PI3K/Akt/mTOR-IN-2

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PI3K/Akt/mTOR-IN-2 

PI3K/Akt/mTOR-IN-2 是一种有效的 PI3K/AKT/mTOR 抑制剂。PI3K/Akt/mTOR-IN-2 具有抗癌作用,并对 MDA-MB-231 细胞具有选择性,IC50 为 2.29 μM。PI3K/Akt/mTOR-IN-2 可诱导癌细胞周期阻滞和细胞凋亡 (apoptosis)。

PI3K/Akt/mTOR-IN-2

PI3K/Akt/mTOR-IN-2 Chemical Structure

CAS No. : 2757804-89-8

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生物活性

PI3K/Akt/mTOR-IN-2 is a PI3K/AKT/mTOR pathway inhibitor. PI3K/Akt/mTOR-IN-2 possess anti-cancer effects and selectivity against MDA-MB-231 cells with IC50 value of 2.29 μM. PI3K/Akt/mTOR-IN-2 can induce cancer cell cycle arrest and apoptosis[1].

IC50 & Target

IC50: 2.29 μM (PI3K/AKT/mTOR) in MDA-MB-231[1]

体外研究
(In Vitro)

PI3K/Akt/mTOR-IN-2 (compound 23) (0.5 – 100 μM; 72 hours) exhibits effective anti-cancer activity with IC50s of 2.29 – 24.63 μM, of which, IC50 in MDA-MB-231 is 2.29 μM[1].
PI3K/Akt/mTOR-IN-2 (1 μM, 2 μM and 4 μM; 24 hours) induces growth inhibition of MDA-MB-231 cells by cell cycle arrest at G0/G1[1].
PI3K/Akt/mTOR-IN-2 (1 μM, 2 μM and 4 μM; 24, 48 and 72 hours) induces apoptosis in MDA-MB-231 cells with both dose- and time-dependent manners[1].
PI3K/Akt/mTOR-IN-2 (1 μM, 2 μM and 4 μM; 48 hours) increases the expression of Bax, and decreases the expression of Bcl-2 in MDA-MB-231 cells[1].
PI3K/Akt/mTOR-IN-2 (1 μM, 2 μM and 4 μM; 24 hours) induces mitochondria-dependent apoptosis in MDA-MB-231 cells through disruption of MMP, accumulation of ROS, depletion of GSH and elevation of intracellular Ca2+[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay

Cell Line: PC3, BGC-823, A549, MCF-7, MDA-MB-231 cells and MCF-10A cells[1]
Concentration: 0.5 – 100 μM
Incubation Time: 72 hours
Result: Exhibited effective anti-cancer activity with IC50s of 2.29 – 24.63 μM, of which, IC50 in MDA-MB-231 was 2.29 μM.

Cell Cycle Analysis

Cell Line: MDA-MB-231[1]
Concentration: 1 μM, 2 μM and 4 μM
Incubation Time: 24 hours
Result: Induced growth inhibition of MDA-MB-231 cells by cell cycle arrest at G0/G1.

Apoptosis Analysis

Cell Line: MDA-MB-231[1]
Concentration: 1 μM, 2 μM and 4 μM
Incubation Time: 24, 48 and 72 hours
Result: Induced apoptosis in MDA-MB-231 cells with both dose- and time-dependent manners.

Western Blot Analysis

Cell Line: MDA-MB-231[1]
Concentration: 1 μM, 2 μM and 4 μM
Incubation Time: 48 hours
Result: Increased the expression of Bax, and decreased the expression of Bcl-2

分子量

285.29

Formula

C17H13F2NO

CAS 号

2757804-89-8

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.

参考文献
  • [1]. Qin J, Sun X, Ma Y, et al. Design, synthesis and biological evaluation of novel 1,3,4,9-tetrahydropyrano[3,4-b]indoles as potential treatment of triple negative breast cancer by suppressing PI3K/AKT/mTOR pathway [published online ahead of print, 2021 Dec 31]. Bioorg Med Chem. 2021;55:116594.

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