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Chemical Structure| 1313881-70-7 同义名 : ARQ-092
CAS号 : 1313881-70-7
货号 : A918378
分子式 : C27H24N6
纯度 : 98+%
分子量 : 432.52
MDL号 : MFCD30187510
存储条件：

粉末 Keep in dark place,Inert atmosphere,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 12 mg/mL(27.74 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
靶点

  • Akt3

    Akt3, IC50:16 nM

  • Akt1

    Akt1, IC50:5 nM

  • Akt2

    Akt2, IC50:4.5 nM
描述 ARQ-092 is an orally bioavailable, selective, and potent allosteric Akt inhibitor with IC50 of 2.7 nM, 14 nM and 8.1 nM for Akt1, Akt2, Akt3, respectively.
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.31mL

0.46mL

0.23mL

11.56mL

2.31mL

1.16mL

23.12mL

4.62mL

2.31mL
参考文献

[1]Wang J, Chandrasekhar V, et al. In vivo efficacy of the AKT inhibitor ARQ 092 in Noonan Syndrome with multiple lentigines-associated hypertrophic cardiomyopathy. PLoS One. 2017 Jun 5;12(6):e0178905.

[2]Lapierre JM, Eathiraj S, et al. Discovery of 3-(3-(4-(1-Aminocyclobutyl)phenyl)-5-phenyl-3H-imidazo[4,5-b] pyridin-2-yl)pyridin-2-amine (ARQ 092): An Orally Bioavailable, Selective, and Potent Allosteric AKT Inhibitor. J Med Chem. 2016 Jul 14;59(13):6455-69.