For research use only.

Catalog No.S1353

4 publications

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.

Size Price Stock Quantity  
10mM (1mL in DMSO) USD 57 In stock
USD 97 In stock
USD 257 In stock
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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 NFPyWYJHfW6ldHnvckBie3OjeR?= NX;aUHA4UW6qaXLpeIlwdiCxZjDQMYdtgWOxcILveIVqdixiaIXtZY4hVC2PRGKxJIV5eHKnc4Pl[EBqdiCOTFOtVGsyKGWyaYTo[Yxq[WxiY3XscJMhfXOrbnegZ4Ft[2Wrbj3BUUBxd2yjcnnzZZRqd25iYYPzZZktKEmFNUC9OE45KM7:TR?= NYTyZVdQOTJ4OUmzPFk>
MCF7 cells MkDDSpVv[3Srb36gZZN{[Xl? Mm\3TY5pcWKrdHnvckBw\iCFWWCyOmEyKGmwIHj1cYFvKE2FRkegZ4VtdHNiYYPz[ZN{\WRiYYOgZYxtNXS{YX7zJJJmfGmwb3njJIFkcWRibXX0ZYJwdGm|bTygTWM2OD1zMjFOwG0> Mn31NVYzPzl5N{C=
human THP1 cells MkjzR5l1d3SxeHnjbZR6KGG|c3H5 M2DCU|Q5KGh? M3vFW2N6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJHRJWDFiY3XscJMh[W[2ZYKgOFghcHK|LDDJR|UxRTR2IN88US=> MnjrNVc6PjB7MkO=
CHO cells NU\kRZVXTnWwY4Tpc44h[XO|YYm= NFrp[phKdmirYnn0bY9vKG:oIFPZVFI1STFiZYjwdoV{e2WmIHnuJGNJVyClZXzsd{whUUN3ME2wMlUzKM7:TR?= MVOyNFY2PTZ{Nh?=
P815B cells MkTGR5l1d3SxeHnjbZR6KGG|c3H5 NHrpT2EzPCCq MUPDfZRwfG:6aXPpeJkh[WejaX7zeEBud3W|ZTDQPFE2SiClZXzsd{Bi\nSncjCyOEBpenNiYomgUXRUN1CPUzDhd5NigSxiTFS1NF0zPSEQvF2= NHz3Z2IzPTB|Nke4PS=>
V79 11B2 cells MlTVSpVv[3Srb36gZZN{[Xl? NF7yTFFKdmirYnn0bY9vKG:oIHj1cYFvKEO\UEGxRlIh\XiycnXzd4VlKGmwIG[3PUAyOUJ{IHPlcIx{NCCLQ{WwQVAvODhzIN88US=> MX:xOlU4ODlzOB?=
V79 cells MVzGeY5kfGmxbjDhd5NigQ>? MoXLTY5pcWKrdHnvckBw\iCqdX3hckBEYVB{NDDofYRzd3i7bHHz[UBmgHC{ZYPz[YQhcW5iVke5JINmdGy|LDDJR|UxRTBwM{GyJO69VQ>? M3XiXVE2PjF3NUO0
hamster V79MZh11B1 cells M4P6NmZ2dmO2aX;uJIF{e2G7 M2q3XWlvcGmkaYTpc44hd2ZiaIXtZY4hS1mSMUHCNUBmgHC{ZYPz[YQhcW5iaHHtd5RmeiCYN{nNXogyOUJzIHPlcIx{NCCLQ{WwQVAvOTJ5IN88US=> NG\pZmoyQDZ5Mki2PC=>
hamster V79MZh11B2 cells NHjQTY5HfW6ldHnvckBie3OjeR?= Mke0TY5pcWKrdHnvckBw\iCqdX3hckBEYVBzMVKyJIV5eHKnc4Pl[EBqdiCqYX3zeIVzKFZ5OV3abFEySjJiY3XscJMtKEmFNUC9NE4xPjdizszN MoPYNVg3PzJ6Nki=
