USP7-797
Based on 1 Customer Validation
USP7-797 (USP7-IN-7) is an orally available, selective USP7 inhibitor (IC50=0.5 nmol/L) with antitumor activity. USP7-797 reduces the level of MDM2, thereby increasing the stability and activity of p53, leading to cell cycle arrest and apoptosis. USP7-797 has low nanomolar cytotoxicity against p53 mutant cancer cell lines, p53 wild-type hematological tumors, and neuroblastoma cell lines.
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- Reinheit: 99.09%
- CAS. Nr.: 2413944-70-2
- Formel: C27H28ClN3O3S
- Molecular Weight:510.05
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Speicherung:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
Biologische Aktivität
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USP7 0.5 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| MM1.S | CC50 |
89 nM
Compound: 41
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Cytotoxicity against human MM1S cells expressing wild type p53 assessed as reduction in cell viability measured after 5 days by CellTiter-Glo assay
Cytotoxicity against human MM1S cells expressing wild type p53 assessed as reduction in cell viability measured after 5 days by CellTiter-Glo assay
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[PMID: 32302140] |
| NCI-H526 | CC50 |
450 nM
Compound: 41
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Cytotoxicity against human NCI-H526 cells expressing p53 mutant assessed as reduction in cell viability measured after 5 days by CellTiter-Glo assay
Cytotoxicity against human NCI-H526 cells expressing p53 mutant assessed as reduction in cell viability measured after 5 days by CellTiter-Glo assay
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[PMID: 32302140] |
| RKO | CC50 |
13 μM
Compound: 41
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Cytotoxicity against human RKO cells assessed as reduction in cellular ATP level measured after 5 days by CellTiter-Glo assay
Cytotoxicity against human RKO cells assessed as reduction in cellular ATP level measured after 5 days by CellTiter-Glo assay
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[PMID: 32302140] |
| RKO | EC50 |
25 nM
Compound: 41
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Inhibition of USP7 in human RKO cells transfected with p53 luciferase reporter vector assessed as increase in p53-dependent luciferase activity measured after 18 hrs by BrightGlo luciferase assay
Inhibition of USP7 in human RKO cells transfected with p53 luciferase reporter vector assessed as increase in p53-dependent luciferase activity measured after 18 hrs by BrightGlo luciferase assay
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[PMID: 32302140] |
USP7-797 (0-1 μM) shows cytotoxicity against p53 wild-type blood cancer cell lines with CC50 values of 0.2, 0.2, 0.4 and 0.1 μM for M07e, OCI-AML5, MOLM13 and MM.IS, respectively[1]. USP7-797 (0-2 μM) shows cytotoxicity against p53 wild-type neuroblastoma cell lines with CC50 values of 1.9, 0.6 and 0.5 μM for SH-SY5Y, CHP-134 and NB-1, respectively[1]. USP7-797 (0-25 μM) shows cytotoxicity against p53-mutant cancer cell lines with CC50 values of 0.5, 0.2 and 0.2 μM for H526, LA-N-2 and SK-N-DZ, respectively[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS. Nr. 2413944-70-2
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Appearance Solid
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Molecular Weight 510.05
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Formel C27H28ClN3O3S
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Color White to off-white
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SMILES
O=C(N1CC2=CC3=NC=CC(C4=CC(Cl)=CC(C)=C4C[C@@H]5CNCCO5)=C3S2)C6C(C)(C)C6C1=O
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Synonyms
USP7-IN-7
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Lösungsmittel & Löslichkeit
DMSO : 75 mg/mL (147.04 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 (protect from light). 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 (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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: ≥ 3.75 mg/mL (7.35 mM); Clear solution
This protocol yields a clear solution of ≥ 3.75 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (37.5 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. * In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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.
Reinheit & Dokumentation
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Data Sheet (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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Handling Instructions (2659 KB)
Verweise
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 (protect from light). 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 | 1.9606 mL | 9.8030 mL | 19.6059 mL | 49.0148 mL |
| 5 mM | 0.3921 mL | 1.9606 mL | 3.9212 mL | 9.8030 mL | |
| 10 mM | 0.1961 mL | 0.9803 mL | 1.9606 mL | 4.9015 mL | |
| 15 mM | 0.1307 mL | 0.6535 mL | 1.3071 mL | 3.2677 mL | |
| 20 mM | 0.0980 mL | 0.4901 mL | 0.9803 mL | 2.4507 mL | |
| 25 mM | 0.0784 mL | 0.3921 mL | 0.7842 mL | 1.9606 mL | |
| 30 mM | 0.0654 mL | 0.3268 mL | 0.6535 mL | 1.6338 mL | |
| 40 mM | 0.0490 mL | 0.2451 mL | 0.4901 mL | 1.2254 mL | |
| 50 mM | 0.0392 mL | 0.1961 mL | 0.3921 mL | 0.9803 mL | |
| 60 mM | 0.0327 mL | 0.1634 mL | 0.3268 mL | 0.8169 mL | |
| 80 mM | 0.0245 mL | 0.1225 mL | 0.2451 mL | 0.6127 mL | |
| 100 mM | 0.0196 mL | 0.0980 mL | 0.1961 mL | 0.4901 mL |
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