Itraconazole
Based on 24 publication(s) in Google Scholar
Itraconazole (R51211) is a triazole antifungal agent and a potent and orally active Hedgehog (Hh) signaling pathway antagonist with an IC50 of ~800 nM. Itraconazole potently inhibits lanosterol 14α-demethylase (cytochrome P450 enzyme), thereby inhibits the oxidative conversion of lanosterol to ergosterol. Itraconazole has anticancer and antiangiogenic effects. Itraconazole is a oxysterol-binding protein (OSBP) inhibitor.
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- Pureza : 99.59%
- No. CAS: 84625-61-6
- Fòrmula: C35H38Cl2N8O4
- Peso molecular:705.63
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Almacenamiento:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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Chemical Information
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Solvente y solubilidad
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Publications Citing Use of MedChemExpress (MCE) Itraconazole
More- Immunity. 2023 Mar 14;56(3):500-515.e6. [Abstract]
- Nat Commun. 2024 Oct 8;15(1):8723. [Abstract]
- J Exp Clin Cancer Res. 2019 Sep 13;38(1):404. [Abstract]
- Adv Sci (Weinh). 2025 Feb;12(7):e2409416. [Abstract]
- Cancer Lett. 2023 Jun 28:564:216208. [Abstract]
- Sci China Life Sci. 2022 Feb;65(2):341-361. [Abstract]
- Cell Rep. 2025 Dec 24;45(1):116797.
- Front Microbiol. 2025 Sep 3:16:1648467. [Abstract]
- Front Cell Infect Microbiol. 2020 Jun 26:10:320. [Abstract]
- BMC Microbiol. 2025 Nov 5;25(1):715. [Abstract]
- Molecules. 2022 Oct 12;27(20):6815. [Abstract]
- AAPS PharmSciTech. 2020 Oct 6;21(7):272. [Abstract]
- Appl Microbiol Biotechnol. 2025 Jan 24;109(1):21. [Abstract]
- Microbiol Spectr. 2025 May 6;13(5):e0318524. [Abstract]
- Microbiol Spectr. 2023 Jun 15;11(3):e0530222. [Abstract]
- Biotechnol Bioeng. 2021 Dec;118(12):4687-4698. [Abstract]
- Med Mycol. 2018 Jun 1;56(4):452-457. [Abstract]
- Mycoses. 2022 Apr;65(4):458-465. [Abstract]
- AAPS J. 2021 Jun 28;23(4):91. [Abstract]
- Infect Drug Resist. 2022 Dec 15:15:7459-7473. [Abstract]
- J Mycol Med. 2025 Sep 2;35(4):101577. [Abstract]
- J Mycol Med. 2022 Mar;32(1):101227. [Abstract]
- Open Life Sci. 2025 Apr 29;20(1):20221062. [Abstract]
- SSRN. 2026 Mar 7.
Customer Validation & Images
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Cell Proliferation/Viability Assay
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In Vivo Efficacy Study
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RT-PCR
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ELISA
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ELISA
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Actividad biológica
Descripciòn
IC50 & Target
Fungal[1]
IC50: ~800 nM (Hedgehog signaling pathway)[1]
14α-demethylase (cytochrome P450 enzyme)[3]
In Vitro
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female outbred athymic nude mice (6-7-week-old) injected with Ptch+/− cells[1]
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Dosage:75 mg/kg, 100 mg/kg
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Administration:Oral gavage; twice per day; for 18 days
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Result:Suppressed Hh pathway activity and the growth of medulloblastoma in a mouse allograft model.
Ensayo clínico
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 84625-61-6
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Appearance Solid
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Peso molecular 705.63
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Fòrmula C35H38Cl2N8O4
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Color White to off-white
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SMILES
ClC1=C(C=CC(Cl)=C1)[C@@]2(O[C@@H](COC3=CC=C(N4CCN(C5=CC=C(N(C=NN6C(C)CC)C6=O)C=C5)CC4)C=C3)CO2)CN7C=NC=N7
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Synonyms
R51211
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Publications (24)
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Journal Impact Factor
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Most Recent
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Immunity
ARMH3-mediated recruitment of PI4KB directs Golgi-to-endosome trafficking and activation of the antiviral effector STING. [Abstract]2023 Mar 14;56(3):500-515.e6. PMID: 36921576 -
Nat Commun
A germline-to-soma signal triggers an age-related decline of mitochondrial stress response. [Abstract]2024 Oct 8;15(1):8723. PMID: 39379393
Itraconazole purchased from MedChemExpress. Usage Cited in: Nat Commun. 2024 Oct 8;15(1):8723. [Abstract]
Litter size of seven-month-old C57BL/6J females treated with DMSO or Itraconazole (10 mg/kg, ip, daily), mated with males of the same treatment group.
Itraconazole purchased from MedChemExpress. Usage Cited in: Nat Commun. 2024 Oct 8;15(1):8723. [Abstract]
qRT-PCR analysis of Gli1, Hhip, and Smo mRNA levels in seven-month-old C57BL/6J male and female mice treated with DMSO or Itraconazole (10 mg/kg, ip, daily).
Itraconazole purchased from MedChemExpress. Usage Cited in: Nat Commun. 2024 Oct 8;15(1):8723. [Abstract]
Serum AMH levels assessed by ELISA in mice treated with DMSO or Itraconazole (10 mg/kg, ip, daily, 7 days).
Itraconazole purchased from MedChemExpress. Usage Cited in: Nat Commun. 2024 Oct 8;15(1):8723. [Abstract]
Testosterone levels assessed by ELISA in mice treated with DMSO or Itraconazole (10 mg/kg, ip, daily).
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J Exp Clin Cancer Res
SCP2-mediated cholesterol membrane trafficking promotes the growth of pituitary adenomas via Hedgehog signaling activation. [Abstract]2019 Sep 13;38(1):404. PMID: 31519191
Itraconazole purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2019 Sep 13;38(1):404. [Abstract]
SCP2-OE GH3 cells are incubated with 10 μM itraconazole (ITR) for 48 h. The distribution of cholesterol (blue) in the different groups (Vector, SCP2-OE and SCP2-OE + ITR) are examined by filipin staining and laser confocal microscopy. Green signal, GH staining; red signal, PI nuclear staining. Scale bar, 10 μm.
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Adv Sci (Weinh)
Itraconazole Reversing Acquired Resistance to Osimertinib in NSCLC by Inhibiting the SHH/DUSP13B/p-STAT3 Axis. [Abstract]2025 Feb;12(7):e2409416. PMID: 39721017
Itraconazole purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2025 Feb;12(7):e2409416. [Abstract]
The effect of Itraconazole (0.5-2 μM, 48 h) in combination with Osimertinib on the proliferation of PC‐9/AR and HCC827/AR cells was determined by CCK8.
