Catalog No.S1353

Ketoconazole Chemical Structure

Molecular Weight(MW): 531.43

Ketoconazole inhibits cyclosporine oxidase and testosterone 6 beta-hydroxylase with IC50 of 0.19 mM and 0.22 mM, respectively.

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Biological Activity

Description Ketoconazole inhibits cyclosporine oxidase and testosterone 6 beta-hydroxylase with IC50 of 0.19 mM and 0.22 mM, respectively.
Features More active than both Econazole and Miconazole against Malassezia species.
Cyclosporine oxidase [1] Testosterone 6 beta-hydroxylase [1]
0.19 mM 0.22 mM
In vitro

Ketoconazole interacts with androgen receptors in a competitive fashion in intact human foreskin fibroblasts. Ketoconazole competes for [3H]dexamethasone binding to fibroblast glucocorticoid receptors with IC50 of 0.3 mM. [2] Ketoconazole reduces cell proliferation and [3H]thymidine incorporation with IC50 of 2.5 mM in the serum independent HT29-S-B6 colon cell clone. Ketoconazole inhibits the incorporation of [3H]thymidine with IC50 of 2 μM and 13 μM in the Evsa-T cell line and MDA-MB-231 cell line, respectively. Ketoconazole induces a decrease of the number of cells in S phase and a corresponding increase of the percentage of cells in Go-G1 in HT29-S-B6 cells. [3] Ketoconazole is susceptable to several Malassezia species with minimum inhibitory concentrations (MICs) of 0.03 µg/mL. [4]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
LLC-PK1 epithelial cells NFKweFhHfW6ldHnvckBie3OjeR?= MU\Jcohq[mm2aX;uJI9nKFBvZ3z5Z49xem:2ZXnuMEBpfW2jbjDMMW1FWjFiZYjwdoV{e2WmIHnuJGxNSy2SS{Gg[ZBqfGinbHnhcEBk\WyuczD1d4lv\yClYXzj[YlvNUGPIIDvcIFzcXOjdHnvckBie3OjeTygTWM2OD12Lkig{txO Mmf0NVI3QTl|OEm=
MCF7 cells NYPUfGpLTnWwY4Tpc44h[XO|YYm= NUCwOXRpUW6qaXLpeIlwdiCxZjDDXXAzPkFzIHnuJIh2dWGwIF3DSlch[2WubIOgZZN{\XO|ZXSgZZMh[WyuLYTyZY5{KHKndHnuc4lkKGGlaXSgcYV1[WKxbHnzcUwhUUN3ME2xNkDPxE1? Mn7QNVYzPzl5N{C=
human THP1 cells NHTVRppEgXSxdH;4bYNqfHliYYPzZZk> NGrPV|M1QCCq NXT6UIR7S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hXEiSMTDj[YxteyCjZoTldkA1QCCqcoOsJGlEPTB;NESg{txO MWWxO|k3ODl{Mx?=
CHO cells NF3lV2NHfW6ldHnvckBie3OjeR?= NYXaVmlZUW6qaXLpeIlwdiCxZjDDXXAzPEFzIHX4dJJme3OnZDDpckBEUE9iY3XscJMtKEmFNUC9NE42OiEQvF2= MlnxNlA3PTV4Mk[=
