Akt1 and Akt2-IN-1 ≥98%
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| 包装规格: | 5mg 10mg 50mg 100mg in glass bottle |
| 产品简介: | 一种有效的变构抑制剂, 抑制 Akt1 (IC50=3.5nM)和Akt2 (IC50=42nM)。 |
| 溶解性: | 溶于DMSO(≥35mg/mL) |
| 储备液保存: | -80°C, 2 years -20°C, 1 year |
| 靶点: | Akt1:3.5 nM (IC50);Akt2:42 nM (IC50) |
| 体外研究: | Consistent with the allosteric mode of inhibition, Akt1/Akt2-IN-1 (Compound 17) is dependent on the PH-domain for Akt inhibition, 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). Akt1/Akt2-IN-1 has moderate activity in an hERG binding assay (IC50=5610 nM) and is a substrate for human P-glycoprotein. |
| 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. |
| 保存条件: | -20℃ |
| 注意事项: | 1、为了您的安全和健康,请穿实验服并戴一次性手套操作。 2、以上信息仅做参考交流之用。 |
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