Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Ribociclib succinate (LEE011 succinate) 是一种高度特异性的CDK4/6抑制剂,IC50值分别为 10 nM 和 39 nM。它对细胞周期蛋白 B/CDK1 复合物的效力低 1000 倍。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
2 mg | ¥ 397 | 现货 | ||
5 mg | ¥ 495 | 现货 | ||
10 mg | ¥ 693 | 现货 | ||
25 mg | ¥ 983 | 现货 | ||
50 mg | ¥ 1,190 | 现货 | ||
100 mg | ¥ 1,790 | 现货 | ||
200 mg | ¥ 2,660 | 现货 | ||
500 mg | ¥ 4,290 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 592 | 现货 |
产品描述 | Ribociclib succinate (LEE011 succinate) is a highly specific CDK4/6 inhibitor (IC50: 10 nM and 39 nM, respectively). It also is over 1,000-fold less potent against the cyclin B/CDK1 complex. |
靶点活性 | CDK4:10 nM, CDK6:39 nM |
体外活性 | Ribociclib succinate treatment of two neuroblastoma cell lines (BE2C and IMR5) with demonstrated sensitivity to CDK4/6 inhibition causes a dose-dependent accumulation of cells in the G0/G1 phase of the cell cycle. This G0/G1 arrest becomes significant at Ribociclib concentrations of 100 nM (p=0.007) and 250 nM (p=0.01), respectively. Treatment with Ribociclib obviously inhibits substrate adherent growth relative to the control in 12 of the 17 neuroblastoma cell lines examined (mean IC50=306±68 nM, considering sensitive lines only, where sensitivity is defined as an IC50 of less than 1 μM. Treating a panel of 17 neuroblastoma cell lines with Ribociclib across a four-log dose range (10 to 10,000 nM) [2]. |
体内活性 | Tumor growth is obviously delayed throughout the 21 days of treatment in mice harboring the BE2C or 1643 xenografts (both, p<0.0001), although growth resumed post-treatment. CB17 immunodeficient mice bearing BE2C, NB-1643 (MYCN amplified, sensitive in vitro), or EBC1 (non-amplified, resistant in vitro) xenografts are treated once daily for 21 days with Ribociclib (LEE011; 200 mg/kg) or with vehicle control. This dosing strategy is well tolerated, as no weight loss or other signs of toxicity are observed in any of the xenograft models [2]. |
别名 | LEE011 琥珀酸盐, 瑞博西尼琥珀酸盐, LEE011 succinate |
分子量 | 552.63 |
分子式 | C27H36N8O5 |
CAS No. | 1374639-75-4 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 41 mg/mL (74.19 mM), sonification is recommended.
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 1.8095 mL | 9.0476 mL | 18.0953 mL | 45.2382 mL |
5 mM | 0.3619 mL | 1.8095 mL | 3.6191 mL | 9.0476 mL | |
10 mM | 0.181 mL | 0.9048 mL | 1.8095 mL | 4.5238 mL | |
20 mM | 0.0905 mL | 0.4524 mL | 0.9048 mL | 2.2619 mL | |
50 mM | 0.0362 mL | 0.181 mL | 0.3619 mL | 0.9048 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。
Ribociclib succinate 1374639-75-4 Cell Cycle/Checkpoint CDK LEE 011 Ribociclib inhibit LEE011 LEE-011 Succinate LEE-011 Ribociclib Succinate LEE011 琥珀酸盐 LEE 011 Succinate Inhibitor LEE011 Succinate Cyclin dependent kinase 瑞博西尼琥珀酸盐 LEE011 succinate inhibitor