P815B cells NW\oXolqS3m2b4TvfIlkcXS7IHHzd4F6 M4r6VFI1KGh? NHzNR5ZEgXSxdH;4bYNqfHliYXfhbY5{fCCvb4Xz[UBRQDF3QjDj[YxteyCjZoTldkAzPCCqcoOgZpkhVVSVL2DNV{Bie3OjeTygUGQ2OD1{NTFOwG0> NWS2V5c{OjVyM{[3PFk>
V79 11B2 cells NHfOR|hHfW6ldHnvckBie3OjeR?= M2jzdGlvcGmkaYTpc44hd2ZiaIXtZY4hS1mSMUHCNkBmgHC{ZYPz[YQhcW5iVke5JFEySjJiY3XscJMtKEmFNUC9NE4xQDFizszN NFL0fJQyPjV5MEmxPC=>
V79 cells MmDzSpVv[3Srb36gZZN{[Xl? M17JW2lvcGmkaYTpc44hd2ZiaIXtZY4hS1mSMkSgbJllem:6eXzhd4Uh\XiycnXzd4VlKGmwIG[3PUBk\WyuczygTWM2OD1yLkOxNkDPxE1? NFPpbVgyPTZzNUWzOC=>
hamster V79MZh11B1 cells NFrTUJFHfW6ldHnvckBie3OjeR?= MmfRTY5pcWKrdHnvckBw\iCqdX3hckBEYVBzMVKxJIV5eHKnc4Pl[EBqdiCqYX3zeIVzKFZ5OV3abFEySjFiY3XscJMtKEmFNUC9NE4yOjdizszN NUnEd3p7OTh4N{K4Olg>
hamster V79MZh11B2 cells NEXCcFhHfW6ldHnvckBie3OjeR?= NYTOTm13UW6qaXLpeIlwdiCxZjDoeY1idiCFWWCxNWIzKGW6cILld5Nm\CCrbjDoZY1{fGW{IG[3PW1bcDFzQkKgZ4VtdHNuIFnDOVA:OC5yNkeg{txO M4\2bVE5Pjd{OE[4
CHO cells MnjBSpVv[3Srb36gZZN{[Xl? M1\2cWlvcGmkaYTpc44hd2ZiaIXtZY4hTVKJIHX4dJJme3OnZDDpckBEUE9iY3XscJMh[nlid3jvcIUh[2WubDDwZZRkcCClbHHtdEB1\WOqbnnxeYUtKEmFNUC9NU46ODV2NjFOwG0> MVKxPFQ1QDN2Mh?=
V79 11B1 cells M1:zcmZ2dmO2aX;uJIF{e2G7 NYW0d3puUW6qaXLpeIlwdiCxZjDoeY1idiCFWWCxNWIyKGW6cILld5Nm\CCrbjDWO|khOTGEMTDj[YxteyxiSVO1NF0xNjJ{NDFOwG0> M{nHcFE3PTdyOUG4
Topp 3 cells NXnyfW5iTnWwY4Tpc44h[XO|YYm= NWfC[XZOUW6qaXLpeIlwdiCxZjDoeY1idiCFWWC1NUBmgHC{ZYPz[YQhcW5iVH;wdEA{KGOnbHzzJIJ6KGyjbn;zeIVzd2xiZHXt[ZRpgWyjc3WgZZN{[XluIFnDOVA:OC5zOTFOwG0> MYOxO|E6PDdzNh?=
V79 cells MkPjSpVv[3Srb36gZZN{[Xl? NXr0OpVHUW6qaXLpeIlwdiCxZjDoeY1idiCFWWCyOGEyKGW6cILld5Nm\CCrbjDjbIlv\XOnIHjhcZN1\XJiVke5JINmdGy|LDDJR|UxRTBwM{GyJO69VQ>? NYrNNWlROjB3OUS4OlI>
V79MZ cells NFvJfpBHfW6ldHnvckBie3OjeR?= NIm2T3RKdmirYnn0bY9vKG:oIHj1cYFvKEO\UEGxRlIh\XiycnXzd4VlKGmwIHjhcZN1\XJiVke5UXoh[2WubIOgeZNqdmdiMUGt[IVwgHmlb4L0bYNwe3Sncn;u[UB{fWK|dILheIUtKEmFNUC9NE4xPjdizszN MomyNlQ6ODB{NEe=
V79MZh cells M2m3V2Z2dmO2aX;uJIF{e2G7 NXy4W2p6UW6qaXLpeIlwdiCxZjDoeY1idiCFWWCxNWIzKGW6cILld5Nm\CCrbjDoZY1{fGW{IG[3PW1bcCClZXzsd{whUUN3ME2wMlA3PyEQvF2= NFfW[IUzODV3MEGxPC=>
human epidermal keratinocytes MVrGeY5kfGmxbjDhd5NigQ>? NV7PVJAxUW6qaXLpeIlwdiCxZjDDXXAzPEFzIHnuJIh2dWGwIHXwbYRmem2jbDDr[ZJifGmwb3P5eIV{NCCLQ{WwQVAvOTJ4IN88US=> NFrO[JEzODV7NEi2Ni=>
V79MZh cells NXHoZmlETnWwY4Tpc44h[XO|YYm= NEX4dVRKdmirYnn0bY9vKG:oIHj1cYFvKEO\UEGxRlEh\XiycnXzd4VlKGmwIHjhcZN1\XJiVke5UXppKGOnbHzzMEBKSzVyPUCuNVI4KM7:TR?= MlTONlA2PTBzMUi=

