D574-0246
Based on 1 Customer Validation
D574-0246 is a dual-activity inhibitor of OXCT1, inhibiting both the ketolytic and succinyltransferase activities of OXCT1. D574-0246 reduces substrate-specific (LACTB K284) and global protein succinylation and decreases OXCT1 ketolytic activity in HepG2 cells. D574-0246 inhibits the viability of HCC cells (IC50: 16.49 μM in PLC cells, 6.656 μM in HepG2 cells). D574-0246 exerts anti-tumor efficacy in nude mice bearing OXCT1-overexpressing HepG2 xenograft tumors. D574-0246 can be used for the study of hepatocellular carcinoma (HCC).
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.95%
- No. CAS: 1269110-12-4
- Fòrmula: C24H26N6O3
- Peso molecular:446.50
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Almacenamiento:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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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
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Actividad biológica
D574-0246 (4 days) reduces the viability of PLC cells with an IC50 of 16.49 μM and HepG2 cells with an IC50 of 6.656 μM[1].
D574-0246 (1-10 μM) significantly reduces both substrate-specific (LACTB K284) and global protein succinylation in HepG2 cells in a dose-dependent manner[1].
D574-0246 (1-10 μM) significantly decreases the ketolytic activity of OXCT1 in HepG2 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:HepG2 cells with OXCT1 overexpression or knockout (2 × 106) were subcutaneously implanted into the flanks of 5-week-old male BALB/c nude mice[1]
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Dosage:55 mg/kg
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Administration:i.p., once every 3 days for 8 times
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Result:Inhibited tumor growth in nude mice bearing OXCT1-overexpressing HepG2 xenograft tumors, while exerting no significant inhibitory effect on tumor growth in nude mice with OXCT1-knockout HepG2 xenograft tumors.
Reduced both global protein succinylation levels and LACTB K284-specific succinylation levels in OXCT1-overexpressing tumor tissues.
Showed no significant changes in body weight.
Caused no significant abnormalities in serum levels of aspartate aminotransferase (AST), alanine aminotransferase (ALT), and alkaline phosphatase (ALP) in nude mice.
Induced no obvious morphological changes in major organs (liver, kidney, and spleen) of nude mice.
Chemical Information
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No. CAS 1269110-12-4
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Appearance Solid
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Peso molecular 446.50
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Fòrmula C24H26N6O3
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Color White to light yellow
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SMILES
CC1=CC=C(C=C1)NC2=NC(N3CCN(CC3)C(NC4=CC=C5OCOC5=C4)=O)=CC(C)=N2
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Synonyms
iOXCT1
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
DMSO : 100 mg/mL (223.96 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. 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. 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: ≥ 5 mg/mL (11.20 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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.
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.
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 (271 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 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. 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 |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.2396 mL | 11.1982 mL | 22.3964 mL | 55.9910 mL |
| 5 mM | 0.4479 mL | 2.2396 mL | 4.4793 mL | 11.1982 mL | |
| 10 mM | 0.2240 mL | 1.1198 mL | 2.2396 mL | 5.5991 mL | |
| 15 mM | 0.1493 mL | 0.7465 mL | 1.4931 mL | 3.7327 mL | |
| 20 mM | 0.1120 mL | 0.5599 mL | 1.1198 mL | 2.7996 mL | |
| 25 mM | 0.0896 mL | 0.4479 mL | 0.8959 mL | 2.2396 mL | |
| 30 mM | 0.0747 mL | 0.3733 mL | 0.7465 mL | 1.8664 mL | |
| 40 mM | 0.0560 mL | 0.2800 mL | 0.5599 mL | 1.3998 mL | |
| 50 mM | 0.0448 mL | 0.2240 mL | 0.4479 mL | 1.1198 mL | |
| 60 mM | 0.0373 mL | 0.1866 mL | 0.3733 mL | 0.9332 mL | |
| 80 mM | 0.0280 mL | 0.1400 mL | 0.2800 mL | 0.6999 mL | |
| 100 mM | 0.0224 mL | 0.1120 mL | 0.2240 mL | 0.5599 mL |
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