Catalog No.S2476 Synonyms: R 51211

Itraconazole Chemical Structure

Molecular Weight(MW): 705.65031

Itraconazole is a relatively potent inhibitor of CYP3A4 with IC50 of 6.1 nM, used as a triazole antifungal agent.

Size Price Stock Quantity  
USD 70 In stock
USD 120 In stock
Bulk Discount

Free Overnight Delivery on orders over $ 500
Next day delivery by 10:00 a.m. Order now.

Cited by 12 Publications

2 Customer Reviews

  • Resistance to itraconazole in MA cells. The parental SUM149-Luc cell line and MA1 cells were treated in parallel with 1 mM itraconazole for 9 days (which killed most of the cells in the parental cell line) and were allowed to recover and grow in a drug-free medium for 5 days before being stained. Since itraconazole was ineffective in killing MA1 cells, the cells grew into a continuous monolayer rather than colonies.

    PLoS One, 2014, 9(10):e109487.. Itraconazole purchased from Selleck.

    MCF-7 and SKBR-3 cells were treated as indicated and morphology of autophagosomes was observed with TEM (C). Autophagosomes (Avi, immature autophagic vacuoles, bold arrow), autolysosomes (Avd, degraded/late autophagic vacuoles, sharp arrow).

    Cancer Lett, 2017, 385:128-136. Itraconazole purchased from Selleck.

Purity & Quality Control

Choose Selective P450 (e.g. CYP17) Inhibitors

Biological Activity

Description Itraconazole is a relatively potent inhibitor of CYP3A4 with IC50 of 6.1 nM, used as a triazole antifungal agent.
CYP3A4 [6]
(human liver microsomes)
6.1 nM
In vitro

Itraconazole is metabolized into hydroxy-itraconazole (OH-ITZ), a known in vivo metabolite of ITZ, and two new metabolites: keto-itraconazole (keto-ITZ) and N-desalkyl-itraconazole (ND-ITZ). Itraconazole is a substrate for CYP3A in vitro and to characterize the metabolites generated. Itraconazole exhibits an unbound Km of 3.9 nM for CYP3A. Itraconazole metabolites are as potent as or more potent CYP3A4 inhibitors than ITZ itself. [1] Itraconazole appears to act on the essential Hh pathway component Smoothened (SMO) by a mechanism distinct from that of cyclopamine and other known SMO antagonists, and prevents the ciliary accumulation of SMO normally caused by Hh stimulation. [2] Itraconazole is active against 60 clinical isolates of Aspergillus spp. with geometric mean (GM) MICs of 0.25 mg/mL. [3] Itraconazole acts primarily by impairing the synthesis of ergosterol, resulting in a defective fungal cell membrane with altered permeability and function. Itraconazole is effective for a wide variety of mycotic infections and some fungal meningeal infections. [4] Itraconazole has an affinity for mammalian cytochrome P-450 enzymes as well as for fungal P-450-dependent enzyme, and thus has the potential for clinically important interactions (e.g., astemizole, terfenadine, rifampin, oral contraceptives, H2 receptor antagonists, warfarin, cyclosporine). [5]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human hepatocytes NWX1T2xHTnWwY4Tpc44h[XO|YYm= MUHJcohq[mm2aX;uJI9nKEO\UEPBOEBqdiCqdX3hckBp\XCjdH;jfZRmeyC3c3nu[{B1\XO2b4P0[ZJwdmViYYOgd5Vje3S{YYTlJIJ6KEiSTFOvUXMwVVNibXX0bI9lNCCLQ{WwQVAvODdizszN NFHhfmkzPDl2OEW2OS=>
human HTLA cells MmjLSpVv[3Srb36gZZN{[Xl? MUWyNEBucW6| M{LVTGlvcGmkaYTpc44hd2ZiQ2izR2wyNXO2aX31cIF1\WRiQ2izR3IyKGmwIHj1cYFvKEiWTFGgZ4VtdHNicILlMYlv[3WkYYTl[EBnd3JiMkCgcYlveyCvZXHzeZJm\CCxbjDkZZkhPCCkeTDi[ZRiKGG{cnXzeIlvNXKnY4L1bZRu\W62IH3l[IlifGWmIHz1Z4ln\XKjc3WgdoVxd3K2ZYKg[4Vv\SCjc4PhfUwhUUN3ME2wMlEh|ryP NG\HZXMzOzR|N{e3Ni=>
LLC-PK1 epithelial cells MV3GeY5kfGmxbjDhd5NigQ>? MnLSTY5pcWKrdHnvckBw\iCSLXfsfYNweHKxdHXpckwhdW:3c3WgUE1u\HJzYTDlfJBz\XO|ZXSgbY4hVEyFLWDLNUBmeGm2aHXsbYFtKGOnbHzzJJV{cW6pIHPhcINmcW5vQV2gdI9t[XKrc3H0bY9vKGG|c3H5MEBKSzVyPUCuNkDPxE1? MWGxNlY6QTN6OR?=
human PBMC NFnycpREgXSxdH;4bYNqfHliYYPzZZk> MnXLO|IhcA>? NImxd|REgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBRSk2FIHHzd4V{e2WmIHHzJINmdGxidnnhZoltcXS7IHHmeIVzKDd{IHjyd{BjgSCPVGSgZZN{[XluIFnDOVA:OS53MzFOwG0> MoP0NlQ1QDV5OEO=
Topp 3 cells M4C5TmZ2dmO2aX;uJIF{e2G7 M3nm[WlvcGmkaYTpc44hd2ZiaIXtZY4hS1mSNUGg[ZhxemW|c3XkJIlvKFSxcICgN{Bk\WyuczDifUBt[W6xc4Tldo9tKGSnbXX0bJlt[XOnIHHzd4F6NCCLQ{WwQVMvPiEQvF2= NUP6XmlxOTdzOUS3NVY>
human MRC5 cells NVK5fm02S3m2b4TvfIlkcXS7IHHzd4F6 MVLDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDNVmM2KGOnbHzzMEBESzVyPUS5MlM{KM7:TR?= M2r4NlIxQDB3M{m4
human HUVEC cells NHvmVG5HfW6ldHnvckBie3OjeR?= NUHHZYM2OiEQvF2= NIjYbFMzPCCq NGjCbolKdmirYnn0bY9vKG:oIG\FS2ZTOiCpbInjc5N6dGG2aX;uJIlvKGi3bXHuJGhWXkWFIHPlcIx{KGG2IEKgeW0h[W[2ZYKgNlQhcHK|IHL5JHdme3Sncn6gZoxwfCCjbnHsfZNqew>? NEDMb5MzOTl|NkWxOC=>

