| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
The compound targets the ERG (ETS-related gene) protein and the RIOK2 (RIO kinase 2) protein. It is reported as a dual inhibitor, with IC50 values of 0.17 uM for ERG and 0.13 uM for RIOK2 in VCaP cells.
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|---|---|
| ln Vitro |
In VCaP cells, ERGi-USU-6 mesylate exhibits potent growth-inhibitory activity (IC50 = 0.089-0.17 uM). It demonstrates selective antiproliferative activity against ERG-positive prostate cancer cell lines.
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| ln Vivo |
Cellular assays in VCaP cells show the compound's growth-inhibitory effects, indicating strong antiproliferative and anticancer activity. It has not been extensively profiled in standard animal efficacy studies.
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| Enzyme Assay |
Not specified for this compound. Standard target engagement assays for kinase targets like RIOK2 can employ radioligand binding or TR-FRET (Time-Resolved Fluorescence Resonance Energy Transfer) methods.
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| Cell Assay |
The standard assay used to evaluate ERGi-USU-6 mesylate is a cell viability assay. VCaP cells are treated with the compound for 120 hours, and inhibition of cell growth is assessed using a Cell Glow ATPase assay.
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| Animal Protocol |
In vivo animal studies using this compound have not been reported. Preclinical efficacy assessment for such inhibitors typically involves subcutaneous xenograft models in immunocompromised mice to evaluate tumor growth inhibition.
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| ADME/Pharmacokinetics |
PK data for ERGi-USU-6 mesylate are not available. However, the mesylate salt formulation is expected to improve the compound's aqueous solubility and overall drug-like properties compared to the free base.
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| Toxicity/Toxicokinetics |
Toxicity data for ERGi-USU-6 mesylate are not detailed. While the parent compound is a potent inhibitor, toxicity studies have not been reported. The in vitro assays indicate it is active against cancer cells, suggesting potential therapeutic indices.
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| References |
[1]. Eldhose B, et al. New Selective Inhibitors of ERG Positive Prostate Cancer: ERGi-USU-6 Salt Derivatives. ACS Med Chem Lett. 2021 Oct 19;12(11):1703-1709.
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| Additional Infomation |
ERGi-USU-6 mesylate is a research compound and has no approved clinical status. The suffix "mesylate" denotes it is the methanesulfonic acid salt form of the free base ERGi-USU-6. It is used exclusively for research purposes.
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| Molecular Formula |
C14H18N4O4S
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|---|---|
| Molecular Weight |
338.38
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| Exact Mass |
338.105
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| CAS # |
2756327-67-8
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| PubChem CID |
163198555
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| Appearance |
Typically exists as solid at room temperature
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
23
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| Complexity |
375
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CN(C)C1=CC(=C(C=C1)N=NC2=CC=CC=N2)O.CS(=O)(=O)O
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| InChi Key |
UKIKMFBVZICNPO-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C13H14N4O.CH4O3S/c1-17(2)10-6-7-11(12(18)9-10)15-16-13-5-3-4-8-14-13;1-5(2,3)4/h3-9,18H,1-2H3;1H3,(H,2,3,4)
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| Chemical Name |
5-(dimethylamino)-2-(pyridin-2-yldiazenyl)phenol;methanesulfonic acid
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| 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 Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.9553 mL | 14.7763 mL | 29.5526 mL | |
| 5 mM | 0.5911 mL | 2.9553 mL | 5.9105 mL | |
| 10 mM | 0.2955 mL | 1.4776 mL | 2.9553 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.
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