Art. -Nr.: HY-B0319

Tioconazole

(Synonyms: UK-20349)

4 Cited Publications

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Based on 4 publication(s) in Google Scholar

Tioconazole (UK-20349) is a broad-spectrum antifungal imidazole derivative. Tioconazole inhibits several dermatophytes and yeasts, with MIC₅₀ values of less than 3.12 mg/L and 9 mg/L, respectively. Additionally, Tioconazole exhibits anti-parasitic activity. Tioconazole exerts anticancer activity by inhibiting the PI3K/AKT/mTOR signaling pathway and blocking autophagy. Tioconazole is applicable for research in the fields of anti-infection and anticancer therapy.

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Reinheit: 99.90%
CAS. Nr.: 65899-73-2
Formel: C₁₆H₁₃Cl₃N₂OS
Molecular Weight:387.71

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Tioconazole Chemical Structure

CAS. Nr.: 65899-73-2

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Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (4)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

Antifungal^[1].

Alle Antibiotic Isoform-spezifische Produkte anzeigen :

Alle Parasite Isoform-spezifische Produkte anzeigen :

Alle Akt Isoform-spezifische Produkte anzeigen :

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In Vitro

Tioconazole (10-40 μM, 24 hours) induces apoptosis and inhibits cell migration in HeLa cells through mitotic arrest, exhibiting anticancer activity (IC₅₀: 14.9 μM)^[3].

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

Cell Proliferation Assay^[3]

Cell Line:

HeLa cells (cervical cancer)
Concentration:

0-80 μM
Incubation Time:

24 hours
Result:

Inhibited HeLa cell proliferation in a concentration-dependent manner, IC₅₀: 14.9 μM. At 5, 10, 15, 20, 30, 60, and 80 μM, cell proliferation inhibition rates were 22%, 28%, 50%, 59%, 65%, 79%, and 86%, respectively.

Cell Cycle Analysis^[3]

Cell Line:

HeLa cells (cervical cancer)
Concentration:

10, 20, 30, 40 μM
Incubation Time:

24 hours
Result:

Induced cell cycle arrest in mitosis, with 13%, 37%, 35%, and 13% of cells arrested at mitosis at 10, 20, 30, and 40 μM, respectively. The highest arrest was observed at 20 μM.

Apoptosis Analysis^[3]

Cell Line:

HeLa cells (cervical cancer)
Concentration:

10, 20, 40 μM
Incubation Time:

24 hours
Result:

Induced apoptosis in HeLa cells, with 4%, 17%, and 32% of cells undergoing apoptosis at 10, 20, and 40 μM, respectively. The 40 μM group showed more pronounced nuclear fragmentation and chromatin condensation.

Cell Migration Assay ^[3]

Cell Line:

HeLa cells (cervical cancer)
Concentration:

10, 20 μM
Incubation Time:

24, 48, 72 hours
Result:

Inhibited HeLa cell migration, with migration rates of 25%, 34%, and 55% in the 10 μM group and 10%, 13%, and 19% in the 20 μM group at 24, 48, and 72 hours, respectively, significantly lower than the control group (p < 0.0001).

In Vivo

Tioconazole (60 mg/kg, i.p., once every 3 days for 43 days) in combination with Doxorubicin (HY-15142) (5 mg/kg) and Chloroquine (HY-17589A) (50 mg/kg) exerts anti-tumor effects in the MCF-7 cell xenograft breast cancer BALB/c mouse model by inhibiting the PI3K/AKT/mTOR signaling pathway and blocking autophagy^[4].
Tioconazole (60 mg/kg, i.p., once every other day for 21 days) enhances the anti-tumor effects of Dox in the HCT116 cell xenograft colorectal cancer nude mouse model^[5].

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

Animal Model:

MCF-7 cell xenograft breast cancer BALB/c mouse model^[4]
Dosage:

60 mg/kg
Administration:

Intraperitoneal injection (i.p.), once every three days, for 43 days
Result:

Inhibited tumor growth, reduced Ki-67 and PI3K/AKT/mTOR signaling activity, promoted LC3-II and p62 accumulation, indicating autophagic flux blockade, and enhanced apoptosis.