CHO cells Mo\lSpVv[3Srb36gZZN{[Xl? MmLnTY5pcWKrdHnvckBw\iCqdX3hckBGWkdiZYjwdoV{e2WmIHnuJGNJVyClZXzsd{BjgSC5aH;s[UBk\WyuIIDheINpKGOuYX3wJJRm[2iwaYH1[UwhUUN3ME2xMlkxPTR4IN88US=> NGHUN3kyQDR2OEO0Ni=>
V79 11B1 cells MUjGeY5kfGmxbjDhd5NigQ>? NV;aU2hyUW6qaXLpeIlwdiCxZjDoeY1idiCFWWCxNWIyKGW6cILld5Nm\CCrbjDWO|khOTGEMTDj[YxteyxiSVO1NF0xNjJ{NDFOwG0> NHr2TXgyPjV5MEmxPC=>
Topp 3 cells M4P3cmZ2dmO2aX;uJIF{e2G7 NEjVb4dKdmirYnn0bY9vKG:oIHj1cYFvKEO\UEWxJIV5eHKnc4Pl[EBqdiCWb4DwJFMh[2WubIOgZpkhdGGwb4P0[ZJwdCCmZX3leIh6dGG|ZTDhd5NigSxiSVO1NF0xNjF7IN88US=> NVvNTG1LOTdzOUS3NVY>
V79 cells M2DvXGZ2dmO2aX;uJIF{e2G7 Moi2TY5pcWKrdHnvckBw\iCqdX3hckBEYVB{NFGxJIV5eHKnc4Pl[EBqdiClaHnu[ZNmKGijbYP0[ZIhXjd7IHPlcIx{NCCLQ{WwQVAvOzF{IN88US=> MUGyNFU6PDh4Mh?=
V79MZ cells NVTPWGJXTnWwY4Tpc44h[XO|YYm= Ml3ITY5pcWKrdHnvckBw\iCqdX3hckBEYVBzMVKyJIV5eHKnc4Pl[EBqdiCqYX3zeIVzKFZ5OV3aJINmdGy|IIXzbY5oKDFzLXTlc5h6[2:{dHnjc5N1\XKxbnWgd5Vje3S{YYTlMEBKSzVyPUCuNFY4KM7:TR?= M{nNOVI1QTByMkS3
V79MZh cells MX7GeY5kfGmxbjDhd5NigQ>? NF3DWZVKdmirYnn0bY9vKG:oIHj1cYFvKEO\UEGxRlIh\XiycnXzd4VlKGmwIHjhcZN1\XJiVke5UXppKGOnbHzzMEBKSzVyPUCuNFY4KM7:TR?= MVWyNFU2ODFzOB?=
human epidermal keratinocytes MXzGeY5kfGmxbjDhd5NigQ>? NEDt[XhKdmirYnn0bY9vKG:oIFPZVFI1STFiaX6gbJVu[W5iZYDp[IVzdWGuIHvldoF1cW6xY4n0[ZMtKEmFNUC9NE4yOjZizszN NIrEeZczODV7NEi2Ni=>
V79MZh cells MVTGeY5kfGmxbjDhd5NigQ>? Ml;MTY5pcWKrdHnvckBw\iCqdX3hckBEYVBzMVKxJIV5eHKnc4Pl[EBqdiCqYX3zeIVzKFZ5OV3abEBk\WyuczygTWM2OD1yLkGyO{DPxE1? MYiyNFU2ODFzOB?=

... 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
  • 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
Smiles CC(=O)N1CCN(CC1)C2=CC=C(OCC3COC(C[N]4C=CN=C4)(O3)C5=CC=C(Cl)C=C5Cl)C=C2

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% DMSO % % Tween 80 % ddH2O

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04212000 Completed Drug: Levoketoconazole|Drug: Ketoconazole Healthy Cortendo AB December 16 2019 Phase 1
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 Unknown status Drug: Ketoconazole|Drug: Terconazole Vaginal Candidiasis Assiut University April 1 2018 Phase 3
NCT03277690 Active not 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