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 NEfaWXNHfW6ldHnvckBie3OjeR?= Ml32TY5pcWKrdHnvckBw\iCSLXfsfYNweHKxdHXpckwhcHWvYX6gUE1OTFJzIHX4dJJme3OnZDDpckBNVENvUFuxJIVxcXSqZXzpZYwh[2WubIOgeZNqdmdiY3HsZ4Vqdi2DTTDwc4xiemm|YYTpc44h[XO|YYmsJGlEPTB;ND64JO69VQ>? M2fR[|EzPjl7M{i5
MCF7 cells MlfjSpVv[3Srb36gZZN{[Xl? NX7t[np3UW6qaXLpeIlwdiCxZjDDXXAzPkFzIHnuJIh2dWGwIF3DSlch[2WubIOgZZN{\XO|ZXSgZZMh[WyuLYTyZY5{KHKndHnuc4lkKGGlaXSgcYV1[WKxbHnzcUwhUUN3ME2xNkDPxE1? MnTvNVYzPzl5N{C=
human THP1 cells M2TsdGN6fG:2b4jpZ4l1gSCjc4PhfS=> M1nkdVQ5KGh? NHmyOmdEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBVUFBzIHPlcIx{KGGodHXyJFQ5KGi{czygTWM2OD12NDFOwG0> MVGxO|k3ODl{Mx?=
CHO cells MkPDSpVv[3Srb36gZZN{[Xl? NGSwTZNKdmirYnn0bY9vKG:oIFPZVFI1STFiZYjwdoV{e2WmIHnuJGNJVyClZXzsd{whUUN3ME2wMlUzKM7:TR?= M1PHelIxPjV3NkK2
P815B cells MnLBR5l1d3SxeHnjbZR6KGG|c3H5 NXfjbIZYOjRiaB?= Ml;MR5l1d3SxeHnjbZR6KGGpYXnud5QhdW:3c3WgVFgyPUJiY3XscJMh[W[2ZYKgNlQhcHK|IHL5JG1VWy:STWOgZZN{[XluIFzEOVA:OjVizszN NUPyV5k1OjVyM{[3PFk>
V79 11B2 cells NY\YNnJXTnWwY4Tpc44h[XO|YYm= MkXRTY5pcWKrdHnvckBw\iCqdX3hckBEYVBzMVKyJIV5eHKnc4Pl[EBqdiCYN{mgNVFDOiClZXzsd{whUUN3ME2wMlA5OSEQvF2= MYGxOlU4ODlzOB?=
V79 cells Ml3mSpVv[3Srb36gZZN{[Xl? NHHMZppKdmirYnn0bY9vKG:oIHj1cYFvKEO\UEK0JIh6\HKxeInsZZNmKGW6cILld5Nm\CCrbjDWO|kh[2WubIOsJGlEPTB;MD6zNVIh|ryP M1HQ[FE2PjF3NUO0
hamster V79MZh11B1 cells MoroSpVv[3Srb36gZZN{[Xl? NV;FeItRUW6qaXLpeIlwdiCxZjDoeY1idiCFWWCxNWIyKGW6cILld5Nm\CCrbjDoZY1{fGW{IG[3PW1bcDFzQkGgZ4VtdHNuIFnDOVA:OC5zMkeg{txO M{PPelE5Pjd{OE[4
hamster V79MZh11B2 cells NVXXSY1WTnWwY4Tpc44h[XO|YYm= NFy1T3pKdmirYnn0bY9vKG:oIHj1cYFvKEO\UEGxRlIh\XiycnXzd4VlKGmwIHjhcZN1\XJiVke5UXppOTGEMjDj[YxteyxiSVO1NF0xNjB4NzFOwG0> NHrZeIsyQDZ5Mki2PC=>
CHO cells NWqzNGNITnWwY4Tpc44h[XO|YYm= NYPNUHB1UW6qaXLpeIlwdiCxZjDoeY1idiCHUleg[ZhxemW|c3XkJIlvKEOKTzDj[YxteyCkeTD3bI9t\SClZXzsJJBifGOqIHPsZY1xKHSnY3jubZF2\SxiSVO1NF0yNjlyNUS2JO69VQ>? MoW3NVg1PDh|NEK=
V79 11B1 cells NVi4[ZR{TnWwY4Tpc44h[XO|YYm= NXnBb5B3UW6qaXLpeIlwdiCxZjDoeY1idiCFWWCxNWIyKGW6cILld5Nm\CCrbjDWO|khOTGEMTDj[YxteyxiSVO1NF0xNjJ{NDFOwG0> NUXRS3pGOTZ3N{C5NVg>
Topp 3 cells NGTPPGlHfW6ldHnvckBie3OjeR?= MnK2TY5pcWKrdHnvckBw\iCqdX3hckBEYVB3MTDlfJBz\XO|ZXSgbY4hXG:ycDCzJINmdGy|IHL5JIxidm:|dHXyc4wh\GWvZYTofYxie2ViYYPzZZktKEmFNUC9NE4yQSEQvF2= M4qz[lE4OTl2N{G2
V79 cells MWTGeY5kfGmxbjDhd5NigQ>? NUPte5NyUW6qaXLpeIlwdiCxZjDoeY1idiCFWWCyOGEyKGW6cILld5Nm\CCrbjDjbIlv\XOnIHjhcZN1\XJiVke5JINmdGy|LDDJR|UxRTBwM{GyJO69VQ>? MUWyNFU6PDh4Mh?=
V79MZ cells MUTGeY5kfGmxbjDhd5NigQ>? MlG2TY5pcWKrdHnvckBw\iCqdX3hckBEYVBzMVKyJIV5eHKnc4Pl[EBqdiCqYX3zeIVzKFZ5OV3aJINmdGy|IIXzbY5oKDFzLXTlc5h6[2:{dHnjc5N1\XKxbnWgd5Vje3S{YYTlMEBKSzVyPUCuNFY4KM7:TR?= NIjpTGQzPDlyMEK0Oy=>
V79MZh cells MUHGeY5kfGmxbjDhd5NigQ>? M{n2SGlvcGmkaYTpc44hd2ZiaIXtZY4hS1mSMUHCNkBmgHC{ZYPz[YQhcW5iaHHtd5RmeiCYN{nNXogh[2WubIOsJGlEPTB;MD6wOlch|ryP M370XlIxPTVyMUG4
human epidermal keratinocytes MVjGeY5kfGmxbjDhd5NigQ>? MUHJcohq[mm2aX;uJI9nKEO\UEK0RVEhcW5iaIXtZY4h\XCrZHXycYFtKGuncnH0bY5w[3m2ZYOsJGlEPTB;MD6xNlYh|ryP M{L6dVIxPTl2OE[y
V79MZh cells M4ThdmZ2dmO2aX;uJIF{e2G7 NWi2O5ljUW6qaXLpeIlwdiCxZjDoeY1idiCFWWCxNWIyKGW6cILld5Nm\CCrbjDoZY1{fGW{IG[3PW1bcCClZXzsd{whUUN3ME2wMlEzPyEQvF2= NXe3ZVRYOjB3NUCxNVg>

... 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 Conditions Sponsor/Collaborators Start Date Phases
NCT02147964 Not yet recruiting Gonadotropin Deficiency University of Washington June 2019 Phase 2
NCT03688971 Recruiting Seborrheic Dermatitis Cutanea Life Sciences Inc. October 22 2018 Phase 2
NCT03621280 Not yet recruiting Cushing Syndrome|Cushing Disease Cortendo AB October 20 2018 Phase 3
NCT03471364 Recruiting Skin Burning Sensation|Skin Rash Mayo Clinic|National Cancer Institute (NCI) August 22 2018 Early Phase 1
NCT02582177 Not yet recruiting Tinea Ache Laboratorios Farmaceuticos S.A. August 1 2018 Phase 3
NCT03473418 Not yet recruiting Vaginal Candidiasis Assiut University April 1 2018 Phase 3

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID