产品描述: | Akt1/Akt2-IN-1 (Compound 17) is an allosteric inhibitor of Akt1 (IC50=3.5 nM) and Akt2 (IC50=42 nM), with potent and balanced activity |
靶点: |
Akt1:3.5 nM (IC50);Akt2:42 nM (IC50);Akt |
体内研究: |
Akt1/Akt2-IN-1 (Compound 17) is well tolerated in at exposures that provide high levels of Akt1 and 2 inhibition in vivo. Akt1/Akt2-IN-1 has also been shown to inhibit the growth of A2780 tumors in vivo when used as monotherapy. Akt1/Akt2-IN-1 has potent inhibitory activity against Akt1 and 2 in vivo in a mouse lung and efficacy in a tumor xenograft model. Akt1/Akt2-IN-1 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/Akt2-IN-1, tolerability and Akt inhibition are assessed in mice. Using an acute dosing schedule (IP dosing of 50 mg/kg at times 0, 3, and 8 h), administration of Akt1/Akt2-IN-1 is well tolerated in mice and shows high levels of Akt inhibition in mouse lung |
参考文献: |
1. Bilodeau MT, Allosteric inhibitors of Akt1 and Akt2: a naphthyridinone with efficacy in an A2780 tumor xenograft model. Bioorg Med Chem Lett. 2008 Jun 1;18(11):3178-82. |
溶解性: |
Soluble in DMSO |
保存条件: |
2-8℃ |
配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
1 mM |
1.853 ml |
9.265 ml |
18.531 ml |
5 mM |
0.371 ml |
1.853 ml |
3.706 ml |
10 mM |
0.185 ml |
0.927 ml |
1.853 ml |
50 mM |
0.037 ml |
0.185 ml |
0.371 ml |
|
注意: |
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