Animal Model:

HCT116 cell xenograft colorectal cancer nude mouse model^[5]
Dosage:

Tioconazole: 60 mg/kg，Doxorubicin: 5 mg/kg，Chloroquine: 50 mg/kg
Administration:

Tioconazole: Intraperitoneal injection (i.p.), once every 3 days, for 43 days; Doxorubicin: Intravenous injection (i.v.), once per week, for 6 weeks; Chloroquine: Intraperitoneal injection (i.p.), once daily, for 43 days
Result:

Reduced xenograft tumor volume and sensitized xenograft tumors to Dox-induced cell death.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 65899-73-2
Appearance Solid
Molecular Weight 387.71
Formel C₁₆H₁₃Cl₃N₂OS
Color White to off-white
SMILES

ClC1=CC=C(C(OCC2=C(Cl)SC=C2)CN3C=CN=C3)C(Cl)=C1
Synonyms

UK-20349
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (4)

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Journal Impact Factor

ACS Environ Au

Machine Learning-Assisted Recognition of Environmental Sulfur-Containing Chemicals in Nontargeted Mass Spectrometry Analysis of Inadequate Mass Resolution. [Abstract]

2025 Aug 5;5(6):573-582. PMID: 41277996
Anal Chem

Exposome-Scale Investigation of Cl-/Br-Containing Chemicals Using High-Resolution Mass Spectrometry, Multistage Machine Learning, and Cloud Computing. [Abstract]

2025 Jun 3;97(21):11099-11109. PMID: 40401576
Drug Metab Dispos

Metabolic flux analysis of bile acid biosynthesis acidic pathway in HepG2 cells reveals CYP8B1 inhibition of azole antifungals. [Abstract]

2025 Nov;53(11):100168. PMID: 41124962
Int J Parasitol Drugs Drug Resist

Lower micromolar activity of the antifungal imidazoles on the bacterial-type bifunctional aldehyde/alcohol dehydrogenase (AdhE) in Cryptosporidium parvum and in vitro efficacy against the zoonotic parasite. [Abstract]

2024 Jun 6:25:100551. PMID: 38875756

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : ≥ 100 mg/mL (257.92 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : < 0.1 mg/mL (insoluble)

* "≥" means soluble, but saturation unknown.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.5792 mL

12.8962 mL

25.7925 mL

5 mM

0.5158 mL

2.5792 mL

5.1585 mL

10 mM

0.2579 mL

1.2896 mL

2.5792 mL

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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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 (6.45 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.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (6.45 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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (6.45 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (286 KB)
SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. S P Clissold, et al. Tioconazole. A review of its antimicrobial activity and therapeutic use in superficial mycoses. Drugs. 1986 Jan;31(1):29-51. [Content Brief]

[2]. Yamamoto ES, et al. Activity of Fenticonazole, Tioconazole and Nystatin on New World Leishmania Species. Curr Top Med Chem. 2018;18(27):2338-2346. [Content Brief]

[3]. Sebastian J, et al. Cytotoxic mechanism of tioconazole involves cell cycle arrest at mitosis through inhibition of microtubule assembly. Cytotechnology. 2022 Feb;74(1):141-162. [Content Brief]

[4]. El-Gowily AH, et al. Tioconazole and Chloroquine Act Synergistically to Combat Doxorubicin-Induced Toxicity via Inactivation of PI3K/AKT/mTOR Signaling Mediated ROS-Dependent Apoptosis and Autophagic Flux Inhibition in MCF-7 Breast Cancer Cells. Pharmaceuticals (Basel). 2021 Mar 11;14(3):254. [Content Brief]

[5]. Liu PF, et al. Drug Repurposing Screening Identifies Tioconazole as an ATG4 Inhibitor that Suppresses Autophagy and Sensitizes Cancer Cells to Chemotherapy. Theranostics. 2018 Jan 1;8(3):830-845. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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	2.5792 mL	12.8962 mL	25.7925 mL	64.4812 mL
	5 mM	0.5158 mL	2.5792 mL	5.1585 mL	12.8962 mL
	10 mM	0.2579 mL	1.2896 mL	2.5792 mL	6.4481 mL
	15 mM	0.1719 mL	0.8597 mL	1.7195 mL	4.2987 mL
	20 mM	0.1290 mL	0.6448 mL	1.2896 mL	3.2241 mL
	25 mM	0.1032 mL	0.5158 mL	1.0317 mL	2.5792 mL
	30 mM	0.0860 mL	0.4299 mL	0.8597 mL	2.1494 mL
	40 mM	0.0645 mL	0.3224 mL	0.6448 mL	1.6120 mL
	50 mM	0.0516 mL	0.2579 mL	0.5158 mL	1.2896 mL
	60 mM	0.0430 mL	0.2149 mL	0.4299 mL	1.0747 mL
	80 mM	0.0322 mL	0.1612 mL	0.3224 mL	0.8060 mL
	100 mM	0.0258 mL	0.1290 mL	0.2579 mL	0.6448 mL

Tioconazole

4 Cited Publications

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Tioconazole

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Publications Citing Use of MedChemExpress (MCE) Tioconazole

Alle Antibiotic Isoform-spezifische Produkte anzeigen

Alle Parasite Isoform-spezifische Produkte anzeigen

Alle Akt Isoform-spezifische Produkte anzeigen

Alle PI3K Isoform-spezifische Produkte anzeigen

Alle mTOR Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (4)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs