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| 25mg |
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Purity: ≥98%
AZ1 is a novel and potent dual inhibitor of the USP25/28 deubiquitinating enzyme subfamily with potential anticancer activity. It has been reported that Ubiquitin specific proteases (USPs) are linked to critical axes for therapeutic intervention and USP28 is required for c-Myc stability, suggesting that USP28 inhibition may represent a novel approach to targeting this so far undruggable oncogene.
| Targets |
USP25(IC50= 0.7 μM);USP28(IC50= 0.6 μM)
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|---|---|
| ln Vivo |
The USP25/28 inhibitor AZ1 (AZ1; 40 mg/kg; gavage; daily; for 7 days) prevents diarrhea and weight loss brought on by dextran sulfate sodium (DSS) as well as impaired colon shortening[1].
Colon tumor numbers are significantly decreased by USP25/28 inhibitor AZ1 (20 mg/kg/day; gavage; 6 times a week in the 1, 3, and 6 weeks) treatment. Tumors exhibit elevated SOCS3 levels, decreased pSTAT3 levels, and Wnt-related gene expression. AZ1 gavage is not effective in treating spontaneous colitis in Il10-/-mice or DSS-induced colitis in Usp25-/-mice[1]. The USP25/28 inhibitor AZ1 (20 mg/kg/day; gavage; every 3 days from 13–20 weeks) prolongs the survival of AOM/Vil-Cre;Trp53fl/fl (VP) mice and significantly inhibits colon tumorigenesis. Treatment with AZ1 has little effect on tumorigenesis in the background deficient in USP25[1]. |
| Animal Protocol |
Animal Model: Male Usp25+/+ and Usp25-/- mice aged 12 weeks[1]
Dosage: 40 mg/kg Administration: Gavage; daily; for 7 days Result: In comparison to control mice, the colons of Usp25-/-mice showed increased expression of proinflammatory cytokines and antibacterial peptides, and they were shielded from the weight loss and diarrhea caused by dextran sulfate sodium (DSS). They also showed impaired colon shortening. |
| References |
| Molecular Formula |
C17H16BRF4NO2
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|---|---|
| Molecular Weight |
422.22
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| Exact Mass |
421.0301
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| CAS # |
2165322-94-9
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| Related CAS # |
2165322-94-9
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| SMILES |
C1=CC(=C(C=C1COC2=C(C=C(C=C2)Br)CNCCO)C(F)(F)F)F
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| InChi Key |
ITHSFXDGKQYOED-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C17H16BrF4NO2/c18-13-2-4-16(12(8-13)9-23-5-6-24)25-10-11-1-3-15(19)14(7-11)17(20,21)22/h1-4,7-8,23-24H,5-6,9-10H2
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| Chemical Name |
2-(5-Bromo-2-(4-fluoro-3-(trifluoromethyl)benzyloxy)benzylamino)ethanol
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| Synonyms |
AZ1 AZ-1 AZ 1 AZ1
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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) |
DMSO : 84~250 mg/mL ( 198.95~592.12 mM )
Ethanol : ~84 mg/mL |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.93 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 20.8 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: 2.08 mg/mL (4.93 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (4.93 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3684 mL | 11.8422 mL | 23.6843 mL | |
| 5 mM | 0.4737 mL | 2.3684 mL | 4.7369 mL | |
| 10 mM | 0.2368 mL | 1.1842 mL | 2.3684 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 |
| NCT00940589 | Completed | Drug: Circadin Drug: Placebo |
Alzheimer's Disease Sleep Disorder |
Neurim Pharmaceuticals Ltd. | September 2009 | Phase 2 |
Products are for research use only; We do not sell to patients
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