For research use only.
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.
Selleck's Ketoconazole has been cited by 6 publications
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|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.|
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.  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.  Ketoconazole is susceptable to several Malassezia species with minimum inhibitory concentrations (MICs) of 0.03 µg/mL. 
|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.  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. |
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
-  Oliver WR Jr, et al. Proc Natl Acad Sci U S A, 2001, 98(9), 5306-5311.
-  Eil C, et al. Horm Metab Res, 1992, 24(8), 367-370.
-  Forgue-Lafitte ME, et al. Cancer Res, 1992, 52(24), 6827-6831.
|In vitro||Ethanol||7 mg/mL (13.17 mM)|
|DMSO||5 mg/mL warmed (9.4 mM)|
|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.
* 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.
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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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