Ketoconazole

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.
Targets
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]

Protocol

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]
+ Expand
  • 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
Formula

C26H28Cl2N4O4

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

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.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID