Flupentixol dihydrochloride 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 dihydrochloride 具有对癌细胞的抗增殖活性并诱导细胞凋亡。Flupentixol dihydrochloride 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] | PI3Kα 127 nM (IC50) | D1Receptor | D2Receptor |
|
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: | A549 and H661 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. |
|
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). |
|
| Clinical Trial | |
| 分子量 | |
| 性状 | |
| Formula | |
| CAS 号 | |
| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | 4°C, sealed storage, away from moisture and light *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light) |
| 溶解性数据 | In Vitro: H2O : 100 mg/mL(197.07 mM;Need ultrasonic) DMSO : 33.33 mg/mL(65.68 mM;Need ultrasonic) 配制储备液 | 1 mM | 1.9707 mL | 9.8534 mL | 19.7068 mL | | 5 mM | 0.3941 mL | 1.9707 mL | 3.9414 mL | | 10 mM | 0.1971 mL | 0.9853 mL | 1.9707 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month (sealed storage, away from moisture and light)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂： ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂： PBS Solubility: 50 mg/mL (98.53 mM); Clear solution; Need ultrasonic 2. 请依序添加每种溶剂： 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.5 mg/mL (4.93 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (4.93 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。 3. 请依序添加每种溶剂： 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 2.5 mg/mL (4.93 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (4.93 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。 4. 请依序添加每种溶剂： 10% DMSO 90%corn oil Solubility: ≥ 2.5 mg/mL (4.93 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (4.93 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。 *以上所有助溶剂都可在本网站选购。
|
m.cnreagent.com