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Ketoconazole (R 41400)

Name: Ketoconazole (R 41400)
Brand: Selleck Chemicals
SKU: S1353
Rating: 5 (11 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 11 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	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
CHO cells	M4rPTmZ2dmO2aX;uJIF{e2G7		NXLQT5YxUW6qaXLpeIlwdiCxZjDDXXAzPEFzIHX4dJJme3OnZDDpckBEUE9iY3XscJMtKEmFNUC9NE42OiEQvF2=	NGqwOIYzODZ3NU[yOi=>
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>

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	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. 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	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 https://clinicaltrials.gov, updated on 2022-01-17)

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