Catalog No.S2476 Synonyms: R 51211
Molecular Weight(MW): 705.65031
Itraconazole is a relatively potent inhibitor of CYP3A4 with IC50 of 6.1 nM, used as a triazole antifungal agent.
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Resistance to itraconazole in MA cells. The parental SUM149-Luc cell line and MA1 cells were treated in parallel with 1 mM itraconazole for 9 days (which killed most of the cells in the parental cell line) and were allowed to recover and grow in a drug-free medium for 5 days before being stained. Since itraconazole was ineffective in killing MA1 cells, the cells grew into a continuous monolayer rather than colonies.
PLoS One, 2014, 9(10):e109487.. Itraconazole purchased from Selleck.
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Choose Selective P450 (e.g. CYP17) Inhibitors
|Description||Itraconazole is a relatively potent inhibitor of CYP3A4 with IC50 of 6.1 nM, used as a triazole antifungal agent.|
Itraconazole is metabolized into hydroxy-itraconazole (OH-ITZ), a known in vivo metabolite of ITZ, and two new metabolites: keto-itraconazole (keto-ITZ) and N-desalkyl-itraconazole (ND-ITZ). Itraconazole is a substrate for CYP3A in vitro and to characterize the metabolites generated. Itraconazole exhibits an unbound Km of 3.9 nM for CYP3A. Itraconazole metabolites are as potent as or more potent CYP3A4 inhibitors than ITZ itself.  Itraconazole appears to act on the essential Hh pathway component Smoothened (SMO) by a mechanism distinct from that of cyclopamine and other known SMO antagonists, and prevents the ciliary accumulation of SMO normally caused by Hh stimulation.  Itraconazole is active against 60 clinical isolates of Aspergillus spp. with geometric mean (GM) MICs of 0.25 mg/mL.  Itraconazole acts primarily by impairing the synthesis of ergosterol, resulting in a defective fungal cell membrane with altered permeability and function. Itraconazole is effective for a wide variety of mycotic infections and some fungal meningeal infections.  Itraconazole has an affinity for mammalian cytochrome P-450 enzymes as well as for fungal P-450-dependent enzyme, and thus has the potential for clinically important interactions (e.g., astemizole, terfenadine, rifampin, oral contraceptives, H2 receptor antagonists, warfarin, cyclosporine). 
|In vivo||Itraconazole, like other Hh pathway antagonists, can suppress Hh pathway activity and the growth of medulloblastoma in a mouse allograft model. |
-  Isoherranen N, et al. Drug Metab Dispos, 2004, 32(10), 1121-1131.
-  Kim J, et al. Cancer Cell, 2010, 17(4), 388-399.
-  Oakley KL, et al. Antimicrob Agents Chemother, 1997, 41(5), 1124-1126.
|In vitro||DMSO||7 mg/mL warmed (9.91 mM)|
|In vivo||Add solvents to the product individually and in order:
5% DMSO+70% PEG 300+ddH2O
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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* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).
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Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT02130661||Withdrawn||Alzheimers Disease||GlaxoSmithKline||October 2017||Phase 1|
|NCT03048110||Not yet recruiting||Biological Availability||Bayer|Orion Corporation, Orion Pharma||February 2017||Phase 1|
|NCT02699723||Not yet recruiting||Skin Basal Cell Carcinoma||Jean Yuh Tang|National Cancer Institute (NCI)|Stanford University||January 2017||--|
|NCT02975037||Not yet recruiting||Healthy||Seoul National University Hospital||December 2016||Phase 4|
|NCT02989389||Recruiting||Healthy||Eli Lilly and Company||December 2016||Phase 1|
|NCT02895529||Recruiting||Hematologic Neoplasms||Xian-Janssen Pharmaceutical Ltd.||November 2016||Phase 4|
Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.
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Frequently Asked Questions
We are finding the best vehicle to administer Itraconazole to mice. We want a mild vehicle (unlike DMSO) which resembles water, PBS, saline (for i.p/ injection) or methyl cellulose (for oral).
We are not able to dissolve S2476 Itraconazole clearly without DMSO. For oral gavage, this compound can be dissolved in 1% CMC Na at 20mg/ml as a homogeneous suspension.