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 MnX5SpVv[3Srb36gZZN{[Xl? M3HMeGlvcGmkaYTpc44hd2ZiUD3ncJlkd3C{b4TlbY4tKGi3bXHuJGwuVUSUMTDlfJBz\XO|ZXSgbY4hVEyFLWDLNUBmeGm2aHXsbYFtKGOnbHzzJJV{cW6pIHPhcINmcW5vQV2gdI9t[XKrc3H0bY9vKGG|c3H5MEBKSzVyPUSuPEDPxE1? MVuxNlY6QTN6OR?=
MCF7 cells MXHGeY5kfGmxbjDhd5NigQ>? NH\Md5hKdmirYnn0bY9vKG:oIFPZVFI3STFiaX6gbJVu[W5iTVPGO{Bk\WyuczDhd5Nme3OnZDDhd{BidGxvdILhcpMhemW2aX7vbYMh[WOrZDDt[ZRi[m:uaYPtMEBKSzVyPUGyJO69VQ>? NWKxd2tLOTZ{N{m3O|A>
human THP1 cells MVjDfZRwfG:6aXPpeJkh[XO|YYm= NG[zdoU1QCCq NIjSd29EgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBVUFBzIHPlcIx{KGGodHXyJFQ5KGi{czygTWM2OD12NDFOwG0> NW\TZ4ZQOTd7NkC5NlM>
CHO cells MXTGeY5kfGmxbjDhd5NigQ>? MV\Jcohq[mm2aX;uJI9nKEO\UEK0RVEh\XiycnXzd4VlKGmwIFPIU{Bk\WyuczygTWM2OD1yLkWyJO69VQ>? NY\KNmpyOjB4NUW2NlY>
P815B cells NXfxPWM1S3m2b4TvfIlkcXS7IHHzd4F6 NVntPZU6OjRiaB?= MmjpR5l1d3SxeHnjbZR6KGGpYXnud5QhdW:3c3WgVFgyPUJiY3XscJMh[W[2ZYKgNlQhcHK|IHL5JG1VWy:STWOgZZN{[XluIFzEOVA:OjVizszN NUi5b2pvOjVyM{[3PFk>
V79 11B2 cells M1rZT2Z2dmO2aX;uJIF{e2G7 MVzJcohq[mm2aX;uJI9nKGi3bXHuJGN[WDFzQkKg[ZhxemW|c3XkJIlvKFZ5OTCxNWIzKGOnbHzzMEBKSzVyPUCuNFgyKM7:TR?= M4nBdVE3PTdyOUG4
V79 cells M{jtVWZ2dmO2aX;uJIF{e2G7 M{\ke2lvcGmkaYTpc44hd2ZiaIXtZY4hS1mSMkSgbJllem:6eXzhd4Uh\XiycnXzd4VlKGmwIG[3PUBk\WyuczygTWM2OD1yLkOxNkDPxE1? MUKxOVYyPTV|NB?=
hamster V79MZh11B1 cells MkDoSpVv[3Srb36gZZN{[Xl? MkPnTY5pcWKrdHnvckBw\iCqdX3hckBEYVBzMVKxJIV5eHKnc4Pl[EBqdiCqYX3zeIVzKFZ5OV3abFEySjFiY3XscJMtKEmFNUC9NE4yOjdizszN NFK1UogyQDZ5Mki2PC=>
hamster V79MZh11B2 cells M3j0dmZ2dmO2aX;uJIF{e2G7 MVzJcohq[mm2aX;uJI9nKGi3bXHuJGN[WDFzQkKg[ZhxemW|c3XkJIlvKGijbYP0[ZIhXjd7TWroNVFDOiClZXzsd{whUUN3ME2wMlA3PyEQvF2= Mk\iNVg3PzJ6Nki=
CHO cells Ml7YSpVv[3Srb36gZZN{[Xl? MYfJcohq[mm2aX;uJI9nKGi3bXHuJGVTTyCneIDy[ZN{\WRiaX6gR2hQKGOnbHzzJIJ6KHeqb3zlJINmdGxicHH0Z4gh[2yjbYCgeIVkcG6rcYXlMEBKSzVyPUGuPVA2PDZizszN MYCxPFQ1QDN2Mh?=
V79 11B1 cells Ml\GSpVv[3Srb36gZZN{[Xl? M3rtZWlvcGmkaYTpc44hd2ZiaIXtZY4hS1mSMUHCNUBmgHC{ZYPz[YQhcW5iVke5JFEySjFiY3XscJMtKEmFNUC9NE4zOjRizszN MmjLNVY2PzB7MUi=
