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 MnPOSpVv[3Srb36gZZN{[Xl? M1;zZWlvcGmkaYTpc44hd2ZiUD3ncJlkd3C{b4TlbY4tKGi3bXHuJGwuVUSUMTDlfJBz\XO|ZXSgbY4hVEyFLWDLNUBmeGm2aHXsbYFtKGOnbHzzJJV{cW6pIHPhcINmcW5vQV2gdI9t[XKrc3H0bY9vKGG|c3H5MEBKSzVyPUSuPEDPxE1? MWOxNlY6QTN6OR?=
MCF7 cells NInUUY9HfW6ldHnvckBie3OjeR?= MnqxTY5pcWKrdHnvckBw\iCFWWCyOmEyKGmwIHj1cYFvKE2FRkegZ4VtdHNiYYPz[ZN{\WRiYYOgZYxtNXS{YX7zJJJmfGmwb3njJIFkcWRibXX0ZYJwdGm|bTygTWM2OD1zMjFOwG0> NYGwVXJOOTZ{N{m3O|A>
human THP1 cells MlrUR5l1d3SxeHnjbZR6KGG|c3H5 NEHGXGc1QCCq Mn6xR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gWGhROSClZXzsd{Bi\nSncjC0PEBpenNuIFnDOVA:PDRizszN NFKzb24yPzl4MEmyNy=>
CHO cells MknsSpVv[3Srb36gZZN{[Xl? MkKyTY5pcWKrdHnvckBw\iCFWWCyOGEyKGW6cILld5Nm\CCrbjDDTG8h[2WubIOsJGlEPTB;MD61NkDPxE1? MkSzNlA3PTV4Mk[=
P815B cells MlL0R5l1d3SxeHnjbZR6KGG|c3H5 MlvyNlQhcA>? NWjhb4tGS3m2b4TvfIlkcXS7IHHnZYlve3RibX;1d4UhWDhzNVKgZ4VtdHNiYX\0[ZIhOjRiaILzJIJ6KE2WUz;QUXMh[XO|YYmsJGxFPTB;MkWg{txO MV[yOVA{Pjd6OR?=
V79 11B2 cells MUnGeY5kfGmxbjDhd5NigQ>? NXP4TYpxUW6qaXLpeIlwdiCxZjDoeY1idiCFWWCxNWIzKGW6cILld5Nm\CCrbjDWO|khOTGEMjDj[YxteyxiSVO1NF0xNjB6MTFOwG0> NU\zUFl{OTZ3N{C5NVg>
V79 cells MYjGeY5kfGmxbjDhd5NigQ>? NFK3dHVKdmirYnn0bY9vKG:oIHj1cYFvKEO\UEK0JIh6\HKxeInsZZNmKGW6cILld5Nm\CCrbjDWO|kh[2WubIOsJGlEPTB;MD6zNVIh|ryP MnrlNVU3OTV3M{S=
hamster V79MZh11B1 cells NH7vT45HfW6ldHnvckBie3OjeR?= M2O4O2lvcGmkaYTpc44hd2ZiaIXtZY4hS1mSMUHCNUBmgHC{ZYPz[YQhcW5iaHHtd5RmeiCYN{nNXogyOUJzIHPlcIx{NCCLQ{WwQVAvOTJ5IN88US=> NGDpT5kyQDZ5Mki2PC=>
hamster V79MZh11B2 cells MnTFSpVv[3Srb36gZZN{[Xl? M3;WXGlvcGmkaYTpc44hd2ZiaIXtZY4hS1mSMUHCNkBmgHC{ZYPz[YQhcW5iaHHtd5RmeiCYN{nNXogyOUJ{IHPlcIx{NCCLQ{WwQVAvODZ5IN88US=> MlXiNVg3PzJ6Nki=
CHO cells NY\YWm94TnWwY4Tpc44h[XO|YYm= NVnzO5c2UW6qaXLpeIlwdiCxZjDoeY1idiCHUleg[ZhxemW|c3XkJIlvKEOKTzDj[YxteyCkeTD3bI9t\SClZXzsJJBifGOqIHPsZY1xKHSnY3jubZF2\SxiSVO1NF0yNjlyNUS2JO69VQ>? MVOxPFQ1QDN2Mh?=
V79 11B1 cells NF7sTpVHfW6ldHnvckBie3OjeR?= M2fPcmlvcGmkaYTpc44hd2ZiaIXtZY4hS1mSMUHCNUBmgHC{ZYPz[YQhcW5iVke5JFEySjFiY3XscJMtKEmFNUC9NE4zOjRizszN MXqxOlU4ODlzOB?=
Topp 3 cells MVnGeY5kfGmxbjDhd5NigQ>? NXjEUHZTUW6qaXLpeIlwdiCxZjDoeY1idiCFWWC1NUBmgHC{ZYPz[YQhcW5iVH;wdEA{KGOnbHzzJIJ6KGyjbn;zeIVzd2xiZHXt[ZRpgWyjc3WgZZN{[XluIFnDOVA:OC5zOTFOwG0> MmO3NVcyQTR5MU[=
V79 cells NX;iOlhnTnWwY4Tpc44h[XO|YYm= MYfJcohq[mm2aX;uJI9nKGi3bXHuJGN[WDJ2QUGg[ZhxemW|c3XkJIlvKGOqaX7ld4UhcGGvc4TldkBXPzliY3XscJMtKEmFNUC9NE4{OTJizszN MYiyNFU6PDh4Mh?=
V79MZ cells MnO0SpVv[3Srb36gZZN{[Xl? M3XyR2lvcGmkaYTpc44hd2ZiaIXtZY4hS1mSMUHCNkBmgHC{ZYPz[YQhcW5iaHHtd5RmeiCYN{nNXkBk\WyuczD1d4lv\yBzMT3k[Y95gWOxcoTpZ49{fGW{b37lJJN2[nO2cnH0[UwhUUN3ME2wMlA3PyEQvF2= NGrWZYozPDlyMEK0Oy=>
V79MZh cells NIXqO2NHfW6ldHnvckBie3OjeR?= MoHBTY5pcWKrdHnvckBw\iCqdX3hckBEYVBzMVKyJIV5eHKnc4Pl[EBqdiCqYX3zeIVzKFZ5OV3abEBk\WyuczygTWM2OD1yLkC2O{DPxE1? MmH3NlA2PTBzMUi=
human epidermal keratinocytes NFnCUWxHfW6ldHnvckBie3OjeR?= NFOzfnBKdmirYnn0bY9vKG:oIFPZVFI1STFiaX6gbJVu[W5iZYDp[IVzdWGuIHvldoF1cW6xY4n0[ZMtKEmFNUC9NE4yOjZizszN NXT6TZdGOjB3OUS4OlI>
V79MZh cells NWjFXVdWTnWwY4Tpc44h[XO|YYm= NV7mO2JjUW6qaXLpeIlwdiCxZjDoeY1idiCFWWCxNWIyKGW6cILld5Nm\CCrbjDoZY1{fGW{IG[3PW1bcCClZXzsd{whUUN3ME2wMlEzPyEQvF2= NXGzcIV6OjB3NUCxNVg>

... 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
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