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瑞卡帕布樟脑磺酸盐  ≥98%

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包装规格：5mg 10mg 25mg 50mg 100mg in glass bottle
溶解性：溶于DMSO（83.33mg/mL 超声）
产品描述：基本信息 产品编号：R10282 产品名称：Rucaparib Camsylate CAS: 1859053-21-6   储存条件 粉末 -20℃ 四年     分子式： C29H34FN3O5S 溶于液体 -80℃ 两年 分子量 555.66 -20℃ 一个月 化学名：  [(1S,4R)-7,7-dimethyl-2-oxo-1-bicyclo[2.2.1]heptanyl]methanesulfonic acid;6-fluoro-2-[4-(methylaminomethyl)phenyl]-3,10-diazatricyclo[6.4.1.04,13]trideca-1,4,6,8(13)-tetraen-9-one   Solubility (25°C)   体外 DMSO 100mg/mL (179.96mM) Ethanol Insoluble Water Insoluble 体内 现配现用   ＜1mg/ml表示微溶或不溶。 普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。   制备储备液   浓度   溶液体积 质量   1mg   5mg   10mg 1mM 1.7997mL 8.9983mL 17.9966mL 5mM 0.3599mL 1.7997mL 3.5993mL 10mM 0.1800mL 0.8998mL 1.7997mL 50mM 0.0360mL 0.1800mL 0.3599mL   生物活性 产品描述 PARP 的抑制剂，对 PARP1 的 Ki 值为 1.4nM。Rucaparib Camsylate 也可结合 PARP 其他八个结构域。 靶点/IC50 PARP1 (Cell-free assay) 1.4nM(Ki)   体外研究 Rucaparib is the most potent PARP inhibitor in enzyme assays (Ki, 1.4nM), 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 1μM in permeabilised D283Med cells.   体内研究 Rucaparib and AG14584 significantly (P < 0.05) increases temozolomide toxicity. Rucaparib (1mg/kg) significantly increases temozolomide-induced body weight loss. Rucaparib (0.1mg/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.   推荐实验方法(仅供参考) 激酶实验： Kinase Assay Inhibition of PARP activity in 5×103 D283Med cells is measured using various concentrations of Rucaparib (0-1μM),compared with DMSO-only. Maximally stimulated PARP activity is measured in samples of permeabilised cells by immunologica   细胞实验:   Cell Assay Medulloblastoma cell lines are seeded in 96-well plates at a density of 1×103, 3×103 and 3×103, respectively. At 24 hours(D384Med) or 48 hours (D283Med and D425Med) after seeding, the cells are exposed to various concentrations of temozolomide in the presence or absence of 0.4μM Rucaparib. After 3 days (D425Med and D384Med) or 5 days (D283Med) of culture, cell viability is evaluated by a XTT cell proliferation kit assay. Cell growth is expressed as a percentage in relation to DMSO or 0.4μM Rucaparib-alone controls. The concentration of temozolomide, alone or in combination with Rucaparib that inhibited growth by 50% (GI50) is calculated. The potentiation factor 50 (PF50) is defined as the ratio of the GI50 of temozolomide in the presence of Rucaparib to the GI50 of temozolomide alone.   动物实验:   Animal Administration A single dose of temozolomide is administrated p.o. as a suspension in saline at 200mg/kg either alone or in combination with a single i.p. administration of PARP inhibitor administered at 0.1 [Rucaparib and MS-AG14644 (equivalent to 0.078mg/kg free AG14644 only)], 1.0, and 10mg/kg (for the mesylate salts equivalent to 0.79 and 7.9mg/kg free AG14451 and AG14452 and 0.78 and 7.8 free AG14531 and AG14644). Control animals are treated with either normal saline p.o. and i.p or normal saline p.o and PARP inhibitor 10 mg/kg i.p.
保存条件：-20℃

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