您好,欢迎来到试剂仪器网! [登录] [免费注册]
试剂仪器网
位置:首页 > 产品库 > PI3K/AKT-IN-1
立即咨询
咨询类型:
     
*姓名:
*电话:
*单位:
Email:
*留言内容:
请详细说明您的需求。
*验证码:
 
PI3K/AKT-IN-1
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
PI3K/AKT-IN-1图片
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议

产品介绍
PI3K/AKT-IN-1 是一种有效的PI3K/AKT双重抑制剂 (PI3Kγ、PI3Kδ 和 AKT 的IC50分别为 6.99 μM、4.01 μM 和 3.36 μM)。PI3K/AKT-IN-1 具有抗癌活性,其作用机制是抑制PI3K/AKT通路,诱导 caspase 3 依赖性凋亡 (apoptosis)。
生物活性

PI3K/AKT-IN-1 is an effectivePI3K/AKTdual inhibitor (IC50of 6.99, 4.01 and 3.36 μM forPI3Kγ,PI3KδandAKT, respectively). PI3K/AKT-IN-1 has anticancer activity and acts by inhibiting PI3K/AKT axis and inducingcaspase 3dependentapoptosis[1].

IC50& Target[1]

PI3Kγ

6.99 μM (IC50)

PI3Kδ

4.01 μM (IC50)

体外研究
(In Vitro)

PI3K/AKT-IN-1 (compound 7f) (0.04-100 μM; 48 hours) has high cytotoxic activity on both cell lines with better activity on leukaemia cell line (K562 IC50=2.62 μM) than on the breast cancer cell line (MCF-7 IC50=3.22 μM)[1].
PI3K/AKT-IN-1 (2.62 μM) can promote S-phase cell cycle arrest and apoptosis induction in K562 cells[1].
PI3K/AKT-IN-1 (2.62 μM; 48 hours) causes an increase in the percentage of Annexin-V positive apoptotic cells both in the early and late stage[1].
PI3K/AKT-IN-1 (2.62 μM; 48 hours) markedly reduces the expression of PI3K, AKT, Cyclin D1 and NF-κB[1].

Cell Cytotoxicity Assay

Cell Line:MCF-7 and K562 cells[1]
Concentration:0.04-100 μM
Incubation Time:48 hours
Result:Demonstrated high cytotoxic activity on both cell lines with better activity on leukaemia cell line (K562 IC50=2.62 μM) than on the breast cancer cell line (MCF-7 IC50=3.22 μM).

Cell Cycle Analysis

Cell Line:K562 cells[1]
Concentration:2.62 μM
Incubation Time:
Result:Promoted S-phase cell cycle arrest and apoptosis induction.

Apoptosis Analysis

Cell Line:K562 cells[1]
Concentration:2.62 μM
Incubation Time:48 hours
Result:Caused an increase in the percentage of Annexin-V positive apoptotic cells both in the early and late stage.

Western Blot Analysis

Cell Line:K562 cells[1]
Concentration:2.62 μM
Incubation Time:48 hours
Result:Markedly reduced the expression of PI3K, p-PI3K, AKT, p-AKT, Cyclin D1 and NF-κB.
体内研究
(In Vivo)

PI3K/AKT-IN-1 (2000 mg/kg; p.o.; single) is non-toxic and is well tolerated by experimental animals[1].

Animal Model:Female rats (180-200g)[1]
Dosage:2000 mg/kg
Administration:p.o.; single
Result:The median lethal dose (LD50) was greater than the test dose (2000 mg/kg).
分子量

465.52

Formula

C23H23N5O4S

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.