Trifluoperazine
(Synonyms: 三氟拉嗪) 目录号 : GC63240
Trifluoperazine (TFP)是一种多巴胺受体拮抗剂，具有抗精神病作用，广泛用于治疗精神分裂症或相关精神病。
Cas No.:117-89-5
Sample solution is provided at 25 µL, 10mM.
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Trifluoperazine (TFP) is an antagonist against dopamine receptors, act as antipsychotic agent and is widely used to treat schizophrenia or related psychoses [1,2]. Trifluoperazine is also a well-known calmodulin antagonist [3].
Trifluoperazine significantly restricted the invasion of glioblastoma cells at a concentration higher than 1 µmol/L, with a half-maximal effective concentration at around 10 µmol/L on invasion of U87MG cells by performing Matrigel transwell invasion assay. The ratio of proliferated glioblastoma cells was significantly decreased in TFP-treated cells [4]. Trifluoperazine inhibits cell vitality, proliferation, and induces cell apoptosis of HCT116 cells with IC50 =14 µM [3]. Trifluoperazine (30 µM, 24h) induced pancreatic adenocarcinoma (PDAC) MiaPaCa-2 cell death and decreased in intracellular availability of ATP [5].
Trifluoperazine (5 mg/kg/day) significantly suppressed the glioblastoma growth of the xenograft mice as evidenced by a marked decrease of glioblastoma tumor size in TFP-treated mice at day 21, there was no lung metastasis in TFP-treated group in the skin xenograft model [4]. Administration of TFP induced remarkably tumor regression with decreased tumor volume in the xenograft model of human HCT116 [3]. Trifluoperazine binds and mimics the effect of the genetic inhibition of NUPR1, a stress protein that promotes tumor growth and acts as a strong anticancer drug in vitro and in vivo in xenografted nude mice [6].
References:
[1]. de Oliveira Marques L, Soares B, de Lima M S. Trifluoperazine for schizophrenia[J]. Cochrane Database of Systematic Reviews, 2004 (1).
[2]. Hong M, Jenner P, Marsden C D. Comparison of the acute actions of amine-depleting drugs and dopamine receptor antagonists on dopamine function in the brain in rats[J]. Neuropharmacology, 1987, 26(2-3): 237-245.
[3]. Qian K, Sun L, Zhou G, et al. Trifluoperazine as an alternative strategy for the inhibition of tumor growth of colorectal cancer[J]. Journal of cellular biochemistry, 2019, 120(9): 15756-15765.
[4]. Kang S, Hong J, Lee J M, et al. Trifluoperazine, a well-known antipsychotic, inhibits glioblastoma invasion by binding to calmodulin and disinhibiting calcium release channel IP3R[J]. Molecular cancer therapeutics, 2017, 16(1): 217-227.
[5]. Huang C, Lan W, Fraunhoffer N, et al. Dissecting the anticancer mechanism of trifluoperazine on pancreatic ductal adenocarcinoma[J]. Cancers, 2019, 11(12): 1869.
[6]. Neira J L, Bintz J, Arruebo M, et al. Identification of a drug targeting an intrinsically disordered protein involved in pancreatic adenocarcinoma[J]. Scientific reports, 2017, 7(1): 1-15.
| Cell experiment [1]: | |
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Cell lines |
U87MG human glioblastoma cells |
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Preparation Method |
Cells were seeded into 96-well plates at a density of 1.5 × 103 cells per well and allowed to attach for 24 hours. Cells were treated with vehicle or the indicated concentrations of Trifluoperazine diluted in complete media for each 24, 48, and 72 hours. Cell proliferation was determined by 3-[4, 5-dimethylthiazol-2-yl]-2, 5-diphenyltetrazolium bromide (MTT) assay. |
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Reaction Conditions |
0-20µM for 24, 48, and 72 hours |
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Applications |
U87MG cell viability decreased time dependently (24, 48, and 72-hour Trifluoperazine treatment) as well as dose dependently (1, 2, 5, 10, and 20 µmol/L of Trifluoperazine) |
| Animal experiment [2]: | |
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Animal models |
nude mice |
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Preparation Method |
In total 2 × 106 HCT116 cells were subcutaneously injected in rear flank of nude mice (five per group). The TFP (10 mg/kg, intraperitoneal) was administrated to each group for five times, 3 days apart. |
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Dosage form |
Intraperitoneal injection, 10 mg/kg, 5 times, 3 days apart |
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Applications |
Administration of TFP induced remarkably tumor regression with decreased tumor volume. The proliferation index Ki-67 was analyzed and found that TFP was able to reduce the Ki-67 levels in vivo. |
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References: [1]: Kang S, Hong J, Lee J M, et al. Trifluoperazine, a well-known antipsychotic, inhibits glioblastoma invasion by binding to calmodulin and disinhibiting calcium release channel IP3R[J]. Molecular cancer therapeutics, 2017, 16(1): 217-227. |
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| Cas No. | 117-89-5 | SDF | |
| 别名 | 三氟拉嗪 | ||
| 分子式 | C21H24F3N3S | 分子量 | 407.5 |
| 溶解度 | DMSO : 50mg/mL | 储存条件 | Store at -20°C |
| General tips | 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°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.454 mL | 12.2699 mL | 24.5399 mL |
| 5 mM | 0.4908 mL | 2.454 mL | 4.908 mL |
| 10 mM | 0.2454 mL | 1.227 mL | 2.454 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet