1. Anti-infection
    Stem Cell/Wnt
    Metabolic Enzyme/Protease
    Autophagy
  2. Fungal
    Hedgehog
    Cytochrome P450
    Autophagy
    Antibiotic
  3. Itraconazole

Itraconazole (Synonyms: R51211)

Cat. No.: HY-17514 Purity: 99.15%
Handling Instructions

Itraconazole (R51211) is a triazole antifungal agent and a potent and orally active Hedgehog (Hh) signaling pathway antagonist with an IC50 of ~800 nM. Itraconazole potently inhibits lanosterol 14α-demethylase (cytochrome P450 enzyme), thereby inhibits the oxidative conversion of lanosterol to ergosterol. Itraconazole has anticancer and antiangiogenic effects.

For research use only. We do not sell to patients.

Itraconazole Chemical Structure

Itraconazole Chemical Structure

CAS No. : 84625-61-6

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Customer Review

Based on 5 publication(s) in Google Scholar

Other Forms of Itraconazole:

Top Publications Citing Use of Products

    Itraconazole purchased from MCE. Usage Cited in: J Exp Clin Cancer Res. 2019 Sep 13;38(1):404.

    SCP2-OE GH3 cells are incubated with 10 μM itraconazole (ITR) for 48 h. The distribution of cholesterol (blue) in the different groups (Vector, SCP2-OE and SCP2-OE + ITR) are examined by filipin staining and laser confocal microscopy. Green signal, GH staining; red signal, PI nuclear staining. Scale bar, 10 μm.
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    Description

    Itraconazole (R51211) is a triazole antifungal agent and a potent and orally active Hedgehog (Hh) signaling pathway antagonist with an IC50 of ~800 nM. Itraconazole potently inhibits lanosterol 14α-demethylase (cytochrome P450 enzyme), thereby inhibits the oxidative conversion of lanosterol to ergosterol. Itraconazole has anticancer and antiangiogenic effects[1][2][3].

    IC50 & Target

    Fungal[1]
    IC50: ~800 nM (Hedgehog signaling pathway)[1]
    14α-demethylase (cytochrome P450 enzyme)[3]

    In Vitro

    Itraconazole has anti-proliferation of HUVEC (IC50 of 0.16 μM)[2].
    Itraconazole inhibits endothelial cell cycle progression at the G1 phase in vitro[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    In Vivo

    Itraconazole (75-100 mg/kg; oral gavage; twice per day; for 18 days; female outbred athymic nude mice) treatment suppresses Hh pathway activity and the growth of medulloblastoma in a mouse allograft model[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Model: Female outbred athymic nude mice (6-7-week-old) injected with Ptch+/− cells[1]
    Dosage: 75 mg/kg, 100 mg/kg
    Administration: Oral gavage; twice per day; for 18 days
    Result: Suppressed Hh pathway activity and the growth of medulloblastoma in a mouse allograft model.
    Clinical Trial
    Molecular Weight

    705.63

    Formula

    C₃₅H₃₈Cl₂N₈O₄

    CAS No.

    84625-61-6

    SMILES

    ClC1=C(C=CC(Cl)=C1)[[email protected]@]2(O[[email protected]@H](COC3=CC=C(N4CCN(C5=CC=C(N(C=NN6C(C)CC)C6=O)C=C5)CC4)C=C3)CO2)CN7C=NC=N7

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage

    4°C, protect from light

    *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

    Solvent & Solubility
    In Vitro: 

    DMSO : 6.25 mg/mL (8.86 mM; Need ultrasonic)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.4172 mL 7.0859 mL 14.1717 mL
    5 mM 0.2834 mL 1.4172 mL 2.8343 mL
    10 mM --- --- ---
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      Add each solvent one by one:  0.5% CMC-Na/saline water

      Solubility: 20 mg/mL (28.34 mM); Suspended solution; Need ultrasonic

    • 2.

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: ≥ 0.62 mg/mL (0.88 mM); Clear solution

    • 3.

      Add each solvent one by one:  10% DMSO    90% corn oil

      Solubility: ≥ 0.62 mg/mL (0.88 mM); Clear solution

    *All of the co-solvents are provided by MCE.
    References
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    Keywords:

    ItraconazoleR51211R 51211R-51211FungalHedgehogCytochrome P450AutophagyAntibioticCYPsTriazoleantifungalHhanticancerCYP-450antiangiogenic14α-demethylaselanosterolergosterolInhibitorinhibitorinhibit

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    Product Name:
    Itraconazole
    Cat. No.:
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