Antitumor agent-153
Based on 1 Customer Validation
Antitumor agent-153 (compound 11b) is an optimized H2A histone ubiquitination inhibitor based on PRT4165 (HY-19817). Antitumor agent-153 inhibits the viability of human osteosarcoma U2OS cells and reduces histone H2A monoubiquitination, exhibiting anticancer activity.
For research use only. We do not sell to patients.
- Purity: 99.62%
- Formula: C16H8N2O6
- Molecular Weight:324.24
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Metabolism/Protease Compound Library
HY-L012
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Anti-Cancer Compound Library
HY-L025
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Oxygen Sensing Compound Library
HY-L045
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Ubiquitination Compound Library
HY-L050
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Metabolic Enzyme Compound Library
HY-L146
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Mitophagy Compound Library
HY-L180
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Bioactive Compound Library Max
HY-L181
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MCE Bioactive Compound Library
HY-L001V
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Bioactive Compound Library
HY-L001
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Amino Acid Metabolism Compound Library
HY-L189
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Cell Proliferation Compound Library
HY-L201
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High-Throughput Bioactive Compound Library
HY-L205
Biological Activity
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| U2OS | IC50 |
5.86 μM
Compound: 11b
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Antiproliferative activity against human U2OS cells assessed as reduction in cell viability incubated for 72 hrs
Antiproliferative activity against human U2OS cells assessed as reduction in cell viability incubated for 72 hrs
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[PMID: 38636717] |
Antitumor agent-153 has an IC50 of 5.86 μM on U2O cells and completely inhibits their proliferation at 30 μM [1].
Reduced H2AK119ub1 levels disrupt tumor development and cancer cell growth. Antitumor agent-153 (24-96 μM; 1 h) can significantly reduce H2AK119ub1 levels in U2O cells in a dose-dependent manner[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:U2O cells
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Concentration:6 μM, 12 μM, 24 μM, 48 μM, 96 μM
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Incubation Time:1 h
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Result:Significantly decreased H2AK119ub1 levels in cells in a dose-dependent manner (24-96 μM).
Chemical Information
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Appearance Solid
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Molecular Weight 324.24
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Formula C16H8N2O6
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Color Light yellow to yellow
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SMILES
O=C(C1=C(C/2=O)C=CC=C1)C2=C/C3=C([N+]([O-])=O)C=CC=C3[N+]([O-])=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 100 mg/mL (308.41 mM; ultrasonic and warming and heat to 60°C; 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 (15.42 mM); Suspended solution
This protocol yields a suspended solution of ≥ 5 mg/mL (saturation unknown). Suspended solution can be used for oral and intraperitoneal injection.
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.
Purity & Documentation
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Data Sheet (276 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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Handling Instructions (2659 KB)
References
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 | 3.0841 mL | 15.4207 mL | 30.8414 mL | 77.1034 mL |
| 5 mM | 0.6168 mL | 3.0841 mL | 6.1683 mL | 15.4207 mL | |
| 10 mM | 0.3084 mL | 1.5421 mL | 3.0841 mL | 7.7103 mL | |
| 15 mM | 0.2056 mL | 1.0280 mL | 2.0561 mL | 5.1402 mL | |
| 20 mM | 0.1542 mL | 0.7710 mL | 1.5421 mL | 3.8552 mL | |
| 25 mM | 0.1234 mL | 0.6168 mL | 1.2337 mL | 3.0841 mL | |
| 30 mM | 0.1028 mL | 0.5140 mL | 1.0280 mL | 2.5701 mL | |
| 40 mM | 0.0771 mL | 0.3855 mL | 0.7710 mL | 1.9276 mL | |
| 50 mM | 0.0617 mL | 0.3084 mL | 0.6168 mL | 1.5421 mL | |
| 60 mM | 0.0514 mL | 0.2570 mL | 0.5140 mL | 1.2851 mL | |
| 80 mM | 0.0386 mL | 0.1928 mL | 0.3855 mL | 0.9638 mL | |
| 100 mM | 0.0308 mL | 0.1542 mL | 0.3084 mL | 0.7710 mL |
Antitumor agent-153 Related Classifications
HY-163518 Related Classifications
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