Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Lurbinectedin (PM01183) 是一种 DNA 小沟共价粘合剂,可抑制 RMG1和 RMG2,IC50值分别为1.25和1.16 nM。它具有高效的抗肿瘤活性。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 3,950 | 现货 | ||
5 mg | ¥ 8,150 | 现货 | ||
10 mg | ¥ 11,700 | 现货 | ||
25 mg | ¥ 17,200 | 现货 |
产品描述 | Lurbinectedin (PM01183) is a DNA minor groove covalent binder. Lurbinectedin also shows effective anti-tumor activity. |
靶点活性 | RMG2:1.16 nM, RMG1:1.25 nM |
体外活性 | Lurbinectedin inhibits RMG1 and RMG2 cell growth (IC50: 1.25 and 1.16 nM, respectively). Lurbinectedin exhibits significant antitumor activity toward chemosensitive and chemoresistant human ovarian clear cell carcinoma (CCC) cells in vitro[1]. Lurbinectedin-DNA adducts in living cells give rise to double-strand breaks, triggering S-phase accumulation, and apoptosis. Lurbinectedin is a new synthetic tetrahydroisoquinoline alkaloid that is currently in phase I clinical development for the treatment of solid tumors. The potent cytotoxic activity of Lurbinectedin is ascertained in a 23-cell line panel with a mean GI50 value of 2.7 nM[2]. |
体内活性 | Lurbinectedin inhibits tumor growth significantly with no weight loss of treated animals, in four murine xenograft models of human cancer[2]. Mouse CCC cell xenografts show that lurbinectedin significantly inhibits tumor growth. Lurbinectedin plus SN-38 causes a significant synergistic effect[1]. |
别名 | 卢比克替定, PM01183 |
分子量 | 784.87 |
分子式 | C41H44N4O10S |
CAS No. | 497871-47-3 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 15 mg/mL (19.11 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 1.2741 mL | 6.3705 mL | 12.741 mL | 31.8524 mL |
5 mM | 0.2548 mL | 1.2741 mL | 2.5482 mL | 6.3705 mL | |
10 mM | 0.1274 mL | 0.637 mL | 1.2741 mL | 3.1852 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。
Lurbinectedin 497871-47-3 Others DNA/RNA Synthesis inhibit 卢比克替定 PM-01183 DNA Alkylator/Crosslinker Inhibitor PM01183 PM 01183 inhibitor