2. GPCR/G Protein Neuronal Signaling Autophagy
  3. 5-HT Receptor Dopamine Receptor Adrenergic Receptor Autophagy
  4. Sertindole

Sertindole  (Synonyms: Lu 23-174)

Cat. No.: HY-14543 Purity: 99.92%
COA Handling Instructions

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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.

For research use only. We do not sell to patients.

Sertindole Chemical Structure

Sertindole Chemical Structure

CAS No. : 106516-24-9

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 63 In-stock
Solution
10 mM * 1 mL in DMSO USD 63 In-stock
Solid
5 mg USD 58 In-stock
10 mg USD 94 In-stock
50 mg USD 424 In-stock
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Based on 2 publication(s) in Google Scholar

Other Forms of Sertindole:

Sertindole Related Antibodies

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α adrenergic receptor β adrenergic receptor

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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[1][2][3].

IC50 & Target

5-HT2A Receptor

 

5-HT2C Receptor

 

In Vitro

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.

Sertindole Related Antibodies

Cell Proliferation Assay[2]

Cell Line: SUM159 and MCF-10A cells
Concentration: 0-100 μM
Incubation Time: 48 hours
Result: Showed IC50s of 9.2 µM and 27.6 µM for SUM159 and MCF-10A cells, respectively.

Cell Proliferation Assay[2]

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
Concentration: 0.8-27.6 μM
Incubation Time: 48 hours
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.

Cell Migration Assay [2]

Cell Line: SUM159 cells
Concentration: 5 μΜ and 10 μΜ
Incubation Time: 24 hours
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).
In Vivo

Sertindole (oral gavage; 10 mg/kg; once daily; 12 d) shows anti-tumor activity in vivo[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Immune-deficient Balb/c mice implanted MDA-MB-231 human TNBC cells[2]
Dosage: 10 mg/kg
Administration: Oral gavage; 10 mg/kg; once daily; 12 days
Result: Exhibited a 22.7% reduction in size after a 12-day administration regimen.
Clinical Trial
Molecular Weight

440.94

Formula

C24H26ClFN4O
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

FC1=CC=C(N2C3=CC=C(Cl)C=C3C(C4CCN(CCN5CCNC5=O)CC4)=C2)C=C1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2679 mL 11.3394 mL 22.6788 mL
5 mM 0.4536 mL 2.2679 mL 4.5358 mL
View the 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.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

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.

  • Protocol 1

    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.
  • Protocol 2

    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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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.
Purity & Documentation

Purity: 99.92%

COA (254 KB) HNMR (262 KB) LCMS (93 KB)

Handling Instructions (2659 KB)
References

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
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Sertindole Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Sertindole106516-24-9Lu 23-1745-HT ReceptorDopamine ReceptorAdrenergic ReceptorAutophagySerotonin Receptor5-hydroxytryptamine ReceptorBeta Receptorantipsychotic activityanti-proliferative activityMCF-10ANCI-H460A549NCI-H446NCI-H661801-DU251A172U118-MGU87-MGAGSMKN45BGC-823SGC-7901HT-29COLO205SW480SW620HCT-15HepG2Bel-7402MCF-7MDA-MB-231SUM159T47DMDA-MB-453ZR-75-1CCRF-CEMK562JurkatInhibitorinhibitorinhibit

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