产品说明书

Afuresertib

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Chemical Structure| 1047644-62-1 同义名 : GSK2110183;LAE002
CAS号 : 1047644-62-1
货号 : A136023
分子式 : C18H17Cl2FN4OS
纯度 : 99%+
分子量 : 427.323
MDL号 : MFCD26961098
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: 105 mg/mL(245.72 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, Ki:2.6 nM

  • Akt1

    Akt1, Ki:0.08 nM

  • Akt2

    Akt2, Ki:2 nM
描述 AKT is the central node of PI3K/AKT/mTOR pathway. The PH domain and ATP-competitive site are the main target site for research of new compound[2]. Afuresertib （GSK2110183） is an ATP-competitive inhibitor of AKT1/2/3 with Ki value of 0.08nM, 2nM and 2.6nM (measured by a filter binding assay), respectively. Treatment of Afuresertib on concentration of 1-10uM can induce G1-arrest and decrease the phosphorylation level of multiple AKT substrate including PRAS40, FOXO and Caspase 9 in BT474 and LNCaP cell lines in a concentration-dependent manner, accompanied by feedback increase in AKT phosphorylation. Afuresertib has more potent anti-proliferative effects on a variety of hematological malignancies (65% were sensitive to Afuresertib with EC50<1uM)). Among solid tumor cell lines, 21% had EC50<1uM in response to Afuresertib. Treatment with Afuresertib at 10, 30 and 100mg/kg, daily for 7 days, can decrease PRAS40 phosphorylation by 8%, 37% and 61% in mice bearing BT474 tumors, which showed the good pharmacodynamics of Afuresertib[1]. Single-agent Afuresertib shows clinical activity against hematologic malignancies, including multiple myeloma[3].
作用机制 Afuresertib is an ATP-competitive AKT inhibitor.[1]
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.34mL

0.47mL

0.23mL

11.70mL

2.34mL

1.17mL

23.40mL

4.68mL

2.34mL