ERG245
Based on 1 Customer Validation
ERG245 is a selective amino acid aminotransferase (BCAT1) inhibitor with a human IC50 of 0.5 nM. ERG245 enhances oxidative phosphorylation (OXPHOS) in CD8+ T cells by specifically inhibiting BCAT1 activity, thereby increasing the cytotoxicity of CD8+ T cells. ERG245 shows anti-inflammatory and anti-tumor activities. ERG245 can be used for the researches of cancer anf inflammation, such as colitis and colon cancer.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.49%
- Fòrmula: C17H15BrO3
- Peso molecular:347.20
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Almacenamiento:
4°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
Actividad biológica
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BCAT1 0.5 nM (IC50) |
ERG245 (0.1-10 nM; 10 min) potently and selectively inhibits recombinant human BCAT1 with an IC50 of ~0.5 nM, while showing minimal activity against recombinant human BCAT2[1].
ERG245 (200 μM) reduces IFNγ and granzyme B production in activated human CD8+ T cells from donors[1].
ERG245 (100 μM; 72-96 h) partially inhibits the proliferation of activated human CD8+ T cells, as measured by reduced Weighted Proliferation Index[1].
ERG245 (100 μM; 24 h) increases mitochondrial OXPHOS in activated human CD8+ T cells after 24 hours[1].
ERG245 (400 μM; 60 min) induces a rapid increase in mitochondrial iron levels in activated wild-type Jurkat cells[1].
ERG245 (200 μM) increases cytosolic aconitase 1 (ACO1) activity in activated human CD8+ T cells[1].
ERG245 (200 μM; 24 h) partially prevents the development of a terminally exhausted phenotype in human CD8+ T cells generated via repeated TGF-β-supplemented activation, reducing CD8+ PD-1+ TIM3+ GZMB+ cell frequency and CXCL13 secretion[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Human CD8+ (hCD8+) T cells
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Concentration:100 μM
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Incubation Time:72, 96 h
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Result:Reduced the Weighted Proliferation Index of activated hCD8+ T cells significantly, indicating partial inhibition of cell expansion.
ERG245 (5 mg/kg; i.p.; twice daily on days 0, 1, and 2) combined with anti-PD-1 induces complete, durable tumor regressions in 83% of mice in the CT26 syngeneic colon cancer model and enhances the frequency of cytotoxic CD8+ T cells in the CT26 tumor microenvironment[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6 (female, 18-20 g, acute Dextran sulfate sodium-induced colitis)[1]
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Dosage:5 mg/kg
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Administration:i.p.; twice daily; 6 days
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Result:Reduced colon mass/length ratio.
Decreased the frequency of activated CD8+ CD25+ T cells in mesenteric lymph nodes.
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Animal Model:Balb/c (female, 6-7 weeks old, syngeneic CT26 colorectal cancer)[1]
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Dosage:5 mg/kg (ERG245); 10 mg/kg (anti-PD-1)
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Administration:i.p.; twice daily on days 0, 1, and 2 (ERG245); i.p.; on days 0, 4, 7, and 11 (anti-PD-1)
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Result:Did not alter tumor growth kinetics or survival as monotherapy.
Resulted in 83% (5/6) complete tumor regression rate when combined with anti-PD-1, compared to 17% (1/6) with anti-PD-1 monotherapy.
Prevented tumor growth after re-inoculation in mice with complete tumor regression, indicating immunological memory.
Chemical Information
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Appearance Solid
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Peso molecular 347.20
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Fòrmula C17H15BrO3
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Color White to off-white
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SMILES
OC(CCC(C(C1=CC=C(Br)C=C1)=O)C2=CC=CC=C2)=O
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
4°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
Solvente y solubilidad
DMSO : 100 mg/mL (288.02 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (7.20 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (7.20 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureza y Documentación
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Ficha de datos (277 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instrucciones de manejo (2659 KB)
Referencias
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 2.8802 mL | 14.4009 mL | 28.8018 mL | 72.0046 mL |
| 5 mM | 0.5760 mL | 2.8802 mL | 5.7604 mL | 14.4009 mL | |
| 10 mM | 0.2880 mL | 1.4401 mL | 2.8802 mL | 7.2005 mL | |
| 15 mM | 0.1920 mL | 0.9601 mL | 1.9201 mL | 4.8003 mL | |
| 20 mM | 0.1440 mL | 0.7200 mL | 1.4401 mL | 3.6002 mL | |
| 25 mM | 0.1152 mL | 0.5760 mL | 1.1521 mL | 2.8802 mL | |
| 30 mM | 0.0960 mL | 0.4800 mL | 0.9601 mL | 2.4002 mL | |
| 40 mM | 0.0720 mL | 0.3600 mL | 0.7200 mL | 1.8001 mL | |
| 50 mM | 0.0576 mL | 0.2880 mL | 0.5760 mL | 1.4401 mL | |
| 60 mM | 0.0480 mL | 0.2400 mL | 0.4800 mL | 1.2001 mL | |
| 80 mM | 0.0360 mL | 0.1800 mL | 0.3600 mL | 0.9001 mL | |
| 100 mM | 0.0288 mL | 0.1440 mL | 0.2880 mL | 0.7200 mL |
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