Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Rucaparib monocamsylate (Rucaparib Camsylate) 是一种口服有效的 PARP 蛋白抑制剂,对 PARP-1 的Ki 为 1.4 nM。它是六磷酸己糖脱氢酶 (H6PD) 抑制剂,有用于去势抵抗性前列腺癌 (CRPC) 的研究潜力。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 248 | 现货 | ||
5 mg | ¥ 578 | 现货 | ||
10 mg | ¥ 975 | 现货 | ||
25 mg | ¥ 1,670 | 现货 | ||
50 mg | ¥ 2,490 | 现货 | ||
100 mg | ¥ 3,730 | 现货 | ||
200 mg | ¥ 5,330 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 693 | 现货 |
产品描述 | Rucaparib monocamsylate (Rucaparib Camsylate) is a PARP inhibitor (PARP1,Ki of 1.4 nM). Rucaparib Camsylate also displays binding affinity to eight other PARP domains. |
靶点活性 | PARP1:1.4 nM (Ki) |
体外活性 | Rucaparib is the most effective PARP inhibitor in enzyme assays (Ki: 1.4 nM). Rucaparib inhibits PARP-1 activity by 97.1% at a concentration of 1 μM in permeabilized D283Med cells. Rucaparib could target NF-κB activated by DNA damage and overcome toxicity observed with classical NF-κB inhibitors without compromising other vital inflammatory functions. The radio-sensitization by Rucaparib is due to downstream inhibition of activation of NF-κB and is independent of SSB repair inhibition [1][2][3]. |
体内活性 | Rucaparib is not toxic but obviously enhances temozolomide-induced TGD in the DNA repair protein-competent D384Med xenografts. Rucaparib and AG14584 obviously (P < 0.05) increase temozolomide toxicity. Rucaparib enhances the antitumor activity of temozolomide and indicates complete and sustained tumor regression in NB1691 and SHSY5Y xenografts. Rucaparib significantly potentiates the cytotoxicity of topotecan and temozolomide in NB-1691, SH-SY-5Y, and SKNBE (2c) cells. 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. Pharmacokinetics studies also show that Rucaparib is detected in the brain tissue, which indicates that Rucaparib has potential in intra-cranial malignancy therapy [1][3][4]. |
别名 | 瑞卡帕布樟脑磺酸盐, Rucaparib Camsylate |
分子量 | 555.66 |
分子式 | C29H34FN3O5S |
CAS No. | 1859053-21-6 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 82.33 mg/mL(148.17 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 1.7997 mL | 8.9983 mL | 17.9966 mL | 44.9915 mL |
5 mM | 0.3599 mL | 1.7997 mL | 3.5993 mL | 8.9983 mL | |
10 mM | 0.18 mL | 0.8998 mL | 1.7997 mL | 4.4992 mL | |
20 mM | 0.09 mL | 0.4499 mL | 0.8998 mL | 2.2496 mL | |
50 mM | 0.036 mL | 0.18 mL | 0.3599 mL | 0.8998 mL | |
100 mM | 0.018 mL | 0.09 mL | 0.18 mL | 0.4499 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
Rucaparib monocamsylate 1859053-21-6 Chromatin/Epigenetic DNA Damage/DNA Repair PARP repair H6PD BRCA1 poly ADP ribose polymerase AG14644 SSB 瑞卡帕布樟脑磺酸盐 PF-01367338 monocamsylate Capan-1 Inhibitor AG014699 monocamsylate NF-κB inhibit MX-1 BRCA2 Rucaparib Camsylate inhibitor