Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Atuveciclib (BAY-1143572) 是一种有效且高度选择性的口服 PTEFb/CDK9抑制剂。Atuveciclib (BAY-1143572) 抑制 CDK9/CycT1,IC50为 13 nM。
产品描述 | Atuveciclib (BAY-1143572) is a potent and highly selective, oral PTEFb / CDK9 inhibitor that inhibits CDK9 / CycT1 with an IC 50 of 13 nM [1]. |
靶点活性 | CDK5-p35:1600 nM, CDK9-CyclinT1:13 nM, CDK9-CyclinT1:6 nM, CDK1-CyclinB:1100 nM, CDK2-CyclinE:1000 nM, CDK3-CyclinE:890 nM |
体外活性 | Positive transcription elongation factor b (PTEFb) is a heterodimer of CDK9 and one of four cyclin partners, cyclin T1, cyclin K, cyclin T2a or cyclin T2b. Atuveciclib (BAY-1143572) shows potent antiproliferative activity against HeLa cells (IC 50 =920 nM) and MOLM-13 cells (IC 50 =310 nM) [1]. |
体内活性 | In vivo efficacy studies in the MOLM-13 xenograft model in mice, Atuveciclib (BAY-1143572) exhibits great potency and high antitumor efficacy. Daily administration of Atuveciclib (BAY-1143572) at 6.25 or 12.5 mg/kg results in a dose-dependent antitumor efficacy with a treatment-to-control (T/C) ratio of 0.64 and 0.49, respectively (p<0.001). In a separate experiment with a higher daily dose of 20 or 25 mg/kg Atuveciclib (BAY-1143572), antitumor efficacy with a T/C ratio of 0.41 and 0.31, respectively, is observed (p<0.001). The 25 mg/kg once daily dose is the maximum tolerated dose in nude mice. Furthermore, Atuveciclib (BAY-1143572) administered at 25 or 35 mg/kg, three days on / two days off, results in a T/C ratio of 0.33 and 0.20, respectively (p<0.001). Treatment with Atuveciclib (BAY-1143572) is well-tolerated, as demonstrated by less than 10 % mean body weight reduction throughout the study. In an in vivo pharmacokinetic study in rats, Atuveciclib (BAY-1143572) shows low blood clearance (CL b 1.1 L/kg per hour) [1]. |
别名 | BAY-1143572 |
分子量 | 387.43 |
分子式 | C18H18FN5O2S |
CAS No. | 2923012-24-0 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 128.5 mg/mL (331.67 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.5811 mL | 12.9056 mL | 25.8111 mL | 64.5278 mL |
5 mM | 0.5162 mL | 2.5811 mL | 5.1622 mL | 12.9056 mL | |
10 mM | 0.2581 mL | 1.2906 mL | 2.5811 mL | 6.4528 mL | |
20 mM | 0.1291 mL | 0.6453 mL | 1.2906 mL | 3.2264 mL | |
50 mM | 0.0516 mL | 0.2581 mL | 0.5162 mL | 1.2906 mL | |
100 mM | 0.0258 mL | 0.1291 mL | 0.2581 mL | 0.6453 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。
Atuveciclib 2923012-24-0 Cell Cycle/Checkpoint CDK BAY1143572 BAY-1143572 BAY 1143572 Inhibitor inhibitor inhibit