Size | Price | Stock | Qty |
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100mg |
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250mg |
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500mg |
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1g |
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Other Sizes |
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Purity: ≥98%
Itraconazole (Orungal, Oriconazole, Sporanox, R51211; R-51211), a marketed triazole-based antifungal drug since 1984, is a potent inhibitor of CYP3A4 that has been widely used for the treatment of fungal infections.
ln Vitro |
HUVEC proliferation is inhibited by itraconazole (IC50 of 0.16 μM)[2]. In vitro, itraconazole suppresses the G1 phase of the endothelium cell cycle[1].
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ln Vivo |
In a mouse allograft model, intrathenazole therapy (75–100 mg/kg; oral gavage; twice daily; for 18 days; female outbred athymic nude mice) inhibits the growth of medulloblastoma and Hh pathway activity[1].
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Animal Protocol |
Animal/Disease Models: Female outbred athymic nude mice (6-7weeks old) injected with Ptch+/− cells[1]
Doses: 75 mg/kg, 100 mg/kg Route of Administration: po (oral gavage); twice per day; for 18 days Experimental Results: Suppressed Hh pathway activity and the growth of medulloblastoma in a mouse allograft model. |
References |
[1]. Kim, J., et al., Itraconazole, a commonly used antifungal that inhibits Hedgehog pathway activity and cancer growth. Cancer Cell, 2010. 17(4): p. 388-99.
[2]. Chong, C.R., et al., Inhibition of angiogenesis by the antifungal drug itraconazole. ACS Chem Biol, 2007. 2(4): p. 263-70. [3]. Pace JR, et al. Repurposing the Clinically Efficacious Antifungal Agent Itraconazole as an Anticancer Chemotherapeutic. J Med Chem. 2016 Apr 28;59(8):3635-49. [4]. Albulescu L, et al. Uncovering oxysterol-binding protein (OSBP) as a target of the anti-enteroviral compound TTP-8307. Antiviral Res. 2017;140:37-44. |
Molecular Formula |
C35H38CL2N8O4
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Molecular Weight |
705.65
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CAS # |
84625-61-6
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Related CAS # |
Hydroxy Itraconazole;112559-91-8;Hydroxy Itraconazole-d8;Itraconazole-d5;1217510-38-7;Itraconazole-d3;1217512-35-0;Itraconazole-d9;1309272-50-1
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SMILES |
O=C1N(C(CC)C)N=CN1C2=CC=C(N3CCN(C4=CC=C(OC[C@@H]5O[C@@](CN6N=CN=C6)(C7=CC=C(Cl)C=C7Cl)OC5)C=C4)CC3)C=C2
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InChi Key |
VHVPQPYKVGDNFY-ZPGVKDDISA-N
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InChi Code |
InChI=1S/C35H38Cl2N8O4/c1-3-25(2)45-34(46)44(24-40-45)29-7-5-27(6-8-29)41-14-16-42(17-15-41)28-9-11-30(12-10-28)47-19-31-20-48-35(49-31,21-43-23-38-22-39-43)32-13-4-26(36)18-33(32)37/h4-13,18,22-25,31H,3,14-17,19-21H2,1-2H3/t25?,31-,35-/m0/s1
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Chemical Name |
2-butan-2-yl-4-[4-[4-[4-[[(2R,4S)-2-(2,4-dichlorophenyl)-2-(1,2,4-triazol-1-ylmethyl)-1,3-dioxolan-4-yl]methoxy]phenyl]piperazin-1-yl]phenyl]-1,2,4-triazol-3-one
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Synonyms |
R51211, Orungal, Oriconazole, Sporanox, R 51211; R-51211, Itraconazole, Itraconazolum, Itraconazol, Itrizole
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 0.62 mg/mL (0.88 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 6.2 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 0.62 mg/mL (0.88 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 6.2 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. View More
Solubility in Formulation 3: 5% DMSO+70% PEG 300+ddH2O: 9mg/mL Solubility in Formulation 4: 20 mg/mL (28.34 mM) in 0.5% CMC-Na/saline water (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 1.4171 mL | 7.0857 mL | 14.1713 mL | |
5 mM | 0.2834 mL | 1.4171 mL | 2.8343 mL | |
10 mM | 0.1417 mL | 0.7086 mL | 1.4171 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
NCT05563766 | Not yet recruiting | Drug: Itraconazole | Esophageal Adenocarcinoma Esophageal Squamous Cell Carcinoma |
VA Office of Research and Development | May 1, 2024 | Phase 2 |
NCT05609253 | Recruiting | Drug: Itraconazole in capsule form Drug: Itraconazole in solution form |
Barrett Oesophagitis With Dysplasia | University of Kansas Medical Center | September 14, 2022 | Phase 1 |
NCT04018872 | Recruiting | Drug: Itraconazole | Esophagus Adenocarcinoma Esophagus Squamous Cell Carcinoma |
Dallas VA Medical Center | June 24, 2019 | Phase 2 |
NCT03572049 | Completed Has Results | Drug: SUBA itraconazole Drug: Conventional itraconazole |
Invasive Fungal Infections | University of Alabama at Birmingham | September 17, 2018 | Phase 2 Phase 3 |