计算溶液所需的质量、体积或浓度。
概述
Akt1/Akt2-IN-1 (Compound 17) is an allosteric inhibitor of Akt1 ( IC 50 =3.5 nM) and Akt2 (IC 50 =42 nM), with potent and balanced activity
In Vitro
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 (IC 50 =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 (IC 50 =5610 nM) and is a substrate for human P-glycoprotein. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
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 . MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Form:Solid
IC50& Target:Akt1 3.5 nM (IC 50 ) Akt2 42 nM (IC 50 )
规格
规格或纯度
≥99%
英文名称
Akt1/Akt2-IN-1
生化机理
Akt1/Akt2-IN-1 （化合物 17）是 Akt1（IC 50 =3.5 nM）和 Akt2（IC 50 =42 nM）的异位抑制剂，具有强效且均衡的活性。
储存条件
-20°C储存
运输条件
超低温运输
作用类型
抑制剂
纯度
≥99%
名称和识别符
分子类型
小分子
分子量
539.63
高级数据
化学和物理性质
溶解性
DMSO : ≥ 35 mg/mL (64.86 mM)
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溶液计算器
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