Itraconazole

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.

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1 Customer Review

  • 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.

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Biological Activity

Description Itraconazole is a relatively potent inhibitor of CYP3A4 with IC50 of 6.1 nM, used as a triazole antifungal agent.
Targets
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 MlvxSpVv[3Srb36gZZN{[Xl? NHnOdpBKdmirYnn0bY9vKG:oIFPZVFNCPCCrbjDoeY1idiCqZYDheI9kgXSnczD1d4lv\yC2ZYP0c5N1\XKxbnWgZZMhe3Wkc4TyZZRmKGK7IFjQUGMwVVNxTWOgcYV1cG:mLDDJR|UxRTBwMEeg{txO NFntVZczPDl2OEW2OS=>
human HTLA cells MXrGeY5kfGmxbjDhd5NigQ>? MkXMNlAhdWmwcx?= NVu0Z5Z4UW6qaXLpeIlwdiCxZjDDXFNEVDFvc4TpcZVt[XSnZDDDXFNEWjFiaX6gbJVu[W5iSGTMRUBk\WyuczDwdoUucW6ldXLheIVlKG[xcjCyNEBucW6|IH3lZZN2emWmIH;uJIRigSB2IHL5JIJmfGFiYYLy[ZN1cW5vcnXjdpVqfG2nboSgcYVlcWG2ZXSgcJVkcW[ncnHz[UBz\XCxcoTldkBo\W6nIHHzd4F6NCCLQ{WwQVAvOSEQvF2= M3HZRlI{PDN5N{ey
LLC-PK1 epithelial cells MlvoSpVv[3Srb36gZZN{[Xl? NX\hV2RpUW6qaXLpeIlwdiCxZjDQMYdtgWOxcILveIVqdixibX;1d4UhVC2vZIKxZUBmgHC{ZYPz[YQhcW5iTFzDMXBMOSCncHn0bIVtcWGuIHPlcIx{KHW|aX7nJINidGOnaX6tRW0heG:uYYLpd4F1cW:wIHHzd4F6NCCLQ{WwQVAvOiEQvF2= NFLvfWQyOjZ7OUO4PS=>
human PBMC NEXMWZpEgXSxdH;4bYNqfHliYYPzZZk> MYC3NkBp NHnGeo5EgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBRSk2FIHHzd4V{e2WmIHHzJINmdGxidnnhZoltcXS7IHHmeIVzKDd{IHjyd{BjgSCPVGSgZZN{[XluIFnDOVA:OS53MzFOwG0> NI[4e|AzPDR6NUe4Ny=>
Topp 3 cells NWfRbWh{TnWwY4Tpc44h[XO|YYm= M3jUbmlvcGmkaYTpc44hd2ZiaIXtZY4hS1mSNUGg[ZhxemW|c3XkJIlvKFSxcICgN{Bk\WyuczDifUBt[W6xc4Tldo9tKGSnbXX0bJlt[XOnIHHzd4F6NCCLQ{WwQVMvPiEQvF2= NXHCbmltOTdzOUS3NVY>
human MRC5 cells MV;DfZRwfG:6aXPpeJkh[XO|YYm= NWH1c3VwS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hVVKFNTDj[YxteyxiQ1O1NF01QS5|MzFOwG0> MXeyNFgxPTN7OB?=
human HUVEC cells NIDPOGRHfW6ldHnvckBie3OjeR?= NYnvfZF[OiEQvF2= M1TrclI1KGh? MkHFTY5pcWKrdHnvckBw\iCYRVfGVlIh\2y7Y3;zfYxifGmxbjDpckBpfW2jbjDIWXZGSyClZXzsd{BifCB{IIXNJIFnfGW{IEK0JIhzeyCkeTDX[ZN1\XKwIHLsc5Qh[W6jbInzbZM> NWLn[XZOOjF7M{[1NVQ>

... 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]

Protocol

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.
9mg/mL

* 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
Formula

C35H38Cl2N8O4

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

Bio Calculators

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03479411 Completed Asthma Pulmatrix Inc. February 9 2018 Phase 1
NCT03535662 Completed Pharmacokinetic Study in Healthy Male Volunteers Nerre Therapeutics Ltd. June 8 2018 Phase 1
NCT03121664 Completed Healthy Pfizer April 7 2017 Phase 1
NCT03077607 Completed Advanced Solid Tumors Pfizer|Medivation Inc. November 7 2016 Phase 1
NCT02354261 Active not recruiting Basal Cell Carcinoma in Basal Cell Nevus Syndrome HedgePath Pharmaceuticals Inc. August 7 2015 Phase 2
NCT02157883 Active not recruiting Advanced Non Small Cell Lung Cancer|Advanced (Inoperable) Non Small Cell Lung Cancer AstraZeneca November 6 2014 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

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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.

P450 (e.g. CYP17) Signaling Pathway Map

Related P450 (e.g. CYP17) Products

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID