| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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EOAI3402143 (EOAI 3402143; EOAI-3402143) is a novel and potent inhibitor of Usp9x, Usp24 and deubiquitinase (DUB) with potential anticancer activity. It dose-dependently inhibits Usp9x and Usp24, leading to cancer cell apoptosis and tumor regression in mice.
| Targets |
Usp5;Usp9x;Usp24
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|---|---|
| ln Vitro |
Strong Usp9x and Usp5 inhibitory activity is maintained by EOAI3402143 [1].EOAI3402143 increases tumor cell apoptosis and dose-dependently inhibits Usp9x and Usp24 activity[2].When UM-2, UM-6, UM-16, and UM-76 are treated with the Usp9x inhibitor EOAI3402143 (G9), there is a dose-dependent suppression of cell survival. In contrast, when UM-2 3D colony growth is compared to untreated vehicle controls, EOAI3402143 at 600 nM completely suppresses it[3].
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| ln Vivo |
The impact of EOAI3402143 (G9) treatment is studied on human MIAPACA2 tumor xenografts in order to investigate this potential. NSG mice receive a subcutaneous injection of human MIAPACA2 cells. Caliper measurements track the primary tumor development. Once measurable, mice are divided into two groups and given either G9 at a dose of 15 mg/kg or vehicle control (PEG300/DMSO). Throughout treatment, the animal's weight, mobility, behavior, and tumor growth are all observed.Simultaneously, 8041 tumors in mice are cultured and exposed to the same G9 treatment and tumor observation schedule as the human MIAPACA2 xenografts. In line with the in vitro results, Usp9x inhibition suppresses the growth of tumors in human tumor xenografts; however, no discernible effect on the growth of 8041 tumor xenografts is noted. Nevertheless, EOAI3402143 treatment effectively inhibits Usp9x activity in both human MIAPACA2 and mouse 8041 xenograft tumors[3].
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| Cell Assay |
In a 96-well plate, 5000 cells per well of UM-2, UM-6, UM-16, and UM-76 are seeded along with the indicated concentrations of EOAI3402143 (1, 2, 3, 4, and 5 μM) and incubated for three days at 37°C in a CO2 incubator. For two hours at 37°C, twenty microliters of a 5 g/L MTT solution are added to each well. After the cells are lysed in 10% SDS buffer, a microplate reader is used to measure the absorbance at 570 nm in relation to a reference wavelength of 630 nm. Cells are plated in triplicates and the samples are processed for the MTT assay on days 0, 1, 2, 3, and 4 in order to assess proliferation using the MTT assay[3].
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| Animal Protocol |
Mice[3]
Mid-dorsally, 2×10^6 8041 or 5×10^6 MIAPACA2 cells are injected into NSG [NOD/SCID/IL2r-g (null)] mice in 0.1 mL of Matrigel/DMEM suspension. After allowing tumors to grow to a size of approximately 100 mm^3, mice with tumors of the same size are matched and assigned to treatment groups, with five mice per vehicle or EOAI3402143, for mice bearing 8041 tumors and four mice per treatment group for mice bearing MIAPACA2 tumors. By intraperitoneal injection, EOAI3402143 is given at a dose of 15 mg/kg every other day in DMSO:PEG300 (1:1). Tumor volume is computed and tumor size is tracked twice a week using caliper measurements[3]. |
| References |
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| Molecular Formula |
C25H28CL2N4O3
|
|---|---|
| Molecular Weight |
503.424
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| Exact Mass |
502.15
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| Elemental Analysis |
C, 59.65; H, 5.61; Cl, 14.08; N, 11.13; O, 9.53
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| CAS # |
1699750-95-2
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| Related CAS # |
1699750-95-2;
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| Appearance |
Solid powder
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| SMILES |
O=C(NC(C1=CC=C(OCCN2CCOCC2)C=C1)CCC)/C(C#N)=C/C3=NC(Cl)=CC=C3Cl
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| InChi Key |
IIKVQQNZHGBYGQ-KNTRCKAVSA-N
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| InChi Code |
InChI=1S/C25H28Cl2N4O3/c1-2-3-22(30-25(32)19(17-28)16-23-21(26)8-9-24(27)29-23)18-4-6-20(7-5-18)34-15-12-31-10-13-33-14-11-31/h4-9,16,22H,2-3,10-15H2,1H3,(H,30,32)/b19-16+
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| Chemical Name |
2-Cyano-3-(3,6-dichloro-pyridin-2-yl)-N-{1-[4-(2-morpholin-4-yl-ethoxy)-phenyl]-butyl}-acrylamide
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| Synonyms |
EOAI 402143; EOAI 3402143; EOAI-3402143; EOAI3402143; G9 free base; G9 free base
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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 |
| 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 : 50~100 mg/mL ( 99.32~198.64 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 | 1.9864 mL | 9.9321 mL | 19.8641 mL | |
| 5 mM | 0.3973 mL | 1.9864 mL | 3.9728 mL | |
| 10 mM | 0.1986 mL | 0.9932 mL | 1.9864 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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