PI3K/AKT-IN-1

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PI3K/AKT-IN-1 

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)。

PI3K/AKT-IN-1

PI3K/AKT-IN-1 Chemical Structure

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生物活性

PI3K/AKT-IN-1 is an effective PI3K/AKT dual inhibitor (IC50 of 6.99, 4.01 and 3.36 μM for PI3Kγ, PI3Kδ and AKT, respectively). PI3K/AKT-IN-1 has anticancer activity and acts by inhibiting PI3K/AKT axis and inducing caspase 3 dependent apoptosis[1].

IC50 & Target[1]

PI3Kγ

6.99 μM (IC50)

PI3Kδ

4.01 μM (IC50)

Akt

3.36 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].

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

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].

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

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

467.54

Formula

C23H25N5O4S
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]. El-Dydamony NM, et al. Pyrimidine-5-carbonitrile based potential anticancer agents as apoptosis inducers through PI3K/AKT axis inhibition in leukaemia K562. J Enzyme Inhib Med Chem. 2022;37(1):895-911.

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