Flupentixol 是一种具有口服活性的D1/D2多巴胺受体拮抗剂和新型PI3K抑制剂 (PI3KαIC50=127 nM)。Flupentixol 具有对癌细胞的抗增殖活性并诱导细胞凋亡。Flupentixol 也可用于精神分裂症、焦虑和抑郁症的研究。
| 生物活性 | Flupentixol is an orally activeD1/D2dopamine receptorantagonist and newPI3Kinhibitor (PI3KαIC50=127 nM). Flupentixol shows anti-proliferative activity tocancercells and inducesapoptosis. Flupentixol can also be used in schizophrenia, anxiolytic and depressive research[1][2][3]. |
| IC50& Target[3] | D1Receptor | D2Receptor | PI3Kα 127 nM (IC50) |
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体外研究
(In Vitro) | Flupentixol (2.5-40 μM; 72 h) treatment inhibits the viability of lung cancer cells in a dose-dependent manner[3].
Flupentixol (2.5-40 μM; 24 h) induces apoptosis in lung cancer cells[3].
Flupentixol (2.5-15 μM; 24 h) inhibits p-AKT and Bcl-2 expression levels[3].
Cell Viability Assay[3] | Cell Line: | A549, H661, SK-SEM-1, and NCAL-H520 cells | | Concentration: | 2.5, 5, 10, 20, or 40 μM | | Incubation Time: | 72 hours | | Result: | Showed the IC50s of 5.708 μM and 6.374 μM for A549 and H661 cells, respectively. |
Apoptosis Analysis[3] | Cell Line: | A549 and H661 cells | | Concentration: | 5, 10, 20 and 40 μM | | Incubation Time: | 24 hours | | Result: | Increased the percentage of cells in early apoptosis compared with the negative control in both A549 and H661 (p< 0.05). Induced the cleavage of PARP and caspase-3 in a dose-dependent manner. |
Western Blot Analysis[3] | Cell Line: | H661 and A549 cells | | Concentration: | 2.5, 5, 10, and 15 μM | | Incubation Time: | 24 hours | | Result: | Decreased AKT phosphorylation levels in a dose-dependent manner, decreased the expression levels of Bcl-2. |
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体内研究
(In Vivo) | Flupentixol (intragastric injection; 40 mg/kg; once daily; 21 d) suppresses A549 xenografted tumor growth in nude mice[3].
| Animal Model: | BALB/C nude mice injected with A549 cells[3] | | Dosage: | 40 mg/kg | | Administration: | Intragastric injection; 40 mg/kg; once daily; 21 days | | Result: | Reduced tumor volumes compared to the vehicle control (p<0.05), reduced tumor weights by 64.1% (p<0.05). |
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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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