Home Metabolism P450 (e.g. CYP17) inhibitor - Androgen Receptor inhibitor - Fungal inhibitor Ketoconazole For research use only.

Ketoconazole

Synonyms: R 41400

Ketoconazole 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 Chemical Structure

Ketoconazole Chemical Structure

CAS: 65277-42-1

Selleck's Ketoconazole has been cited by 21 publications

Purity & Quality Control

Batch: Purity: 99.95%
99.95

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Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
LLC-PK1 epithelial cells Function assay Inhibition of P-glycoprotein, human L-MDR1 expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay, IC50=4.8 μM 12699389
MCF7 cells Function assay Inhibition of CYP26A1 in human MCF7 cells assessed as all-trans retinoic acid metabolism, IC50=12 μM 16279770
human THP1 cells Cytotoxicity assay 48 h Cytotoxicity against human THP1 cells after 48 hrs, IC50=44 μM 17960923
CHO cells Function assay Inhibition of CYP24A1 expressed in CHO cells, IC50=0.52 μM 20655626
P815B cells Cytotoxicity assay 24 h Cytotoxicity against mouse P815B cells after 24 hrs by MTS/PMS assay, LD50=25 μM 25036789
V79 11B2 cells Function assay Inhibition of human CYP11B2 expressed in V79 11B2 cells, IC50=0.081 μM 16570918
V79 cells Function assay Inhibition of human CYP24 hydroxylase expressed in V79 cells, IC50=0.312 μM 15615534
hamster V79MZh11B1 cells Function assay Inhibition of human CYP11B1 expressed in hamster V79MZh11B1 cells, IC50=0.127 μM 18672868
hamster V79MZh11B2 cells Function assay Inhibition of human CYP11B2 expressed in hamster V79MZh11B2 cells, IC50=0.067 μM 18672868
CHO cells Function assay Inhibition of human ERG expressed in CHO cells by whole cell patch clamp technique, IC50=1.90546 μM 18448342
V79 11B1 cells Function assay Inhibition of human CYP11B1 expressed in V79 11B1 cells, IC50=0.224 μM 16570918
Topp 3 cells Function assay Inhibition of human CYP51 expressed in Topp 3 cells by lanosterol demethylase assay, IC50=0.19 μM 17194716
V79 cells Function assay Inhibition of human CYP24A1 expressed in chinese hamster V79 cells, IC50=0.312 μM 20594862
V79MZ cells Function assay Inhibition of human CYP11B2 expressed in hamster V79MZ cells using 11-deoxycorticosterone substrate, IC50=0.067 μM 24900247
V79MZh cells Function assay Inhibition of human CYP11B2 expressed in hamster V79MZh cells, IC50=0.067 μM 20550118
human epidermal keratinocytes Function assay Inhibition of CYP24A1 in human epidermal keratinocytes, IC50=0.126 μM 20594862
V79MZh cells Function assay Inhibition of human CYP11B1 expressed in hamster V79MZh cells, IC50=0.127 μM 20550118
Click to View More Cell Line Experimental Data

Biological Activity

Description Ketoconazole 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.
Targets
Cyclosporine oxidase [1] Testosterone 6 beta-hydroxylase [1]
0.19 mM 0.22 mM
In vitro
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]
Kinase Assay 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 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.
In Vivo
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]
Animal Research Animal Models male Wistar rats
Dosages 25 mg/kg
Administration Intraperitoneal injection
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT04869449 Recruiting Glioblastoma|Glioblastoma Multiforme|Glioblastoma Multiforme of Brain|Glioblastoma Multiforme Adult Milton S. Hershey Medical Center May 12 2022 Early Phase 1
NCT04212000 Completed Healthy Cortendo AB December 16 2019 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
NCT04872920 Recruiting Cushing Syndrome HRA Pharma December 20 2018 --
NCT03473418 Unknown status Vaginal Candidiasis Assiut University April 1 2018 Phase 3

Chemical lnformation & Solubility

Molecular Weight 531.43 Formula

C26H28Cl2N4O4
CAS No. 65277-42-1 SDF Download Ketoconazole SDF
Smiles CC(=O)N1CCN(CC1)C2=CC=C(C=C2)OCC3COC(O3)(CN4C=CN=C4)C5=C(C=C(C=C5)Cl)Cl
Storage (From the date of receipt)

In vitro
Batch:

Ethanol : 7 mg/mL

DMSO : 3 mg/mL ( (5.64 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble


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In vivo
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