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Itraconazole | Autophagy inducer / Inhibits glioblastoma growth

Itraconazole (84625-61-6) inhibits the conversion of lanosterol to ergosterol via inhibition of the 14-α demethylase, a cytochrome P-450 enzyme.1 Clinically useful antifungal agent. It inhibits the proliferation of glioblastoma cells in vitro and in vivo by inducing autophagic progression via inhibiting the trafficking of cholesterol from late endosomes and lysosomes to the plasma membrane.2 Inhibits the hedgehog pathway by binding to Smoothened (SMO) via a mechanism distinct from that of cyclopamine.3 Inhibits angiogenesis via inhibiting the binding of VEGF to VEGFR2.4

References/Citations

1) Vanden Bossche et al. (1993), Effects of itraconazole on cytochrome P-450-dependent sterol 14 alpha-demethylation and reduction of 3-ketosteroids in Cryptococcus neoformans; Antimicrob. Agents Chemother., 37 2101
2) Liu et al. (2014), Itraconazole suppresses the growth of glioblastoma through induction of autophagy: involvement of abnormal cholesterol trafficking; Autophagy, 10 1241
3) Kim et al. (2010), Itraconazole, a commonly used antifungal that inhibits Hedgehog pathway activity and cancer growth; Cancer Cell, 17 388
4) Nacev et al. (2011), The antifungal drug itraconazole inhibits vascular endothelial growth factor receptor 2 (VEGFR2) glycosylation, trafficking, and signaling in endothelial cells; J. Biol. Chem., 286 44045

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Catalog#  10-2033

$40.00
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CAS:
84625-61-6
Catalog Number:
10-2033
Activity:
Autophagy inducer / Inhibits glioblastoma growth
Alternate Names:
Oriconazole; R51211
Molecular Weight:
705.63
Molecular Formula:
C35H36Cl2N8O4
Solubility:
Soluble in DMSO (up to 1.5 mg/ml with warming)
Physical Properties:
White solid
Purity:
98% by HPLC
NMR (Conforms)
Storage Temperature:
-20°C (des.)
Stability:
Stable for 1 year as supplied. Solutions in DMSO may be stored at -20°C for up to 1 month.
Shipping Code:
RT
Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications.

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