Topp 3 cells M{KyemZ2dmO2aX;uJIF{e2G7 M4\LOWlvcGmkaYTpc44hd2ZiaIXtZY4hS1mSNUGg[ZhxemW|c3XkJIlvKFSxcICgN{Bk\WyuczDifUBt[W6xc4Tldo9tKGSnbXX0bJlt[XOnIHHzd4F6NCCLQ{WwQVAvOTlizszN MVWxO|E6PDdzNh?=
V79 cells MorCSpVv[3Srb36gZZN{[Xl? M4fqc2lvcGmkaYTpc44hd2ZiaIXtZY4hS1mSMkTBNUBmgHC{ZYPz[YQhcW5iY3jpcoV{\SCqYX3zeIVzKFZ5OTDj[YxteyxiSVO1NF0xNjNzMjFOwG0> M4LqSFIxPTl2OE[y
V79MZ cells NX7QdGxuTnWwY4Tpc44h[XO|YYm= MXPJcohq[mm2aX;uJI9nKGi3bXHuJGN[WDFzQkKg[ZhxemW|c3XkJIlvKGijbYP0[ZIhXjd7TWqgZ4VtdHNidYPpcochOTFvZHXvfJlkd3K2aXPvd5Rmem:wZTDzeYJ{fHKjdHWsJGlEPTB;MD6wOlch|ryP MV2yOFkxODJ2Nx?=
V79MZh cells NVfiOJhkTnWwY4Tpc44h[XO|YYm= MVvJcohq[mm2aX;uJI9nKGi3bXHuJGN[WDFzQkKg[ZhxemW|c3XkJIlvKGijbYP0[ZIhXjd7TWroJINmdGy|LDDJR|UxRTBwME[3JO69VQ>? MkLuNlA2PTBzMUi=
human epidermal keratinocytes NUjsXXRJTnWwY4Tpc44h[XO|YYm= M2ruUGlvcGmkaYTpc44hd2ZiQ2nQNlRCOSCrbjDoeY1idiCncHnk[ZJu[Wxia3XyZZRqdm:leYTld{whUUN3ME2wMlEzPiEQvF2= M{jxVVIxPTl2OE[y
V79MZh cells MYDGeY5kfGmxbjDhd5NigQ>? M1vlb2lvcGmkaYTpc44hd2ZiaIXtZY4hS1mSMUHCNUBmgHC{ZYPz[YQhcW5iaHHtd5RmeiCYN{nNXogh[2WubIOsJGlEPTB;MD6xNlch|ryP MonXNlA2PTBzMUi=

... 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(Data is from Selleck tests instead of citations):
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
in solvent
Synonyms N/A

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03796273 Recruiting Other: Best Practice|Drug: Ketoconazole Anatomic Stage IV Breast Cancer AJCC v8|Astrocytoma|Breast Carcinoma Metastatic in the Brain|Glioma|Invasive Breast Carcinoma|Oligodendroglioma|Prognostic Stage IV Breast Cancer AJCC v8|Recurrent Glioma Wake Forest University Health Sciences|National Cancer Institute (NCI) March 13 2019 Early Phase 1
NCT03473418 Not yet recruiting Drug: Ketoconazole|Drug: Terconazole Vaginal Candidiasis Assiut University April 1 2018 Phase 3
NCT03277690 Recruiting Drug: Levoketoconazole|Drug: Placebo Endogenous Cushing''s Syndrome Cortendo AB September 26 2017 Phase 3
NCT01924299 Completed Drug: Baricitinib|Drug: Ketoconazole|Drug: Fluconazole Healthy Volunteers Eli Lilly and Company August 2013 Phase 1

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID