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 NYjKZ41RTnWwY4Tpc44h[XO|YYm= NVrWNnBpUW6qaXLpeIlwdiCxZjDQMYdtgWOxcILveIVqdixiaIXtZY4hVC2PRGKxJIV5eHKnc4Pl[EBqdiCOTFOtVGsyKGWyaYTo[Yxq[WxiY3XscJMhfXOrbnegZ4Ft[2Wrbj3BUUBxd2yjcnnzZZRqd25iYYPzZZktKEmFNUC9OE45KM7:TR?= M3O5VlEzPjl7M{i5
MCF7 cells Ml;1SpVv[3Srb36gZZN{[Xl? M{jlcWlvcGmkaYTpc44hd2ZiQ2nQNlZCOSCrbjDoeY1idiCPQ1[3JINmdGy|IHHzd4V{e2WmIHHzJIFtdC22cnHud{Bz\XSrbn;pZ{Bi[2mmIH3leIFjd2yrc32sJGlEPTB;MUKg{txO NXTkNVRUOTZ{N{m3O|A>
human THP1 cells M3vOSmN6fG:2b4jpZ4l1gSCjc4PhfS=> MnXtOFghcA>? NGfQ[IREgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBVUFBzIHPlcIx{KGGodHXyJFQ5KGi{czygTWM2OD12NDFOwG0> NV\xfIpjOTd7NkC5NlM>
CHO cells NWG1SGh4TnWwY4Tpc44h[XO|YYm= NUjaS|lEUW6qaXLpeIlwdiCxZjDDXXAzPEFzIHX4dJJme3OnZDDpckBEUE9iY3XscJMtKEmFNUC9NE42OiEQvF2= MkW5NlA3PTV4Mk[=
P815B cells MmjCR5l1d3SxeHnjbZR6KGG|c3H5 NUPXfWtVOjRiaB?= M3LHSmN6fG:2b4jpZ4l1gSCjZ3HpcpN1KG2xdYPlJHA5OTWEIHPlcIx{KGGodHXyJFI1KGi{czDifUBOXFNxUF3TJIF{e2G7LDDMSFUxRTJ3IN88US=> Mm\0NlUxOzZ5OEm=
V79 11B2 cells NHrjc2JHfW6ldHnvckBie3OjeR?= MUXJcohq[mm2aX;uJI9nKGi3bXHuJGN[WDFzQkKg[ZhxemW|c3XkJIlvKFZ5OTCxNWIzKGOnbHzzMEBKSzVyPUCuNFgyKM7:TR?= MVixOlU4ODlzOB?=
V79 cells NGmydVRHfW6ldHnvckBie3OjeR?= M1vwS2lvcGmkaYTpc44hd2ZiaIXtZY4hS1mSMkSgbJllem:6eXzhd4Uh\XiycnXzd4VlKGmwIG[3PUBk\WyuczygTWM2OD1yLkOxNkDPxE1? MUixOVYyPTV|NB?=
hamster V79MZh11B1 cells MWDGeY5kfGmxbjDhd5NigQ>? NWftVItJUW6qaXLpeIlwdiCxZjDoeY1idiCFWWCxNWIyKGW6cILld5Nm\CCrbjDoZY1{fGW{IG[3PW1bcDFzQkGgZ4VtdHNuIFnDOVA:OC5zMkeg{txO Ml[yNVg3PzJ6Nki=
hamster V79MZh11B2 cells M4fITGZ2dmO2aX;uJIF{e2G7 MX3Jcohq[mm2aX;uJI9nKGi3bXHuJGN[WDFzQkKg[ZhxemW|c3XkJIlvKGijbYP0[ZIhXjd7TWroNVFDOiClZXzsd{whUUN3ME2wMlA3PyEQvF2= M2i4VlE5Pjd{OE[4
CHO cells M1e4O2Z2dmO2aX;uJIF{e2G7 M4\NVWlvcGmkaYTpc44hd2ZiaIXtZY4hTVKJIHX4dJJme3OnZDDpckBEUE9iY3XscJMh[nlid3jvcIUh[2WubDDwZZRkcCClbHHtdEB1\WOqbnnxeYUtKEmFNUC9NU46ODV2NjFOwG0> MVWxPFQ1QDN2Mh?=
V79 11B1 cells NUi3OlQxTnWwY4Tpc44h[XO|YYm= Mn\4TY5pcWKrdHnvckBw\iCqdX3hckBEYVBzMVKxJIV5eHKnc4Pl[EBqdiCYN{mgNVFDOSClZXzsd{whUUN3ME2wMlIzPCEQvF2= M3HpWVE3PTdyOUG4
Topp 3 cells NGjhVFFHfW6ldHnvckBie3OjeR?= NX3SdmQ6UW6qaXLpeIlwdiCxZjDoeY1idiCFWWC1NUBmgHC{ZYPz[YQhcW5iVH;wdEA{KGOnbHzzJIJ6KGyjbn;zeIVzd2xiZHXt[ZRpgWyjc3WgZZN{[XluIFnDOVA:OC5zOTFOwG0> NHXyNZoyPzF7NEexOi=>
V79 cells NH:wNmVHfW6ldHnvckBie3OjeR?= NEPJOI9KdmirYnn0bY9vKG:oIHj1cYFvKEO\UEK0RVEh\XiycnXzd4VlKGmwIHPobY5me2ViaHHtd5RmeiCYN{mgZ4VtdHNuIFnDOVA:OC5|MUKg{txO M{joelIxPTl2OE[y
V79MZ cells NH3E[WRHfW6ldHnvckBie3OjeR?= M1jTTWlvcGmkaYTpc44hd2ZiaIXtZY4hS1mSMUHCNkBmgHC{ZYPz[YQhcW5iaHHtd5RmeiCYN{nNXkBk\WyuczD1d4lv\yBzMT3k[Y95gWOxcoTpZ49{fGW{b37lJJN2[nO2cnH0[UwhUUN3ME2wMlA3PyEQvF2= M1uze|I1QTByMkS3
V79MZh cells MnXUSpVv[3Srb36gZZN{[Xl? NE\OWHhKdmirYnn0bY9vKG:oIHj1cYFvKEO\UEGxRlIh\XiycnXzd4VlKGmwIHjhcZN1\XJiVke5UXppKGOnbHzzMEBKSzVyPUCuNFY4KM7:TR?= MX6yNFU2ODFzOB?=
human epidermal keratinocytes M17XfGZ2dmO2aX;uJIF{e2G7 M{C4V2lvcGmkaYTpc44hd2ZiQ2nQNlRCOSCrbjDoeY1idiCncHnk[ZJu[Wxia3XyZZRqdm:leYTld{whUUN3ME2wMlEzPiEQvF2= M4fxb|IxPTl2OE[y
V79MZh cells MomwSpVv[3Srb36gZZN{[Xl? M{\1WWlvcGmkaYTpc44hd2ZiaIXtZY4hS1mSMUHCNUBmgHC{ZYPz[YQhcW5iaHHtd5RmeiCYN{nNXogh[2WubIOsJGlEPTB;MD6xNlch|ryP M1rLbFIxPTVyMUG4

... 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(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
Formula

C26H28Cl2N4O4

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

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02147964 Not yet recruiting Gonadotropin Deficiency University of Washington June 2019 Phase 2
NCT02147964 Not yet recruiting Gonadotropin Deficiency University of Washington June 2019 Phase 2
NCT03845348 Not yet recruiting Scalp Dermatitis Sunstar Joint Stock Company|Big Leap Clinical Research Support Joint Stock Company April 1 2019 Phase 3
NCT03845348 Not yet recruiting Scalp Dermatitis Sunstar Joint Stock Company|Big Leap Clinical Research Support Joint Stock Company April 1 2019 Phase 3
NCT03796273 Recruiting 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
NCT03796273 Recruiting 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

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID