Ketoconazole (R 41400)

Catalog No.S1353

For research use only.

Ketoconazole (R 41400) inhibits cyclosporine oxidase and testosterone 6 beta-hydroxylase with IC50 of 0.19 mM and 0.22 mM, respectively. Ketoconazole is an androgen biosynthesis inhibitor.

Ketoconazole (R 41400) Chemical Structure

CAS No. 65277-42-1

Selleck's Ketoconazole (R 41400) has been cited by 11 Publications

Purity & Quality Control

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Biological Activity

Description Ketoconazole (R 41400) inhibits cyclosporine oxidase and testosterone 6 beta-hydroxylase with IC50 of 0.19 mM and 0.22 mM, respectively. Ketoconazole is an androgen biosynthesis inhibitor.
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 M1z5VmZ2dmO2aX;uJIF{e2G7 NUn5eWwxUW6qaXLpeIlwdiCxZjDQMYdtgWOxcILveIVqdixiaIXtZY4hVC2PRGKxJIV5eHKnc4Pl[EBqdiCOTFOtVGsyKGWyaYTo[Yxq[WxiY3XscJMhfXOrbnegZ4Ft[2Wrbj3BUUBxd2yjcnnzZZRqd25iYYPzZZktKEmFNUC9OE45KM7:TR?= Mni3NVI3QTl|OEm=
MCF7 cells M4S0e2Z2dmO2aX;uJIF{e2G7 MofSTY5pcWKrdHnvckBw\iCFWWCyOmEyKGmwIHj1cYFvKE2FRkegZ4VtdHNiYYPz[ZN{\WRiYYOgZYxtNXS{YX7zJJJmfGmwb3njJIFkcWRibXX0ZYJwdGm|bTygTWM2OD1zMjFOwG0> M2eybVE3Ojd7N{ew
human THP1 cells M{PVPGN6fG:2b4jpZ4l1gSCjc4PhfS=> MnflOFghcA>? NUW4fIJCS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hXEiSMTDj[YxteyCjZoTldkA1QCCqcoOsJGlEPTB;NESg{txO M3fC[VE4QTZyOUKz
P815B cells MWjDfZRwfG:6aXPpeJkh[XO|YYm= M2HiR|I1KGh? MULDfZRwfG:6aXPpeJkh[WejaX7zeEBud3W|ZTDQPFE2SiClZXzsd{Bi\nSncjCyOEBpenNiYomgUXRUN1CPUzDhd5NigSxiTFS1NF0zPSEQvF2= NFr6OIozPTB|Nke4PS=>
V79 11B2 cells MVrGeY5kfGmxbjDhd5NigQ>? NED0d|RKdmirYnn0bY9vKG:oIHj1cYFvKEO\UEGxRlIh\XiycnXzd4VlKGmwIG[3PUAyOUJ{IHPlcIx{NCCLQ{WwQVAvODhzIN88US=> NXrLR4lsOTZ3N{C5NVg>
V79 cells NXy1eI42TnWwY4Tpc44h[XO|YYm= NGPNRphKdmirYnn0bY9vKG:oIHj1cYFvKEO\UEK0JIh6\HKxeInsZZNmKGW6cILld5Nm\CCrbjDWO|kh[2WubIOsJGlEPTB;MD6zNVIh|ryP M2r4SVE2PjF3NUO0
hamster V79MZh11B1 cells MkP0SpVv[3Srb36gZZN{[Xl? NV\Oe3FmUW6qaXLpeIlwdiCxZjDoeY1idiCFWWCxNWIyKGW6cILld5Nm\CCrbjDoZY1{fGW{IG[3PW1bcDFzQkGgZ4VtdHNuIFnDOVA:OC5zMkeg{txO NFPteGsyQDZ5Mki2PC=>
hamster V79MZh11B2 cells MUfGeY5kfGmxbjDhd5NigQ>? M1vHUWlvcGmkaYTpc44hd2ZiaIXtZY4hS1mSMUHCNkBmgHC{ZYPz[YQhcW5iaHHtd5RmeiCYN{nNXogyOUJ{IHPlcIx{NCCLQ{WwQVAvODZ5IN88US=> NIDzUmcyQDZ5Mki2PC=>
CHO cells NInYU3lHfW6ldHnvckBie3OjeR?= MknSTY5pcWKrdHnvckBw\iCqdX3hckBGWkdiZYjwdoV{e2WmIHnuJGNJVyClZXzsd{BjgSC5aH;s[UBk\WyuIIDheINpKGOuYX3wJJRm[2iwaYH1[UwhUUN3ME2xMlkxPTR4IN88US=> MUSxPFQ1QDN2Mh?=
V79 11B1 cells MmjSSpVv[3Srb36gZZN{[Xl? NGnXZoxKdmirYnn0bY9vKG:oIHj1cYFvKEO\UEGxRlEh\XiycnXzd4VlKGmwIG[3PUAyOUJzIHPlcIx{NCCLQ{WwQVAvOjJ2IN88US=> NIfmNW0yPjV5MEmxPC=>
Topp 3 cells NV7PR5c{TnWwY4Tpc44h[XO|YYm= NFXF[IdKdmirYnn0bY9vKG:oIHj1cYFvKEO\UEWxJIV5eHKnc4Pl[EBqdiCWb4DwJFMh[2WubIOgZpkhdGGwb4P0[ZJwdCCmZX3leIh6dGG|ZTDhd5NigSxiSVO1NF0xNjF7IN88US=> MYqxO|E6PDdzNh?=
V79 cells MXXGeY5kfGmxbjDhd5NigQ>? NG\u[IdKdmirYnn0bY9vKG:oIHj1cYFvKEO\UEK0RVEh\XiycnXzd4VlKGmwIHPobY5me2ViaHHtd5RmeiCYN{mgZ4VtdHNuIFnDOVA:OC5|MUKg{txO M1;CN|IxPTl2OE[y
V79MZ cells MorPSpVv[3Srb36gZZN{[Xl? M2TMNGlvcGmkaYTpc44hd2ZiaIXtZY4hS1mSMUHCNkBmgHC{ZYPz[YQhcW5iaHHtd5RmeiCYN{nNXkBk\WyuczD1d4lv\yBzMT3k[Y95gWOxcoTpZ49{fGW{b37lJJN2[nO2cnH0[UwhUUN3ME2wMlA3PyEQvF2= NVjscIZoOjR7MECyOFc>
V79MZh cells NH7WdGpHfW6ldHnvckBie3OjeR?= NILGcpdKdmirYnn0bY9vKG:oIHj1cYFvKEO\UEGxRlIh\XiycnXzd4VlKGmwIHjhcZN1\XJiVke5UXppKGOnbHzzMEBKSzVyPUCuNFY4KM7:TR?= NF;idlczODV3MEGxPC=>
human epidermal keratinocytes Ml\PSpVv[3Srb36gZZN{[Xl? NFu3WFFKdmirYnn0bY9vKG:oIFPZVFI1STFiaX6gbJVu[W5iZYDp[IVzdWGuIHvldoF1cW6xY4n0[ZMtKEmFNUC9NE4yOjZizszN NH;hZ2MzODV7NEi2Ni=>
V79MZh cells M2fTdWZ2dmO2aX;uJIF{e2G7 MXXJcohq[mm2aX;uJI9nKGi3bXHuJGN[WDFzQkGg[ZhxemW|c3XkJIlvKGijbYP0[ZIhXjd7TWroJINmdGy|LDDJR|UxRTBwMUK3JO69VQ>? NVPsRotoOjB3NUCxNVg>
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 (from reference)

Kinase Assay:[1]
  • 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]
  • 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.
Animal Research:[4]
  • Animal Models: male Wistar rats
  • Dosages: 25 mg/kg
  • Administration: Intraperitoneal injection

Solubility (25°C)

In vitro

DMSO 5 mg/mL warmed
(9.4 mM)
Water Insoluble
Ethanol '''7 mg/mL

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

Chemical Information

Molecular Weight 531.43


CAS No. 65277-42-1
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC(=O)N1CCN(CC1)C2=CC=C(C=C2)OCC3COC(O3)(CN4C=CN=C4)C5=C(C=C(C=C5)Cl)Cl

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

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% DMSO % % Tween 80 % ddH2O

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04869449 Not yet recruiting Drug: Ketoconazole Glioblastoma|Glioblastoma Multiforme|Glioblastoma Multiforme of Brain|Glioblastoma Multiforme Adult Milton S. Hershey Medical Center January 2022 Early Phase 1
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
NCT04872920 Recruiting -- Cushing Syndrome HRA Pharma December 20 2018 --
NCT03473418 Unknown status Drug: Ketoconazole|Drug: Terconazole Vaginal Candidiasis Assiut University April 1 2018 Phase 3

(data from, updated on 2022-01-17)

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.

Handling Instructions

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