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Cancer Lett
Myeloid-derived suppressor cells deficient in cholesterol biosynthesis promote tumor immune evasion. [Abstract]2023 Jun 28:564:216208. PMID: 37150500 -
Sci China Life Sci
2022 Feb;65(2):341-361. PMID: 34047913 -
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Front Microbiol
Ire1 inhibitors attenuate Candida albicans pathogenicity and demonstrate potential for application in antifungal therapy. [Abstract]2025 Sep 3:16:1648467. PMID: 40969430 -
Front Cell Infect Microbiol
Caenorhabditis elegans- Based Aspergillus fumigatus Infection Model for Evaluating Pathogenicity and Drug Efficacy. [Abstract]2020 Jun 26:10:320. PMID: 32670897 -
BMC Microbiol
In vitro combination effects and mechanisms of Revaprazan with Triazole antifungal drugs on Aspergillus. [Abstract]2025 Nov 5;25(1):715. PMID: 41194018 -
Molecules
Itraconazole-Induced Increases in Gilteritinib Exposure Are Mediated by CYP3A and OATP1B. [Abstract]2022 Oct 12;27(20):6815. PMID: 36296409 -
AAPS PharmSciTech
A Novel Nanoemulsion Intermediate Gel as a Promising Approach for Delivery of Itraconazole: Design, In Vitro and Ex Vivo Appraisal. [Abstract]2020 Oct 6;21(7):272. PMID: 33025308 -
Appl Microbiol Biotechnol
Aloin remodels the cell wall of Candida albicans to reduce its hyphal virulence against oral candidiasis. [Abstract]2025 Jan 24;109(1):21. PMID: 39853490 -
Microbiol Spectr
Synergistic antifungal activity of minocycline as an effective augmenting agent of fluconazole against drug-resistant Candida tropicalis. [Abstract]2025 May 6;13(5):e0318524. PMID: 40162832 -
Microbiol Spectr
In Vitro and In Vivo Evaluation of Synergistic Effects of Everolimus in Combination with Antifungal Agents on Exophiala dermatitidis. [Abstract]2023 Jun 15;11(3):e0530222. PMID: 37140396 -
Biotechnol Bioeng
An integrated biomimetic array chip for establishment of collagen-based 3D primary human hepatocyte model for prediction of clinical drug-induced liver injury. [Abstract]2021 Dec;118(12):4687-4698. PMID: 34478150 -
Med Mycol
2018 Jun 1;56(4):452-457. PMID: 29420769 -
Mycoses
COVID-19-associated pulmonary aspergillosis in ICU patients in a German reference centre: Phenotypic and molecular characterisation of Aspergillus fumigatus isolates. [Abstract]2022 Apr;65(4):458-465. PMID: 35138651 -
AAPS J
Cannabinoid Interactions with Cytochrome P450 Drug Metabolism: a Full-Spectrum Characterization. [Abstract]2021 Jun 28;23(4):91. PMID: 34181150 -
Infect Drug Resist
Correlation Between Drug Resistance and Virulence of Candida Isolates from Patients with Candidiasis. [Abstract]2022 Dec 15:15:7459-7473. PMID: 36544991 -
J Mycol Med
Novel antifungal activity of broxyquinoline against ITC-Resistant mutants via inhibition of methionine aminopeptidase in Aspergillus fumigatus. [Abstract]2025 Sep 2;35(4):101577. PMID: 40957269 -
J Mycol Med
In vitro synergistic effect of minocycline combined with antifungals against Cryptococcus neoformans. [Abstract]2022 Mar;32(1):101227. PMID: 34800920 -
Open Life Sci
2025 Apr 29;20(1):20221062. PMID: 40321158 -
Solvente y solubilidad
In Vitro:
DMSO : 6.25 mg/mL (8.86 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, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 0.62 mg/mL (0.88 mM); Clear solution
This protocol yields a clear solution of ≥ 0.62 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (6.2 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.
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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: 0.5% CMC-Na/saline water
Solubility: 20 mg/mL (28.34 mM); Suspended solution; Need ultrasonic
In Vivo Dissolution Calculator
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. * In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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 (281 KB)
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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)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Kim, J., et al., Itraconazole, a commonly used antifungal that inhibits Hedgehog pathway activity and cancer growth. Cancer Cell, 2010. 17(4): p. 388-99. [Content Brief]
[2]. Chong, C.R., et al., Inhibition of angiogenesis by the antifungal drug itraconazole. ACS Chem Biol, 2007. 2(4): p. 263-70. [Content Brief]
[3]. Pace JR, et al. Repurposing the Clinically Efficacious Antifungal Agent Itraconazole as an Anticancer Chemotherapeutic. J Med Chem. 2016 Apr 28;59(8):3635-49. [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, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.4172 mL | 7.0859 mL | 14.1717 mL | 35.4293 mL |
| 5 mM | 0.2834 mL | 1.4172 mL | 2.8343 mL | 7.0859 mL |
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