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) |
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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. |
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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). |
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| 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. |
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