Ketoconazole

For research use only.

Catalog No.S1353

6 publications

Ketoconazole Chemical Structure

CAS No. 65277-42-1

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) EUR 77 In stock
EUR 95 In stock
EUR 252 In stock
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Selleck's Ketoconazole has been cited by 6 publications

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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 MVPGeY5kfGmxbjDhd5NigQ>? M{W0TWlvcGmkaYTpc44hd2ZiUD3ncJlkd3C{b4TlbY4tKGi3bXHuJGwuVUSUMTDlfJBz\XO|ZXSgbY4hVEyFLWDLNUBmeGm2aHXsbYFtKGOnbHzzJJV{cW6pIHPhcINmcW5vQV2gdI9t[XKrc3H0bY9vKGG|c3H5MEBKSzVyPUSuPEDPxE1? NFnLN2kyOjZ7OUO4PS=>
MCF7 cells NXTYZ4V3TnWwY4Tpc44h[XO|YYm= MUXJcohq[mm2aX;uJI9nKEO\UEK2RVEhcW5iaIXtZY4hVUOINzDj[YxteyCjc4Pld5Nm\CCjczDhcIwufHKjboOgdoV1cW6xaXOgZYNq\CCvZYThZo9tcXOvLDDJR|UxRTF{IN88US=> NFLrO|AyPjJ5OUe3NC=>
human THP1 cells MlHHR5l1d3SxeHnjbZR6KGG|c3H5 MlfGOFghcA>? M1PJfWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJHRJWDFiY3XscJMh[W[2ZYKgOFghcHK|LDDJR|UxRTR2IN88US=> NFyx[2oyPzl4MEmyNy=>
CHO cells M1uwcWZ2dmO2aX;uJIF{e2G7 M2XNTmlvcGmkaYTpc44hd2ZiQ2nQNlRCOSCneIDy[ZN{\WRiaX6gR2hQKGOnbHzzMEBKSzVyPUCuOVIh|ryP NIT5bGIzODZ3NU[yOi=>
P815B cells NHzCbFBEgXSxdH;4bYNqfHliYYPzZZk> M3\4Z|I1KGh? NVezNpZpS3m2b4TvfIlkcXS7IHHnZYlve3RibX;1d4UhWDhzNVKgZ4VtdHNiYX\0[ZIhOjRiaILzJIJ6KE2WUz;QUXMh[XO|YYmsJGxFPTB;MkWg{txO NXTxPIwzOjVyM{[3PFk>
V79 11B2 cells MVXGeY5kfGmxbjDhd5NigQ>? MkPRTY5pcWKrdHnvckBw\iCqdX3hckBEYVBzMVKyJIV5eHKnc4Pl[EBqdiCYN{mgNVFDOiClZXzsd{whUUN3ME2wMlA5OSEQvF2= M{PX[|E3PTdyOUG4
V79 cells NF3PZZdHfW6ldHnvckBie3OjeR?= NIm4N4pKdmirYnn0bY9vKG:oIHj1cYFvKEO\UEK0JIh6\HKxeInsZZNmKGW6cILld5Nm\CCrbjDWO|kh[2WubIOsJGlEPTB;MD6zNVIh|ryP NWjxU5VSOTV4MUW1N|Q>
hamster V79MZh11B1 cells M{HtcWZ2dmO2aX;uJIF{e2G7 M1zGW2lvcGmkaYTpc44hd2ZiaIXtZY4hS1mSMUHCNUBmgHC{ZYPz[YQhcW5iaHHtd5RmeiCYN{nNXogyOUJzIHPlcIx{NCCLQ{WwQVAvOTJ5IN88US=> M2jFcVE5Pjd{OE[4
hamster V79MZh11B2 cells MXjGeY5kfGmxbjDhd5NigQ>? MXjJcohq[mm2aX;uJI9nKGi3bXHuJGN[WDFzQkKg[ZhxemW|c3XkJIlvKGijbYP0[ZIhXjd7TWroNVFDOiClZXzsd{whUUN3ME2wMlA3PyEQvF2= NYTVUnJ7OTh4N{K4Olg>