... Click to View More Cell Line Experimental Data

In vivo Itraconazole, like other Hh pathway antagonists, can suppress Hh pathway activity and the growth of medulloblastoma in a mouse allograft model. [2]


Solubility (25°C)

In vitro DMSO 7 mg/mL warmed (9.91 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
5% DMSO+70% PEG 300+ddH2O
For best results, use promptly after mixing.

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 705.65031


CAS No. 84625-61-6
Storage powder
in solvent
Synonyms R 51211

Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

  • Mass
    Molecular Weight

*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

  • C1

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04121910 Not yet recruiting Drug: Savolitinib|Drug: Itraconazole Solid Tumour AstraZeneca|Parexel October 31 2019 Phase 1
NCT03923010 Recruiting Drug: Itraconazole Mycoses Janssen Research & Development LLC August 6 2019 Phase 4
NCT03960606 Recruiting Combination Product: PUR1900 Asthma Pulmatrix Inc. July 31 2019 Phase 2
NCT04018872 Recruiting Drug: Itraconazole Esophagus Adenocarcinoma|Esophagus Squamous Cell Carcinoma|Gastroesophageal Junction Adenocarcinoma Dallas VA Medical Center June 24 2019 Phase 2
NCT04031053 Enrolling by invitation Other: Pharmacokinetic study Pharmacokinetics|Efavirenz|Penicilliosis Chiang Mai University|Thailand Research Fund June 1 2019 --
NCT03991312 Completed Drug: itraconazole|Drug: rifampin|Drug: mitapivat sulfate Healthy Volunteers Agios Pharmaceuticals Inc. June 20 2019 Phase 1

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

  • * Indicates a Required Field

Frequently Asked Questions

  • Question 1:

    We are finding the best vehicle to administer Itraconazole to mice. We want a mild vehicle (unlike DMSO) which resembles water, PBS, saline (for i.p/ injection) or methyl cellulose (for oral).

  • Answer:

    We are not able to dissolve S2476 Itraconazole clearly without DMSO. For oral gavage, this compound can be dissolved in 1% CMC Na at 20mg/ml as a homogeneous suspension.

P450 (e.g. CYP17) Signaling Pathway Map

Related P450 (e.g. CYP17) Products

Tags: buy Itraconazole | Itraconazole supplier | purchase Itraconazole | Itraconazole cost | Itraconazole manufacturer | order Itraconazole | Itraconazole distributor
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID