77.31 mM)，配合低频超声，并调节pH至4，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO |
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| 动物实验配方： |
| 生物活性 | |||
|---|---|---|---|
| 描述 | PARP1, also called as Poly(ADP-ribose) polymerase, is involved in the signaling of DNA damage. It can recognize and bind DNA single or double-strand breaks, thus possessing various cellular function, including regulation of apoptosis and chromosome stability, gene amplification and transcription, as well as cell division and differentiation. Rucaparib is a potent PARP inhibitor with Ki value of 1.4nM (measured by enzyme assays). Rucaparib at dose ranging in 1-10μM can suppress the level of PAR, as well as induce γ-H2AX, formation and PARP cleavage in a dose-dependent manner indicative of DNA damage and apoptosis, respectively, in MDA-MB468, MDA-MB-231, and Cal-51 cells in the presence of 5% FBS-supplemented DMEM medium for 72h. Rucaparib at concentrations>2.5μM decreased the p-Stat3 in MDA-MB-468 and MDA-MB-231, as well as dose-dependently increased the p-Akt-S473 in MDA-MB-468 and Cal-51 cells. Rucaparib can chemosensitize neuroblastoma cell lines to temozolomide or topotecan in vitro and in vivo. Rucaparib at concentration of 0.4μM caused a significant sensitization of topotecan (1-30nM) and temozolomide (1-200μM) in NB-1691, SH-SY-5Y and SKNBE(2c) cells. Rucaparib (1mg/kg) increased the temozolomide-induced (68mg/kg) tumor growth delay by 50% (to >89 days) and complete and increased the number of mice with complete and persistent tumor regressions (≥100 days). Co-administration of Rucaparib (1mg/kg) with topotecan (1mg/kg) increased total number of complete regressions. | ||
| 实验方案 | |||
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| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
3.09mL 0.62mL 0.31mL |
15.46mL 3.09mL 1.55mL |
30.93mL 6.19mL 3.09mL |
| 参考文献 |
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