Itraconazole

Name: Itraconazole
Brand: Tocris Bioscience
SKU: 5981

Tocris Bioscience, part of Bio-Techne | Catalog # 5981

Citations (6)

COA / SDS

SMO antagonist; acts at different binding site to cyclopamine (Cat No. 1623)

Key Product Details

Description:	SMO antagonist; acts at different binding site to cyclopamine (Cat No. 1623)
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
Purity:	≥98% (HPLC)
Molecular Weight:	705.63

View Full Technical Details for Itraconazole

Technical Data
Citations

Biological Activity for Itraconazole

Itraconazole is a 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 for Itraconazole

M. Wt	705.63
Formula	C₃₅H₃₈Cl₂N₈O₄
Storage	Store at -20°C
Purity	≥98% (HPLC)
CAS Number	84625-61-6
PubChem ID	3793
InChi Key	OPJPKRNKYPEBBY-YFWMVZQVSA-N
Smiles	CCC(N1N=CN(C2=CC=C(N3CCN(C4=CC=C(C=C4)OC[C@H]5CO[C@@](O5)(C6=C(C=C(C=C6)Cl)Cl)CN7C=NC=N7)CC3)C=C2)C1=O)C.CCC(N8N=CN(C9=CC=C(N%10CCN(C%11=CC=C(C=C%11)OC[C@@H]%12CO[C@](O%12)(C%13=C(C=C(C=C%13)Cl)Cl)CN%14C=NC=N%14)CC%10)C=C9)C8=O)C

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility for Itraconazole

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
Solubility	DMSO	14.11	20 with gentle warming

Preparing Stock Solutions for Itraconazole

The following data is based on the product molecular weight 705.63.

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
0.2 mM	7.09 mL	35.43 mL	70.86 mL
1 mM	1.42 mL	7.09 mL	14.17 mL
2 mM	0.71 mL	3.54 mL	7.09 mL
10 mM	0.14 mL	0.71 mL	1.42 mL

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References for Itraconazole

References are publications that support the biological activity of the product.

Pace Repurposing the clinically efficacious antifungal agent itracon. as an anticancer chemotherapeutic. J.Med.Chem. 2016 PMID: 27014922
Kim Itraconazole and arsenic trioxide inhibit Hedgehog pathway activation and tumor growth associated with acquired resistance to smoothened antagonists. Cancer Cell 2013 PMID: 23291299
Kim Itraconazole, a commonly used antifungal that inhibits Hedgehog pathway activity and cancer growth. Cancer Cell 2010 PMID: 20385363
Chong Inhibition of angiogenesis by the antifungal drug itracon. ACS Chem.Biol. 2007 PMID: 17432820