Thioridazine hydrochloride 是一种具有口服活性的多巴胺受体D2家族蛋白的拮抗剂,具有有效的的抗焦虑活性。Thioridazine hydrochloride 也是一种有效的PI3K-Akt-mTOR信号通路的抑制剂,具有抗血管生成作用。Thioridazine hydrochloride 在多种类型的癌细胞中显示出抗增殖和凋亡诱导作用,对靶向癌症干细胞 (CSCs) 具有特异性。
生物活性 | Thioridazine hydrochloride, an orally active antagonist of thedopamine receptorD2family proteins, exhibits potent anti-psychotic and anti-anxiety activities. Thioridazine hydrochloride is also a potent inhibitor ofPI3K-Akt-mTORsignaling pathways with anti-angiogenic effect. Thioridazine hydrochloride shows antiproliferative andapoptosisinduction effects in various types ofcancercells, with specificity on targetingcancer stem cells(CSCs)[1][2][3][4]. |
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体外研究 (In Vitro) | Thioridazine (0.01-100 μM; 48 h) reduces the cell viability of NCI-N87 and AGS cells in a concentration-dependent manner[2]. Thioridazine (15 μM; 24 h) reduces cell viability of the cervical (HeLa, Caski and C33A) and endometrial (HEC-1-A and KLE) cancer cells[4]. Thioridazine (1-15 μM; 24-48 h) induces gastric cancer cell death via the mitochondrial apoptosis pathway and mitochondrial pathway[2]. Thioridazine (15 μM; 24 h) modulates the regulation of cell cycle progression by interfering with the PI3K/Akt pathway and induces G1cell cycle arrest in cervical and endometrial cancer cells[4]. Thioridazine inhibits the growth of antibiotic-sensitive and multidrug-resistant strains ofA. baumannii[3].
Cell Proliferation Assay[1] Cell Line: | NCI-N87 and AGS cells | Concentration: | 0.01, 0.1, 0.5, 1, 5, 10, 20, 50, 100 μM | Incubation Time: | 48 hours | Result: | Exhibited cytotoxicity in gastric cancer cells. |
Western Blot Analysis[1] Cell Line: | NCI-N87 and AGS cells | Concentration: | 1, 5, 10, 15 μM | Incubation Time: | 24, 48 hours | Result: | Downregulated the precursors of caspase-9, caspase-8 and caspase-3. |
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体内研究 (In Vivo) | Thioridazine (25 mg/kg; i.p. every 3 days for 3 weeks) extends the survival of tumor-bearing mice and reduces the number of pluripotent embryonal carcinoma (EC) cells within tumors[5]. Thioridazine (1.0-5.0 mg/kg; s.c.) reduces oral behavior and selectively blocks repetitive head bobbing[1].
Animal Model: | Nude and Rag2KO mice were injected with iPS cells or NT2D1 cells[5] | Dosage: | 25 mg/kg | Administration: | I.p. every 3 days for 3 weeks | Result: | Reduced the number of OCT4-expressing cells within malignant teratocarcinomas and extended the survival of tumor-bearing mice. With no effect on fertility. |
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中文名称 | 盐酸硫利达嗪;盐酸硫代利哒;甲硫达嗪盐酸盐;甲硫哒嗪盐酸盐 |
运输条件 | Room temperature in continental US; may vary elsewhere. |
储存方式 | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
溶解性数据 | In Vitro: H2O : 100 mg/mL(245.68 mM;Need ultrasonic) DMSO : ≥ 45 mg/mL(110.55 mM) *"≥" means soluble, but saturation unknown. 配制储备液 1 mM | 2.4568 mL | 12.2838 mL | 24.5676 mL | 5 mM | 0.4914 mL | 2.4568 mL | 4.9135 mL | 10 mM | 0.2457 mL | 1.2284 mL | 2.4568 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)。-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: 12.5 mg/mL (30.71 mM); Clear solution; Need ultrasonic and warming and heat to 60℃ 2. 请依序添加每种溶剂: 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.08 mg/mL (5.11 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (5.11 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 20.8 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: ≥ 2.08 mg/mL (5.11 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (5.11 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 20.8 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: ≥ 2.08 mg/mL (5.11 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (5.11 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 20.8 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。
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