Itraconazole

Cat. No. 5981

Itraconazole C35H38Cl2N8O4 [84625-61-6]

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Chemical Name: 4-[4-[4-[4-[[2-(2,4-Dichlorophenyl)-2-(1H-1,2,4-triazol-1-ylmethyl)-1,3-dioxolan-4-yl]methoxy]phenyl]-1-piperazinyl]phenyl]-2,4-dihydro-2-(1-methylpropyl)-3H-1,2,4-triazol-3-one

Biological Activity

SMO antagonist (IC50 = 690 nM); acts at different binding site to cyclopamine (Cat. No. 1623). Also cytochrome p450 inhibitor (IC50 = 16-26 nM). Inhibits cell cycle at G1 phase in vitro and blocks angiogenesis in vivo (IC50 = 160 nM). Antifungal.

Technical Data

M.Wt:
705.63
Formula:
C35H38Cl2N8O4
Solubility:
Soluble to 20 mM in DMSO with gentle warming
Purity:
>99 %
Storage:
Store at -20°C
CAS No:
84625-61-6

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.

Certificate of Analysis / Product Datasheet / Safety Datasheet

References are publications that support the products' biological activity.

Pace et al (2016) Repurposing the clinically efficacious antifungal agent itraconazole as an anticancer chemotherapeutic. J.Med.Chem. 59 3635. PMID: 27014922.

Kim et al (2013) Itraconazole and arsenic trioxide inhibit Hedgehog pathway activation and tumor growth associated with acquired resistance to smoothened antagonists. Cancer Cell 23 23. PMID: 23291299.

Kim et al (2010) Itraconazole, a commonly used antifungal that inhibits Hedgehog pathway activity and cancer growth. Cancer Cell 17 388. PMID: 20385363.

Chong et al (2007) Inhibition of angiogenesis by the antifungal drug itraconazole. ACS Chem.Biol. 2 263. PMID: 17432820.

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Keywords: Itraconazole, supplier, SMO, antagonists, smoothened, receptors, cytochrome, p450, inhiibitors, inhibits, cell, cycle, angiogenesis, antifungals, hedgehog, Tocris Bioscience, Smoothened Receptor Antagonist products

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