Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Roniciclib (BAY 1000394) 是一种有效的泛 CDK 抑制剂和新型口服细胞毒剂,对 CDK1、CDK2、CDK3、CDK4、CDK7 和 CDK9 的 IC50值为 5-25 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
2 mg | ¥ 2,350 | 5日内发货 | ||
5 mg | ¥ 3,150 | 5日内发货 | ||
1 mL * 10 mM (in DMSO) | ¥ 3,780 | 5日内发货 |
产品描述 | Roniciclib (BAY 1000394) is a potent pan-CDK inhibitor and a novel oral cytotoxic agent. Roniciclib inhibits the activity of cell-cycle CDKs CDK1, CDK2, CDK3, CDK4, and of transcriptional CDKs CDK7 and CDK9 with IC(50) values in the range between 5 and 25 nmol/L. |
靶点活性 | CDK2-CyclinE:9 nM, CDK4-CyclinD:11 nM, CDK9-CyclinT1:5 nM, CDK1-CyclinB:7 nM, CDK7-CyclinH-MAT1:25 nM |
体外活性 | Roniciclib inhibits the kinase activity of the cell-cycle CDKs CDK1/cyclin B, CDK2/cyclin E, and CDK4/cyclinD (IC50: 7, 9, and 11 nM, respectively). Roniciclibeffectively inhibits the proliferation of various human and murine tumor cell lines with a very balanced profile (mean IC50 on human tumor cells: 16 nM). The transcriptional CDKs CDK9/cyclin T1 and CDK7/cyclin H/MAT1 are inhibited in a similar range (5 and 25 nM) [1][2]. |
体内活性 | Roniciclib has low blood clearance rates in mouse, rat, and dog (0.51, 0.78, and 0.50 Lh-1kg-1, respectively). Roniciclib strongly inhibits the growth of HeLa-MaTu tumors that have been grown to a size of approximately 50mm2 before the start of treatment. Roniciclib (1.5 and 1 mg/kg) treatment slow tumor growth to T/C values of 0.15 and 0.62, respectively. The addition of Roniciclib to cisplatin causes a strong tumor growth inhibition with T/C values of 0.01 (1.0 mg/kg Roniciclib) and -0.02 (1.5 mg/kg Roniciclib) [1][2]. |
别名 | BAY 1000394 |
分子量 | 430.44 |
分子式 | C18H21F3N4O3S |
CAS No. | 1223498-69-8 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 249 mg/mL (578.47 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.3232 mL | 11.616 mL | 23.232 mL | 58.0801 mL |
5 mM | 0.4646 mL | 2.3232 mL | 4.6464 mL | 11.616 mL | |
10 mM | 0.2323 mL | 1.1616 mL | 2.3232 mL | 5.808 mL | |
20 mM | 0.1162 mL | 0.5808 mL | 1.1616 mL | 2.904 mL | |
50 mM | 0.0465 mL | 0.2323 mL | 0.4646 mL | 1.1616 mL | |
100 mM | 0.0232 mL | 0.1162 mL | 0.2323 mL | 0.5808 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。
Roniciclib 1223498-69-8 Cell Cycle/Checkpoint CDK BAY 1000394 Cyclin dependent kinase BAY1000394 BAY-1000394 inhibit Inhibitor inhibitor