... Click to View More Cell Line Experimental Data

In vivo Ketoconazole (25 mg/kg, i.p.) significantly decreases plasma corticosterone and reduces low dose cocaine self-administration without affecting food-reinforced responding in rats. [5] Ketoconazole raises the AUC of orally administered digoxin from 63 mg x h/L to 411 mg x h/L in rats. Ketoconazole raises the AUC of intravenously administered digoxin from 93 mg × h/L to 486 mg × h/L in rats. Ketoconazole increases digoxin bioavailability from 0.68 to 0.84 in rats, while mean absorption time is reduced from 1.1 hours to 0.3 hour. [6]


Kinase Assay:[1]
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Whole Cell [3H]R1881 Binding Assay:

Fibroblasts are grown to confluence in five or six 150 cm2 tissue culture flasks for routine assay. This usually requires 4-6 weeks from the time of the initial seeding of the cell line. All studies are performed between passages 3-20. Two days before assay, the medium is changed to one lacking fetal calf serum. This is repeated again 24 hours before assay. Competition assays are performed with 0.5-1.0 nM [3H]R1881 and increasing amounts of the nonradioactive compounds. Binding to low affinity sites is determined in the presence of 5 × 10-7 M R1881 and is subtracted from whole cell binding of [3H]R 1881 obtained in the absence of any inhibitor to assess binding to 5 high affinity site
Cell Research:[3]
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  • Cell lines: HT29-S-B6 colon cell
  • Concentrations: 25 μM
  • Incubation Time: 72 hours
  • Method: HT29-S-B6 cells (5×105) are plated in 35-mm Petri dishes. The next day, the medium is changed and effectors are added in a small volume (10-20 μL). The incubation medium is renewed every day during the experiments. The same triplicate dishes are used for cell counts, [3H]thymidine incorporation, and flow cytometry. [3H]Thymidine (0.5 μCi) is allowed to incorporate for 24 hours; at the end of incubation, cells are rinsed with 1 mL of medium, detached with 1 mL of trypsin-EDTA, and diluted (1:3) with the culture medium. An aliquot (0.5-1 mL) is used for cell count with a Coulter Counter.
    (Only for Reference)
Animal Research:[4]
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  • Animal Models: male Wistar rats
  • Formulation: Saline
  • Dosages: 25 mg/kg
  • Administration: Intraperitoneal injection
    (Only for Reference)

Solubility (25°C)

In vitro Ethanol 7 mg/mL (13.17 mM)
DMSO 5 mg/mL warmed (9.4 mM)
Water Insoluble
In vivo Add solvents to the product individually and in order:
30% propylene glycol, 5% Tween 80, 65% D5W
For best results, use promptly after mixing.
30 mg/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 531.43


CAS No. 65277-42-1
Storage powder
Synonyms N/A

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02582177 Not yet recruiting Tinea Ache Laboratorios Farmaceuticos S.A. August 2017 Phase 3
NCT02147964 Not yet recruiting Gonadotropin Deficiency University of Washington January 2017 Phase 2
NCT02606383 Withdrawn Tinea Pedis Biolab Sanus Farmaceutica June 2016 Phase 3
NCT02560051 Recruiting Prostatic Neoplasms The University of Texas Health Science Center, Houston November 2015 Phase 2
NCT02494713 Recruiting Prostate Cancer The University of Texas Health Science Center, Houston October 2015 Phase 2
NCT02256865 Recruiting Insulin Resistance Los Angeles Biomedical Research Institute October 2014 --

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID