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EOAI3402143 Tosylate (EOAI-3402143;
EOAI 3402143), the Tosylate salt of EOAI-3402143, is a potent inhibitor of Usp9x, Usp24 and
deubiquitinase (DUB) with potential antitumor activity. It
dose-dependently inhibits Usp9x and Usp24, leading to cancer cell
apoptosis and tumor regression in mice.
| ln Vitro |
Strong Usp9x and Usp5 inhibitory action is retained by EOAI3402143 [1]. Tumor cell apoptosis is increased and Usp9x and Usp24 activities are dose-dependently inhibited by EOAI3402143 [2]. When UM-2, UM-6, UM-16, and UM-76 were treated with the Usp9x inhibitor EOAI3402143 (G9), cell survival was dose-dependently reduced in comparison to the untreated vehicle; however, UM-2 3D colony growth control was entirely blocked by 600 nM EOAI3402143.
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| ln Vivo |
The impact of EOAI3402143 (G9) therapy on human MIAPACA2 tumor xenografts was investigated in order to investigate this possibility. NSG mice received subcutaneous injections of human MIAPCA2 cells. Caliper measurements were used to track the primary tumor development. Once the tumor was detectable, mice were split into two groups and given either 15 mg/kg of G9 or a vehicle control (PEG300/DMSO). While receiving treatment, keep an eye on the animal's body weight, temperament, and tumor growth. Simultaneously, mice bearing 8041 tumors were generated and subjected to G9 therapy and tumor observation protocols akin to those employed with human MIAPACA2 xenografts. Usp9x inhibition inhibited the growth of tumors in human tumor xenografts, which is consistent with in vitro studies. However, there was no discernible effect on the growth of tumors in 8041 tumor xenografts; however, EOAI3402143 treatment effectively inhibited the growth of tumors in both human MIAPACA2 and 2 Usp9x activity. and 8041 xenograft tumors in mice [3].
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| References |
[1]. Potu H, et al. Usp5 links suppression of p53 and FAS levels in melanoma to the BRAF pathway. Oncotarget. 2014 Jul 30;5(14):5559-69.
[2]. Peterson LF, et al. Targeting deubiquitinase activity with a novel small-molecule inhibitor as therapy for B-cell malignancies. Blood. 2015 Jun 4;125(23):3588-97. [3]. Pal A, et al. Usp9x Promotes Survival in Human Pancreatic Cancer and Its Inhibition Suppresses Pancreatic Ductal Adenocarcinoma In Vivo Tumor Growth. Neoplasia. 2018 Feb;20(2):152-164 |
| Molecular Formula |
C32H36CL2N4O6S
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|---|---|
| Molecular Weight |
675.62
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| Exact Mass |
674.1733
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| CAS # |
1699750-95-2
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| Related CAS # |
1699750-95-2;
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| SMILES |
ClC1=CC=C(N=C1/C=C(\C#N)/C(NC(C1C=CC(=CC=1)OCCN1CCOCC1)CCC)=O)Cl.S(C1C=CC(C)=CC=1)(=O)(=O)O
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| Synonyms |
EOAI-3402143 Tosylate EOAI 3402143 Tosylate EOAI 402143 Tosylate
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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 : ~50 mg/mL (~99.32 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.97 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 25.0 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: ≥ 2.5 mg/mL (4.97 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 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. View More
Solubility in Formulation 3: 10 mg/mL (19.86 mM) in 50% PEG300 50% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.4801 mL | 7.4006 mL | 14.8012 mL | |
| 5 mM | 0.2960 mL | 1.4801 mL | 2.9602 mL | |
| 10 mM | 0.1480 mL | 0.7401 mL | 1.4801 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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