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 MXLGeY5kfGmxbjDhd5NigQ>? MlXtTY5pcWKrdHnvckBw\iCSLXfsfYNweHKxdHXpckwhcHWvYX6gUE1OTFJzIHX4dJJme3OnZDDpckBNVENvUFuxJIVxcXSqZXzpZYwh[2WubIOgeZNqdmdiY3HsZ4Vqdi2DTTDwc4xiemm|YYTpc44h[XO|YYmsJGlEPTB;ND64JO69VQ>? NIfIXWQyOjZ7OUO4PS=>
MCF7 cells MkfoSpVv[3Srb36gZZN{[Xl? MVTJcohq[mm2aX;uJI9nKEO\UEK2RVEhcW5iaIXtZY4hVUOINzDj[YxteyCjc4Pld5Nm\CCjczDhcIwufHKjboOgdoV1cW6xaXOgZYNq\CCvZYThZo9tcXOvLDDJR|UxRTF{IN88US=> M13CTVE3Ojd7N{ew
human THP1 cells M2qyemN6fG:2b4jpZ4l1gSCjc4PhfS=> NV60eZdDPDhiaB?= NYrWbWJCS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hXEiSMTDj[YxteyCjZoTldkA1QCCqcoOsJGlEPTB;NESg{txO NIfCcnUyPzl4MEmyNy=>
CHO cells M3nrNWZ2dmO2aX;uJIF{e2G7 NY[zUoVlUW6qaXLpeIlwdiCxZjDDXXAzPEFzIHX4dJJme3OnZDDpckBEUE9iY3XscJMtKEmFNUC9NE42OiEQvF2= MkHkNlA3PTV4Mk[=
P815B cells NXnXR3E{S3m2b4TvfIlkcXS7IHHzd4F6 MnPLNlQhcA>? MV7DfZRwfG:6aXPpeJkh[WejaX7zeEBud3W|ZTDQPFE2SiClZXzsd{Bi\nSncjCyOEBpenNiYomgUXRUN1CPUzDhd5NigSxiTFS1NF0zPSEQvF2= MVGyOVA{Pjd6OR?=
V79 11B2 cells NXHoSoJ1TnWwY4Tpc44h[XO|YYm= M3jWXmlvcGmkaYTpc44hd2ZiaIXtZY4hS1mSMUHCNkBmgHC{ZYPz[YQhcW5iVke5JFEySjJiY3XscJMtKEmFNUC9NE4xQDFizszN MVKxOlU4ODlzOB?=
V79 cells NYPQTHF7TnWwY4Tpc44h[XO|YYm= Mn2zTY5pcWKrdHnvckBw\iCqdX3hckBEYVB{NDDofYRzd3i7bHHz[UBmgHC{ZYPz[YQhcW5iVke5JINmdGy|LDDJR|UxRTBwM{GyJO69VQ>? MWixOVYyPTV|NB?=
hamster V79MZh11B1 cells NFvz[YlHfW6ldHnvckBie3OjeR?= MmiyTY5pcWKrdHnvckBw\iCqdX3hckBEYVBzMVKxJIV5eHKnc4Pl[EBqdiCqYX3zeIVzKFZ5OV3abFEySjFiY3XscJMtKEmFNUC9NE4yOjdizszN NIrpPGoyQDZ5Mki2PC=>
hamster V79MZh11B2 cells MYrGeY5kfGmxbjDhd5NigQ>? M4HMOWlvcGmkaYTpc44hd2ZiaIXtZY4hS1mSMUHCNkBmgHC{ZYPz[YQhcW5iaHHtd5RmeiCYN{nNXogyOUJ{IHPlcIx{NCCLQ{WwQVAvODZ5IN88US=> M2r5ZlE5Pjd{OE[4
CHO cells MojSSpVv[3Srb36gZZN{[Xl? Ml[0TY5pcWKrdHnvckBw\iCqdX3hckBGWkdiZYjwdoV{e2WmIHnuJGNJVyClZXzsd{BjgSC5aH;s[UBk\WyuIIDheINpKGOuYX3wJJRm[2iwaYH1[UwhUUN3ME2xMlkxPTR4IN88US=> NEC4WlQyQDR2OEO0Ni=>
V79 11B1 cells NF:4[5pHfW6ldHnvckBie3OjeR?= MmG4TY5pcWKrdHnvckBw\iCqdX3hckBEYVBzMVKxJIV5eHKnc4Pl[EBqdiCYN{mgNVFDOSClZXzsd{whUUN3ME2wMlIzPCEQvF2= MXGxOlU4ODlzOB?=
Topp 3 cells Mn;GSpVv[3Srb36gZZN{[Xl? NHyyWVBKdmirYnn0bY9vKG:oIHj1cYFvKEO\UEWxJIV5eHKnc4Pl[EBqdiCWb4DwJFMh[2WubIOgZpkhdGGwb4P0[ZJwdCCmZX3leIh6dGG|ZTDhd5NigSxiSVO1NF0xNjF7IN88US=> NGD3U3oyPzF7NEexOi=>
V79 cells NFPTclVHfW6ldHnvckBie3OjeR?= MmC2TY5pcWKrdHnvckBw\iCqdX3hckBEYVB{NFGxJIV5eHKnc4Pl[EBqdiClaHnu[ZNmKGijbYP0[ZIhXjd7IHPlcIx{NCCLQ{WwQVAvOzF{IN88US=> M37nOVIxPTl2OE[y
V79MZ cells Ml\ESpVv[3Srb36gZZN{[Xl? M1O3UWlvcGmkaYTpc44hd2ZiaIXtZY4hS1mSMUHCNkBmgHC{ZYPz[YQhcW5iaHHtd5RmeiCYN{nNXkBk\WyuczD1d4lv\yBzMT3k[Y95gWOxcoTpZ49{fGW{b37lJJN2[nO2cnH0[UwhUUN3ME2wMlA3PyEQvF2= MVWyOFkxODJ2Nx?=
V79MZh cells M1:wWGZ2dmO2aX;uJIF{e2G7 NUjtXVZvUW6qaXLpeIlwdiCxZjDoeY1idiCFWWCxNWIzKGW6cILld5Nm\CCrbjDoZY1{fGW{IG[3PW1bcCClZXzsd{whUUN3ME2wMlA3PyEQvF2= MkLCNlA2PTBzMUi=
human epidermal keratinocytes NFf6SY1HfW6ldHnvckBie3OjeR?= MlXMTY5pcWKrdHnvckBw\iCFWWCyOGEyKGmwIHj1cYFvKGWyaXTldo1idCCtZYLheIlvd2O7dHXzMEBKSzVyPUCuNVI3KM7:TR?= M37Ne|IxPTl2OE[y
V79MZh cells NGDkOFFHfW6ldHnvckBie3OjeR?= MonrTY5pcWKrdHnvckBw\iCqdX3hckBEYVBzMVKxJIV5eHKnc4Pl[EBqdiCqYX3zeIVzKFZ5OV3abEBk\WyuczygTWM2OD1yLkGyO{DPxE1? MoXqNlA2PTBzMUi=

... 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 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 --

Tech Support

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID