Catalog Number: 5981
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:
  • Formula:
  • Solubility:
    Soluble to 20 mM in DMSO with gentle warming
  • Purity:
  • Storage:
    Store at -20°C
  • CAS No:
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.
Background References
  1. Itraconazole, a commonly used antifungal that inhibits Hedgehog pathway activity and cancer growth.
    Kim et al.
    Cancer Cell, 2010;17:388
  2. Inhibition of angiogenesis by the antifungal drug itraconazole.
    Chong et al.
    ACS Chem.Biol., 2007;2:263
  3. Repurposing the clinically efficacious antifungal agent itraconazole as an anticancer chemotherapeutic.
    Pace et al.
    J.Med.Chem., 2016;59:3635
  4. Itraconazole and arsenic trioxide inhibit Hedgehog pathway activation and tumor growth associated with acquired resistance to smoothened antagonists.
    Kim et al.
    Cancer Cell, 2013;23:23
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