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  • Akt1 and Akt2-IN-1
Akt1 and Akt2-IN-1的可视化放大

Akt1 and Akt2-IN-1

Akt1andAkt2-IN-1是一种有效的变构抑制剂,抑制Akt1(IC50=3.5nM)和Akt2(IC50=42nM)。

原价
¥3737-22250
价格
2990-17800
Akt1 and Akt2-IN-1的二维码

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  • 库存: 现货
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  • 货号: ajce50120
  • CAS: 893422-47-4
  • 别名: 3-苯基-2-[4-[[4-[5-(2-吡啶)-1H-1,2,4-三唑-3-基]-1-哌啶]甲基]苯基]-1,6-萘啶-5(6H)-酮
  • 分子式: C33H29N7O
  • 分子量: 539.63
  • 纯度: >98%
  • 溶解度: DMSO : ≥ 35 mg/mL (64.86 mM)
  • 储存: Store at -20°C
  • 库存: 现货

Background

Akt1 and Akt2-IN-1 is an allosteric inhibitor of Akt1 (IC50=3.5 nM) and Akt2 (IC50=42 nM), with potent and balanced activity.


Consistent with the allosteric mode of inhibition, Akt1 and 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 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].


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) has also been shown to inhibit the growth of A2780 tumors in vivo when used as monotherapy. Akt1 and Akt2-IN-1 (Compound 17) has potent inhibitory activity against Akt1 and 2 in vivo in a mouse lung and efficacy in a tumor xenograft model. 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. 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].


[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.

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