Ketoconazole

製品コードS1353 バッチS135302

化学情報

	Synonyms	R 41400	Storage (From the date of receipt)	3 years -20°C powder 1 years -80°C in solvent
	化学式	C₂₆H₂₈Cl₂N₄O₄
	分子量	531.43	CAS No.	65277-42-1
Solubility (25°C)*	体外	Ethanol	7 mg/mL (13.17 mM)
		DMSO	3 mg/mL warmed with 50ºC water bath (5.64 mM)
		Water	Insoluble
* <1 mg/ml means slightly soluble or insoluble. * 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.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	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.
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]
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]
特徴	More active than both Econazole and Miconazole against Malassezia species.

プロトコル(参考用のみ)

キナーゼアッセイ	Whole Cell [³H]R1881 Binding Assay
キナーゼアッセイ	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
細胞アッセイ	細胞株	HT29-S-B6 colon cell
	濃度	25 μM
	反応時間	72 hours
	実験の流れ	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.
動物実験	動物モデル	male Wistar rats
	投薬量	25 mg/kg
	投与方法	Intraperitoneal injection

参考

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Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

NFX1-123: A potential therapeutic target in cervical cancer [ J Med Virol, 2023, 95(6):e28856]	PubMed: 37288708
TPX2 enhances the transcription factor activation of PXR and enhances the resistance of hepatocellular carcinoma cells to antitumor drugs [ Cell Death Dis, 2023, 14(1):64]	PubMed: 36707511
Hexokinase 2 confers radio-resistance in hepatocellular carcinoma by promoting autophagy-dependent degradation of AIMP2 [ Cell Death Dis, 2023, 14(8):488]	PubMed: 37524692
Genetically engineered human pituitary corticotroph tumor organoids exhibit divergent responses to glucocorticoid receptor modulators [ Transl Res, 2023, S1931-5244(23)00002-6]	PubMed: 36640905
Quantitative chemometric phenotyping of three-dimensional liver organoids by Raman spectral imaging [ Cell Rep Methods, 2023, 3(4):100440]	PubMed: 37159662
Quantitative chemometric phenotyping of three-dimensional liver organoids by Raman spectral imaging [ Cell Reports Methods, 2023, 10.1016/j.crmeth.2023.100440]	PubMed: None
Integration of glucose and cardiolipin anabolism confers radiation resistance of HCC [ Hepatology, 2022, 75(6):1386-1401]	PubMed: 34580888
Development of Human Pituitary Neuroendocrine Tumor Organoids to Facilitate Effective Targeted Treatments of Cushing's Disease [ Cells, 2022, 11(21)3344]	PubMed: 36359740
Terconazole, an Azole Antifungal Drug, Increases Cytotoxicity in Antimitotic Drug-Treated Resistant Cancer Cells with Substrate-Specific P-gp Inhibitory Activity [ Int J Mol Sci, 2022, 23(22)13809]	PubMed: 36430288
An FDA-Approved Antifungal, Ketoconazole, and Its Novel Derivative Suppress tGLI1-Mediated Breast Cancer Brain Metastasis by Inhibiting the DNA-Binding Activity of Brain Metastasis-Promoting Transcription Factor tGLI1 [ Cancers (Basel), 2022, 14(17)4256]	PubMed: 36077791

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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