Sertindole
Based on 3 publication(s) in Google Scholar
Sertindole (Lu 23-174) is an orally active 5-HT2A, 5-HT2C, dopamine D2, and αl-adrenergic receptors antagonist. Sertindole shows antipsychotic activity and anti-proliferative activity to multiple cancer cells.
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- Pureza: 99.92%
- No. CAS: 106516-24-9
- Fòrmula: C24H26ClFN4O
- Peso molecular:440.94
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Publications Citing Use of MedChemExpress (MCE) Sertindole
MoreVer todos los productos específicos de isoformas 5-HT Receptor
MoreVer todos los productos específicos de isoformas Dopamine Receptor
MoreVer todos los productos específicos de isoformas Adrenergic Receptor
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Actividad biológica
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5-HT2A Receptor |
5-HT2C Receptor |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO | IC50 |
2.7 nM
Compound: sertindole
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Inhibition of human cloned ERG expressed in CHO cells assessed as inhibition of potassium channel current by automated patch clamp assay
Inhibition of human cloned ERG expressed in CHO cells assessed as inhibition of potassium channel current by automated patch clamp assay
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[PMID: 24805037] |
| CHO | IC50 |
3 nM
Compound: Sertindole
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Inhibition of K+ channel activity in CHO cells expressing HERG Kv11.1
Inhibition of K+ channel activity in CHO cells expressing HERG Kv11.1
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[PMID: 12729675] |
| CHO | IC50 |
6.3 μM
Compound: sertindole
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Inhibition of Cav1.2 current measured using QPatch automatic path clamp system in CHO cells expressing Cav1.2, beta-2 and alpha-2/delta-1 subunits
Inhibition of Cav1.2 current measured using QPatch automatic path clamp system in CHO cells expressing Cav1.2, beta-2 and alpha-2/delta-1 subunits
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[PMID: 23812503] |
Sertindole (0-100 μM; 48 h) attenuates proliferation of breast cancer cells[2].
Sertindole (0.8-27.6 μM; 48 h) inhibits proliferation toward many cancers in vitro[2].
Sertindole (5 μΜ and 10 μΜ; 24 h) attenuates migration of breast cancer cells[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:SUM159 and MCF-10A cells
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Concentration:0-100 μM
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Incubation Time:48 hours
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Result:Showed IC50s of 9.2 µM and 27.6 µM for SUM159 and MCF-10A cells, respectively.
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Cell Line:NCI-H460, A549, NCI-H446, NCI-H661, 801-D, U251, A172, U118-MG, U87-MG, AGS, MKN45, BGC-823, SGC-7901, HT-29, COLO205, SW480, SW620, HCT-15, HepG2, Bel-7402, MCF-7, MDA-MB-231, SUM159, T47D, MDA-MB-453, ZR-75-1, CCRF-CEM, K562, Jurkat, MCF-10A cells
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Concentration:0.8-27.6 μM
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Incubation Time:48 hours
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Result:Showed IC50s ranging between 0.8-12.7 µM, 2.7-4.6 µM, 12.7-15.3 µM and 8.6-16.1 µM for breast cancer, leukemia, hepatoma and glioblastoma lines, respectively.
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Cell Line:SUM159 cells
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Concentration:5 μΜ and 10 μΜ
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Incubation Time:24 hours
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Result:Blocked around 50% cells traversing the membranes at 5 μΜ, and almost all the cells lost traversing ability at 10 μΜ.
Elevated LC3II conversion significantly (P < 0.01).
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Immune-deficient Balb/c mice implanted MDA-MB-231 human TNBC cells[2]
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Dosage:10 mg/kg
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Administration:Oral gavage; 10 mg/kg; once daily; 12 days
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Result:Exhibited a 22.7% reduction in size after a 12-day administration regimen.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 106516-24-9
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Appearance Solid
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Peso molecular 440.94
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Fòrmula C24H26ClFN4O
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Color White to off-white
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SMILES
FC1=CC=C(N2C3=CC=C(Cl)C=C3C(C4CCN(CCN5CCNC5=O)CC4)=C2)C=C1
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Synonyms
Lu 23-174
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (3)
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Journal Impact Factor
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Most Recent
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Microsyst Nanoeng
A biosensing system using a multiparameter nonlinear dynamic analysis of cardiomyocyte beating for drug-induced arrhythmia recognition. [Abstract]2022 May 9;8:49. PMID: 35547605 -
Eur J Pharm Sci
Repurposing of FDA-approved drugs by targeting SIRT2 to alleviate inflammatory response and kidney injury. [Abstract]2025 Sep 27:214:107296. PMID: 41022315 -
ACS Omega
Antibacterial and Antibiofilm Activities of Sertindole and Its Antibacterial Mechanism against Staphylococcus aureus. [Abstract]2023 Feb 3;8(6):5415-5425. PMID: 36816695
Solvente y solubilidad
DMSO : 25 mg/mL (56.70 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.67 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (5.67 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureza y Documentación
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Ficha de datos (282 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. David Murdoch, et al. Sertindole : a review of its use in schizophrenia. CNS Drugs. 2006;20(3):233-55. [Content Brief]
[2]. Wei Zhang, et al. Antiproliferative activities of the second-generation antipsychotic drug sertindole against breast cancers with a potential application for treatment of breast-to-brain metastases. Sci Rep. 2018 Oct 25;8(1):15753. [Content Brief]
[3]. Mario F Juruena, et al. Sertindole in the management of schizophrenia. J Cent Nerv Syst Dis. 2011 May 17;3:75-85. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.2679 mL | 11.3394 mL | 22.6788 mL | 56.6971 mL |
| 5 mM | 0.4536 mL | 2.2679 mL | 4.5358 mL | 11.3394 mL | |
| 10 mM | 0.2268 mL | 1.1339 mL | 2.2679 mL | 5.6697 mL | |
| 15 mM | 0.1512 mL | 0.7560 mL | 1.5119 mL | 3.7798 mL | |
| 20 mM | 0.1134 mL | 0.5670 mL | 1.1339 mL | 2.8349 mL | |
| 25 mM | 0.0907 mL | 0.4536 mL | 0.9072 mL | 2.2679 mL | |
| 30 mM | 0.0756 mL | 0.3780 mL | 0.7560 mL | 1.8899 mL | |
| 40 mM | 0.0567 mL | 0.2835 mL | 0.5670 mL | 1.4174 mL | |
| 50 mM | 0.0454 mL | 0.2268 mL | 0.4536 mL | 1.1339 mL |
Sertindole Related Classifications
HY-14543 Related Classifications
Powered by Bioz
- Sertindole
- 106516-24-9
- Lu 23-174
- 5-HT Receptor
- Dopamine Receptor
- Adrenergic Receptor
- Autophagy
- antipsychotic activity
- anti-proliferative activity
- MCF-10A
- NCI-H460
- A549
- NCI-H446
- NCI-H661
- 801-D
- U251
- A172
- U118-MG
- U87-MG
- AGS
- MKN45
- BGC-823
- SGC-7901
- HT-29
- COLO205
- SW480
- SW620
- HCT-15
- HepG2
- Bel-7402
- MCF-7
- MDA-MB-231
- SUM159
- T47D
- MDA-MB-453
- ZR-75-1
- CCRF-CEM
- K562
- Jurkat
- Inhibitor
- inhibitor
- inhibit