产品
编 号:F762800
分子式:C23H23N5O4S
分子量:465.52
产品类型
结构图
CAS No: 3033069-84-7
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产品详情
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.
体内研究:
PI3K/AKT-IN-1 (2000 mg/kg; p.o.; single) is non-toxic and is well tolerated by experimental animals.Animal Model:Female rats (180-200g)
Dosage:2000 mg/kg
Administration:p.o.; single
Result:The median lethal dose (LD50) was greater than the test dose (2000?mg/kg).
体外研究:
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).PI3K/AKT-IN-1 (2.62 μM) can promote S-phase cell cycle arrest and apoptosis induction in K562 cells.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.PI3K/AKT-IN-1 (2.62 μM; 48 hours) markedly reduces the expression of PI3K, AKT, Cyclin D1 and NF-κB.