Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Fluzoparib (SHR3162) 是口服活性 PARP1抑制剂,IC50为1.46±0.72 nM,在体内具有良好的药代动力学特性,具有抗肿瘤活性,可用于癌症研究。它选择性地抑制同源重组修复(HR) 缺陷细胞的增殖,并使 HR 缺陷细胞对细胞毒性药物敏感。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 525 | 现货 | ||
2 mg | ¥ 762 | 现货 | ||
5 mg | ¥ 1,230 | 现货 | ||
10 mg | ¥ 1,980 | 现货 | ||
25 mg | ¥ 3,550 | 现货 | ||
50 mg | ¥ 5,130 | 现货 | ||
100 mg | ¥ 7,270 | 现货 | ||
500 mg | ¥ 14,500 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 1,370 | 现货 |
产品描述 | Fluzoparib (SHR3162) is a novel, potent, and orally available inhibitor of PARP, potentially for the treatment of solid tumours. |
靶点活性 | PARP1:1.46±0.72 nM (IC50) |
体外活性 | Fluzoparib potently inhibited PARP1 enzyme activity and induced DNA double-strand breaks, G2 /M arrest, and apoptosis in homologous recombination repair (HR)-deficient cells.?Fluzoparib preferentially inhibited the proliferation of HR-deficient cells and sensitized both HR-deficient and HR-proficient cells to cytotoxic drugs.?Notably, fluzoparib showed good pharmacokinetic properties, favorable toxicity profile, and superior antitumor activity in HR-deficient xenografts models.?Furthermore, fluzoparib in combination with apatinib or with apatinib plus paclitaxel elicited significantly improved antitumor responses without extra toxicity. |
体内活性 | In vitro experiments in NSCLC cell lines along with in vivo experiments using an NSCLC xenograft mouse model demonstrated the radiosensitization effect of fluzoparib.?The underlying mechanisms involved increased apoptosis, cell-cycle arrest, enhanced irradiation-induced DNA damage, and delayed DNA-damage repair. |
别名 | HS10160, SHR3162, 氟唑帕利 |
分子量 | 472.4 |
分子式 | C22H16F4N6O2 |
CAS No. | 1358715-18-0 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 94 mg/mL (198.98 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.1169 mL | 10.5843 mL | 21.1685 mL | 52.9213 mL |
5 mM | 0.4234 mL | 2.1169 mL | 4.2337 mL | 10.5843 mL | |
10 mM | 0.2117 mL | 1.0584 mL | 2.1169 mL | 5.2921 mL | |
20 mM | 0.1058 mL | 0.5292 mL | 1.0584 mL | 2.6461 mL | |
50 mM | 0.0423 mL | 0.2117 mL | 0.4234 mL | 1.0584 mL | |
100 mM | 0.0212 mL | 0.1058 mL | 0.2117 mL | 0.5292 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。
Fluzoparib 1358715-18-0 Chromatin/Epigenetic DNA Damage/DNA Repair PARP homologous recombination repair Inhibitor poly ADP ribose polymerase inhibit ovarian SHR-3162 PARP1 HS 10160 HS-10160 HS10160 Fuzuloparib SHR3162 氟唑帕利 cancer SHR 3162 inhibitor