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Ketoconazole (R 41400)

Name: Ketoconazole (R 41400)
Brand: Selleck Chemicals
SKU: S1353
Rating: 5 (12 reviews)

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 12 Publications

Purity & Quality Control

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P450 (e.g. CYP17) Signaling Pathway Map

Biological Activity

Description

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	MXzGeY5kfGmxbjDhd5NigQ>?		NGTn[nhKdmirYnn0bY9vKG:oIGCt[4x6[2:ycn;0[YlvNCCqdX3hckBNNU2GUkGg[ZhxemW\|c3XkJIlvKEyOQz3QT\|Eh\XCrdHjlcIlidCClZXzsd{B2e2mwZzDjZYxk\WmwLVHNJJBwdGG{aYPheIlwdiCjc4PhfUwhUUN3ME20Mlgh\|ryP	MWGxNlY6QTN6OR?=
MCF7 cells	NH3zcXFHfW6ldHnvckBie3OjeR?=		MoPlTY5pcWKrdHnvckBw\iCFWWCyOmEyKGmwIHj1cYFvKE2FRkegZ4VtdHNiYYPz[ZN{\WRiYYOgZYxtNXS{YX7zJJJmfGmwb3njJIFkcWRibXX0ZYJwdGm\|bTygTWM2OD1zMjFOwG0>	M1;3c\|E3Ojd7N{ew
human THP1 cells	NIX5WYhEgXSxdH;4bYNqfHliYYPzZZk>	NHTweIE1QCCq	NEjCRWFEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBVUFBzIHPlcIx{KGGodHXyJFQ5KGi{czygTWM2OD12NDFOwG0>	MknHNVc6PjB7MkO=
CHO cells	M{H0SmZ2dmO2aX;uJIF{e2G7		NYe0NZVSUW6qaXLpeIlwdiCxZjDDXXAzPEFzIHX4dJJme3OnZDDpckBEUE9iY3XscJMtKEmFNUC9NE42OiEQvF2=	NIHlcWozODZ3NU[yOi=>
P815B cells	MnjYR5l1d3SxeHnjbZR6KGG\|c3H5	M4[1U\|I1KGh?	NEC3SG9EgXSxdH;4bYNqfHliYXfhbY5{fCCvb4Xz[UBRQDF3QjDj[YxteyCjZoTldkAzPCCqcoOgZpkhVVSVL2DNV{Bie3OjeTygUGQ2OD1{NTFOwG0>	NWjnUVRzOjVyM{[3PFk>
V79 11B2 cells	NULMOXpNTnWwY4Tpc44h[XO\|YYm=		NYDoOIZQUW6qaXLpeIlwdiCxZjDoeY1idiCFWWCxNWIzKGW6cILld5Nm\CCrbjDWO\|khOTGEMjDj[YxteyxiSVO1NF0xNjB6MTFOwG0>	NIH6V4syPjV5MEmxPC=>
V79 cells	NUC3OYtGTnWwY4Tpc44h[XO\|YYm=		MmLpTY5pcWKrdHnvckBw\iCqdX3hckBEYVB{NDDofYRzd3i7bHHz[UBmgHC{ZYPz[YQhcW5iVke5JINmdGy\|LDDJR\|UxRTBwM{GyJO69VQ>?	MWexOVYyPTV\|NB?=
hamster V79MZh11B1 cells	M2jyUWZ2dmO2aX;uJIF{e2G7		NELsdVBKdmirYnn0bY9vKG:oIHj1cYFvKEO\UEGxRlEh\XiycnXzd4VlKGmwIHjhcZN1\XJiVke5UXppOTGEMTDj[YxteyxiSVO1NF0xNjF{NzFOwG0>	MXixPFY4Ojh4OB?=
hamster V79MZh11B2 cells	NHGxOZNHfW6ldHnvckBie3OjeR?=		NGSzdHBKdmirYnn0bY9vKG:oIHj1cYFvKEO\UEGxRlIh\XiycnXzd4VlKGmwIHjhcZN1\XJiVke5UXppOTGEMjDj[YxteyxiSVO1NF0xNjB4NzFOwG0>	NHnOVXUyQDZ5Mki2PC=>
CHO cells	M3LNbmZ2dmO2aX;uJIF{e2G7		MortTY5pcWKrdHnvckBw\iCqdX3hckBGWkdiZYjwdoV{e2WmIHnuJGNJVyClZXzsd{BjgSC5aH;s[UBk\WyuIIDheINpKGOuYX3wJJRm[2iwaYH1[UwhUUN3ME2xMlkxPTR4IN88US=>	Mm[yNVg1PDh\|NEK=
V79 11B1 cells	MULGeY5kfGmxbjDhd5NigQ>?		NXTpNWhNUW6qaXLpeIlwdiCxZjDoeY1idiCFWWCxNWIyKGW6cILld5Nm\CCrbjDWO\|khOTGEMTDj[YxteyxiSVO1NF0xNjJ{NDFOwG0>	NVL4dlZxOTZ3N{C5NVg>
Topp 3 cells	MV\GeY5kfGmxbjDhd5NigQ>?		NEe1Z\|RKdmirYnn0bY9vKG:oIHj1cYFvKEO\UEWxJIV5eHKnc4Pl[EBqdiCWb4DwJFMh[2WubIOgZpkhdGGwb4P0[ZJwdCCmZX3leIh6dGG\|ZTDhd5NigSxiSVO1NF0xNjF7IN88US=>	NV3QTIxzOTdzOUS3NVY>
V79 cells	NH;PUVdHfW6ldHnvckBie3OjeR?=		NF\EZZpKdmirYnn0bY9vKG:oIHj1cYFvKEO\UEK0RVEh\XiycnXzd4VlKGmwIHPobY5me2ViaHHtd5RmeiCYN{mgZ4VtdHNuIFnDOVA:OC5\|MUKg{txO	NHjHZ\|QzODV7NEi2Ni=>
V79MZ cells	M1\W[mZ2dmO2aX;uJIF{e2G7		M2TKWmlvcGmkaYTpc44hd2ZiaIXtZY4hS1mSMUHCNkBmgHC{ZYPz[YQhcW5iaHHtd5RmeiCYN{nNXkBk\WyuczD1d4lv\yBzMT3k[Y95gWOxcoTpZ49{fGW{b37lJJN2[nO2cnH0[UwhUUN3ME2wMlA3PyEQvF2=	NXfnNHFHOjR7MECyOFc>
V79MZh cells	NGnvcYFHfW6ldHnvckBie3OjeR?=		M2jGcmlvcGmkaYTpc44hd2ZiaIXtZY4hS1mSMUHCNkBmgHC{ZYPz[YQhcW5iaHHtd5RmeiCYN{nNXogh[2WubIOsJGlEPTB;MD6wOlch\|ryP	MnXDNlA2PTBzMUi=
human epidermal keratinocytes	NYnITWhHTnWwY4Tpc44h[XO\|YYm=		NV3UVGI5UW6qaXLpeIlwdiCxZjDDXXAzPEFzIHnuJIh2dWGwIHXwbYRmem2jbDDr[ZJifGmwb3P5eIV{NCCLQ{WwQVAvOTJ4IN88US=>	MWWyNFU6PDh4Mh?=
V79MZh cells	NWD2UFhlTnWwY4Tpc44h[XO\|YYm=		MVXJcohq[mm2aX;uJI9nKGi3bXHuJGN[WDFzQkGg[ZhxemW\|c3XkJIlvKGijbYP0[ZIhXjd7TWroJINmdGy\|LDDJR\|UxRTBwMUK3JO69VQ>?	NH7IOJYzODV3MEGxPC=>

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 (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

References

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Solubility (25°C)

In vitro


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. Click to purchase: Tween 80	30 mg/mL

Chemical Information

Molecular Weight	531.43
Formula	C₂₆H₂₈Cl₂N₄O₄
CAS No.	65277-42-1
Storage	3 years	-20°C	powder
Storage	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

Download Ketoconazole (R 41400) SDF

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Clinical Trial Information

NCT Number	Recruitment	Interventions	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT04869449	Recruiting	Drug: Ketoconazole	Glioblastoma\|Glioblastoma Multiforme\|Glioblastoma Multiforme of Brain\|Glioblastoma Multiforme Adult	Milton S. Hershey Medical Center	May 12 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 https://clinicaltrials.gov, updated on 2022-08-01)

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