CHO cells MX7GeY5kfGmxbjDhd5NigQ>? MWPJcohq[mm2aX;uJI9nKGi3bXHuJGVTTyCneIDy[ZN{\WRiaX6gR2hQKGOnbHzzJIJ6KHeqb3zlJINmdGxicHH0Z4gh[2yjbYCgeIVkcG6rcYXlMEBKSzVyPUGuPVA2PDZizszN MorPNVg1PDh|NEK=
V79 11B1 cells NWP4bYpITnWwY4Tpc44h[XO|YYm= NH3KdnFKdmirYnn0bY9vKG:oIHj1cYFvKEO\UEGxRlEh\XiycnXzd4VlKGmwIG[3PUAyOUJzIHPlcIx{NCCLQ{WwQVAvOjJ2IN88US=> MVixOlU4ODlzOB?=
Topp 3 cells NGrWPVdHfW6ldHnvckBie3OjeR?= NFPWeJVKdmirYnn0bY9vKG:oIHj1cYFvKEO\UEWxJIV5eHKnc4Pl[EBqdiCWb4DwJFMh[2WubIOgZpkhdGGwb4P0[ZJwdCCmZX3leIh6dGG|ZTDhd5NigSxiSVO1NF0xNjF7IN88US=> M3zae|E4OTl2N{G2
V79 cells M2jHcmZ2dmO2aX;uJIF{e2G7 NEjkeVRKdmirYnn0bY9vKG:oIHj1cYFvKEO\UEK0RVEh\XiycnXzd4VlKGmwIHPobY5me2ViaHHtd5RmeiCYN{mgZ4VtdHNuIFnDOVA:OC5|MUKg{txO M4HtbFIxPTl2OE[y
V79MZ cells M2fIS2Z2dmO2aX;uJIF{e2G7 NGXKR3RKdmirYnn0bY9vKG:oIHj1cYFvKEO\UEGxRlIh\XiycnXzd4VlKGmwIHjhcZN1\XJiVke5UXoh[2WubIOgeZNqdmdiMUGt[IVwgHmlb4L0bYNwe3Sncn;u[UB{fWK|dILheIUtKEmFNUC9NE4xPjdizszN NHrGZVIzPDlyMEK0Oy=>
V79MZh cells NX\0OIYxTnWwY4Tpc44h[XO|YYm= M1;kUmlvcGmkaYTpc44hd2ZiaIXtZY4hS1mSMUHCNkBmgHC{ZYPz[YQhcW5iaHHtd5RmeiCYN{nNXogh[2WubIOsJGlEPTB;MD6wOlch|ryP NGPsWXEzODV3MEGxPC=>
human epidermal keratinocytes NVzhfGxNTnWwY4Tpc44h[XO|YYm= M4HYNmlvcGmkaYTpc44hd2ZiQ2nQNlRCOSCrbjDoeY1idiCncHnk[ZJu[Wxia3XyZZRqdm:leYTld{whUUN3ME2wMlEzPiEQvF2= MUCyNFU6PDh4Mh?=
V79MZh cells M4[1NWZ2dmO2aX;uJIF{e2G7 NXWweY51UW6qaXLpeIlwdiCxZjDoeY1idiCFWWCxNWIyKGW6cILld5Nm\CCrbjDoZY1{fGW{IG[3PW1bcCClZXzsd{whUUN3ME2wMlEzPyEQvF2= NWG0eJh{OjB3NUCxNVg>

... 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]
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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
Formula

C26H28Cl2N4O4

CAS No. 65277-42-1
Storage powder
in solvent
Synonyms N/A
Smiles CC(=O)N1CCN(CC1)C2=CC=C(C=C2)OCC3COC(O3)(CN4C=CN=C4)C5=C(C=C(C=C5)Cl)Cl

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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 Completed 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