Cat. No.: HY-17514

Itraconazole

(Synonyms: R51211)

24 Cited Publications

Customer Review

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.

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

Purity: 99.59%
CAS No.: 84625-61-6
Formula: C₃₅H₃₈Cl₂N₈O₄
Molecular Weight:705.63

Storage:

4°C, protect from light

* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Itraconazole Chemical Structure

CAS No.: 84625-61-6

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

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

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (24)
Solvent & Solubility
- In Vitro
- In Vivo
Purity & Documentation
References
Help & FAQs
Bioz

Biological Activity

Description

IC₅₀ & Target

Fungal^[1]
IC50: ~800 nM (Hedgehog signaling pathway)^[1]
14α-demethylase (cytochrome P450 enzyme)^[3]

All Cytochrome P450 Isoforms :

All Antibiotic Isoforms :

In Vitro

Itraconazole has anti-proliferation of HUVEC (IC₅₀ of 0.16 μM)^[2].
Itraconazole inhibits endothelial cell cycle progression at the G1 phase in vitro^[1].

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

In Vivo

Itraconazole (75-100 mg/kg; oral gavage; twice per day; for 18 days; female outbred athymic nude mice) treatment suppresses Hh pathway activity and the growth of medulloblastoma in a mouse allograft model^[1].

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

Animal Model:

Female outbred athymic nude mice (6-7-week-old) injected with Ptch^+/− cells^[1]
Dosage:

75 mg/kg, 100 mg/kg
Administration:

Oral gavage; twice per day; for 18 days
Result:

Suppressed Hh pathway activity and the growth of medulloblastoma in a mouse allograft model.

Clinical Trial

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

Chemical Information

CAS No. 84625-61-6
Appearance Solid
Molecular Weight 705.63
Formula C₃₅H₃₈Cl₂N₈O₄
Color White to off-white
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
Synonyms

R51211
Initial Source
- Microorganisms
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, protect from light

* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Publications (24)

All Cell Proliferation/Viability AssayIn Vivo Efficacy StudyRT-PCRELISAIF

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Journal Impact Factor

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).
Adv Sci (Weinh)

Itraconazole Reversing Acquired Resistance to Osimertinib in NSCLC by Inhibiting the SHH/DUSP13B/p-STAT3 Axis. [Abstract]

2024 Dec 25:e2409416. PMID: 39721017

Itraconazole purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2024 Dec 25: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.
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.
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

NPC1-regulated dynamic of clathrin-coated pits is essential for viral entry. [Abstract]

2022 Feb;65(2):341-361. PMID: 34047913
Cell Rep

2025 Dec 24;45(1):116797.
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
Molecules

Itraconazole-Induced Increases in Gilteritinib Exposure Are Mediated by CYP3A and OATP1B. [Abstract]

2022 Oct 12;27(20):6815. PMID: 36296409
Front Microbiol

Ire1 inhibitors attenuate Candida albicans pathogenicity and demonstrate potential for application in antifungal therapy. [Abstract]

2025 Sep 3:16:1648467. PMID: 40969430
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
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
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
Microbiol Spectr

Synergistic antifungal activity of minocycline as an effective augmenting agent of fluconazole against drug-resistant Candida tropicalis. [Abstract]

2025 Mar 31: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
AAPS J

Cannabinoid Interactions with Cytochrome P450 Drug Metabolism: a Full-Spectrum Characterization. [Abstract]

2021 Jun 28;23(4):91. PMID: 34181150
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
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
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
Med Mycol

Lonafarnib synergizes with azoles against Aspergillus spp. and Exophiala spp. [Abstract]

2018 Jun 1;56(4):452-457. PMID: 29420769
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

Effects of Ire1 gene on virulence and pathogenicity of Candida albicans. [Abstract]

2025 Apr 29;20(1):20221062. PMID: 40321158
SSRN

2026 Mar 7.

Solvent & Solubility

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)

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

1.4172 mL

7.0859 mL

14.1717 mL

5 mM

0.2834 mL

1.4172 mL

2.8343 mL

10 mM

---

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.

Molarity Calculator

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

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: ≥ 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.

Protocol 2

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

Solubility: ≥ 0.62 mg/mL (0.88 mM); Clear solution

This protocol yields a clear solution of ≥ 0.62 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 (6.2 mg/mL) to 900 μL Corn oil, and mix evenly.

Working 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.

Protocol 1

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:

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

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (274 KB)
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)
- Portuguese - PT (393 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)

References

[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]

[4]. Albulescu L, et al. Uncovering oxysterol-binding protein (OSBP) as a target of the anti-enteroviral compound TTP-8307. Antiviral Res. 2017;140:37-44.

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

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
DMSO	5 mM	0.2834 mL	1.4172 mL	2.8343 mL	7.0859 mL

Itraconazole

24 Cited Publications

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Itraconazole

Anti-Infection Compound Library

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Publications Citing Use of MedChemExpress (MCE) Itraconazole

All Cytochrome P450 Isoforms

All Antibiotic Isoforms

Biological Activity

Chemical Information

Publications (24)

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Itraconazole Related Classifications

Cat. No.: HY-17514