For research use only.

Catalog No.S2476 Synonyms: R 51211

18 publications

Itraconazole Chemical Structure

CAS No. 84625-61-6

Itraconazole (R 51211) is a relatively potent inhibitor of CYP3A4 with IC50 of 6.1 nM, used as a triazole antifungal agent. Itraconazole is a potent antagonist of the Hedgehog (Hh) signaling pathway. Itraconazole suppresses the growth of glioblastoma through induction of autophagy.

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Selleck's Itraconazole has been cited by 18 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 Hedgehog/Smoothened Inhibitors

Biological Activity

Description Itraconazole (R 51211) is a relatively potent inhibitor of CYP3A4 with IC50 of 6.1 nM, used as a triazole antifungal agent. Itraconazole is a potent antagonist of the Hedgehog (Hh) signaling pathway. Itraconazole suppresses the growth of glioblastoma through induction of autophagy.
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 NHHDd5lHfW6ldHnvckBie3OjeR?= M3TPWGlvcGmkaYTpc44hd2ZiQ2nQN2E1KGmwIHj1cYFvKGincHH0c4N6fGW|IIXzbY5oKHSnc4Tvd5Rmem:wZTDhd{B{fWK|dILheIUh[nliSGDMR{9OWy:PUzDt[ZRpd2RuIFnDOVA:OC5yNzFOwG0> MnHLNlQ6PDh3NkW=
human HTLA cells MWLGeY5kfGmxbjDhd5NigQ>? MW[yNEBucW6| NYL1e3FJUW6qaXLpeIlwdiCxZjDDXFNEVDFvc4TpcZVt[XSnZDDDXFNEWjFiaX6gbJVu[W5iSGTMRUBk\WyuczDwdoUucW6ldXLheIVlKG[xcjCyNEBucW6|IH3lZZN2emWmIH;uJIRigSB2IHL5JIJmfGFiYYLy[ZN1cW5vcnXjdpVqfG2nboSgcYVlcWG2ZXSgcJVkcW[ncnHz[UBz\XCxcoTldkBo\W6nIHHzd4F6NCCLQ{WwQVAvOSEQvF2= MVmyN|Q{Pzd5Mh?=
LLC-PK1 epithelial cells NEL1V5JHfW6ldHnvckBie3OjeR?= NYDGToIxUW6qaXLpeIlwdiCxZjDQMYdtgWOxcILveIVqdixibX;1d4UhVC2vZIKxZUBmgHC{ZYPz[YQhcW5iTFzDMXBMOSCncHn0bIVtcWGuIHPlcIx{KHW|aX7nJINidGOnaX6tRW0heG:uYYLpd4F1cW:wIHHzd4F6NCCLQ{WwQVAvOiEQvF2= MoTRNVI3QTl|OEm=
human PBMC MkTiR5l1d3SxeHnjbZR6KGG|c3H5 MorQO|IhcA>? M{n1OGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJHBDVUNiYYPz[ZN{\WRiYYOgZ4VtdCC4aXHibYxqfHliYX\0[ZIhPzJiaILzJIJ6KE2WVDDhd5NigSxiSVO1NF0yNjV|IN88US=> MoXkNlQ1QDV5OEO=
Topp 3 cells MlzDSpVv[3Srb36gZZN{[Xl? NH3UTlJKdmirYnn0bY9vKG:oIHj1cYFvKEO\UEWxJIV5eHKnc4Pl[EBqdiCWb4DwJFMh[2WubIOgZpkhdGGwb4P0[ZJwdCCmZX3leIh6dGG|ZTDhd5NigSxiSVO1NF0{NjZizszN M3TTSVE4OTl2N{G2
human MRC5 cells MmW5R5l1d3SxeHnjbZR6KGG|c3H5 NEGzXpVEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBOWkN3IHPlcIx{NCCFQ{WwQVQ6NjN|IN88US=> NHjP[HAzODhyNUO5PC=>
human HUVEC cells NWnScGd7TnWwY4Tpc44h[XO|YYm= NFzUVnUzKM7:TR?= MlHUNlQhcA>? M4ThU2lvcGmkaYTpc44hd2ZiVlXHSnIzKGeueXPvd5lt[XSrb36gbY4hcHWvYX6gTHVXTUNiY3XscJMh[XRiMjD1UUBi\nSncjCyOEBpenNiYomgW4V{fGW{bjDicI91KGGwYXz5d4l{ NH\melQzOTl|NkWxOC=>

... Click to View More Cell Line Experimental Data

Methods Test Index PMID
Western blot
pACC / ACC / p-S6K / S6K ; 

PubMed: 28103683     

HUVEC were treated with drugs as indicated for 1 h, and AMPK/mTOR activity was monitored by phosphorylation of their respective substrates. Unlike itraconazole, the NPC phenotype-inducing compounds U18666A and imipramine inhibited mTOR without affecting AMPK activity. 

GLI1 / GLI2 / p-AKT1 / AKT1 / Cyclin D1 ; 

PubMed: 27388747     

Pathway components of Hh and AKT signaling are decreased in ASZ001 cells treated with itraconazole. ASZ001 cells were treated with varying concentrations of itraconazole for 24 hours. The levels of GLI1, GLI2, p-AKT1, and cyclin D1 were assessed by Western blotting.

28103683 27388747
Growth inhibition assay
Cell viability; 

PubMed: 24905460     

U87 or C6 cells were treated with indicated concentrations of itraconazole for 36 h. Cell viability was measured by the MTT assay. The data were representative of 5 independent experiments. 

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+40% PEG 300+10% Tween 80+45% 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
Smiles CCC(C)N1C(=O)N(C=N1)C2=CC=C(C=C2)N3CCN(CC3)C4=CC=C(C=C4)OCC5COC(O5)(CN6C=NC=N6)C7=C(C=C(C=C7)Cl)Cl

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Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Dosage mg/kg Average weight of animals g Dosing volume per animal ul Number of animals
Step 2: Enter the in vivo formulation ()
% DMSO % % Tween 80 % ddH2O

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04312282 Recruiting Drug: Tesetaxel|Drug: Itraconazole|Drug: Rifampin Advanced Solid Tumors Odonate Therapeutics Inc. March 6 2020 Phase 1
NCT04121910 Completed Drug: Savolitinib|Drug: Itraconazole Solid Tumour AstraZeneca|Parexel November 7 2019 Phase 1
NCT04166669 Completed Drug: APX001|Drug: Itraconazole|Drug: Rifampin Fungal Infection Amplyx Pharmaceuticals November 12 2019 Phase 1
NCT03923010 Recruiting Drug: Itraconazole Mycoses Janssen Research & Development LLC August 6 2019 Phase 4
NCT03960606 Terminated Combination Product: PUR1900 Asthma Pulmatrix Inc. July 31 2019 Phase 2

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.

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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.

Hedgehog/Smoothened Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID