| 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 |
Brown to black solid
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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 Vitro) |
DMSO: ~14.3 mg/mL (~42.2 mM; with ultrasonication and warming by heating to 160°C)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 1.43 mg/mL (4.23 mM) in 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), Clear solution; with ultrasonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (14.3 mg/mL) to 400 μL of PEG300 and mix well; then add 50 μL of Tween-80 and mix well; finally add 450 μL of physiological saline and 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: 1.43 mg/mL (4.23 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), Clear solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (14.3 mg/mL) to 900 μL of 20% SBE-β-CD saline and mix well. 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| 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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