Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Akt1 and Akt2-IN-1 is an allosteric inhibitor of Akt1 (IC50=3.5 nM) and Akt2 (IC50=42 nM). It has potent and balanced activity.
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
2 mg | ¥ 1,950 | 5日内发货 | ||
5 mg | ¥ 2,890 | 5日内发货 | ||
25 mg | ¥ 9,620 | 6-8周 | ||
50 mg | ¥ 12,500 | 6-8周 | ||
100 mg | ¥ 17,500 | 6-8周 | ||
1 mL * 10 mM (in DMSO) | ¥ 3,450 | 5日内发货 |
产品描述 | Akt1 and Akt2-IN-1 is an allosteric inhibitor of Akt1 (IC50=3.5 nM) and Akt2 (IC50=42 nM). It has potent and balanced activity. |
靶点活性 | Akt2:42 nM, Akt1:3.5 nM |
体外活性 | Akt1 and Akt2-IN-1 (Compound 17) has moderate activity in an hERG binding assay (IC50=5610 nM) and is a substrate for human P-glycoprotein[1]. Consistent with the allosteric mode of inhibition, Akt1 and Akt2-IN-1 (Compound 17) is dependent on the PH-domain for Akt inhibition. Akt1 and Akt2-IN-1 (Compound 17) is selective for Akt1/2 over Akt3 (IC50=1900 nM), and is highly selective over other members of the AGC family of kinases (>50 μM vs PKA, PKC, SGK). |
体内活性 | Akt1 and Akt2-IN-1 (Compound 17) is well tolerated in at exposures that provide high levels of Akt1 and 2 inhibition in vivo. Akt1 and Akt2-IN-1 (Compound 17) shows good pharmacokinetics in rat with a low clearance of 4.6 mL/min/kg and a half-life of 3.8 h. Due to the improved cell potency, physical properties, and rodent pharmacokinetics of Akt1 and Akt2-IN-1 (Compound 17), tolerability and Akt inhibition are assessed in mice. Akt1 and Akt2-IN-1 (Compound 17) has also been shown to inhibit the growth of A2780 tumors in vivo when used as monotherapy and has potent inhibitory activity against Akt1 and 2 in vivo in a mouse lung and efficacy in a tumor xenograft model. Using an acute dosing schedule (IP dosing of 50 mg/kg at times 0, 3, and 8 h), administration of Akt1 and Akt2-IN-1 (Compound 17) is well tolerated in mice and shows high levels of Akt inhibition in mouse lung[1]. |
分子量 | 539.63 |
分子式 | C33H29N7O |
CAS No. | 893422-47-4 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 35 mg/mL (64.86 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 1.8531 mL | 9.2656 mL | 18.5312 mL | 46.328 mL |
5 mM | 0.3706 mL | 1.8531 mL | 3.7062 mL | 9.2656 mL | |
10 mM | 0.1853 mL | 0.9266 mL | 1.8531 mL | 4.6328 mL | |
20 mM | 0.0927 mL | 0.4633 mL | 0.9266 mL | 2.3164 mL | |
50 mM | 0.0371 mL | 0.1853 mL | 0.3706 mL | 0.9266 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。
Akt1 and Akt2-IN-1 893422-47-4 Cytoskeletal Signaling PI3K/Akt/mTOR signaling Akt Akt-1 and Akt2-IN-1 Akt1 and Akt2IN1 Akt1 and Akt2 IN 1 Inhibitor inhibitor inhibit