NVS-VHL720
Based on 1 Customer Validation
NVS-VHL720 is a selective VHL-based cysteine dioxygenase (CDO1) molecular glue degrader. NVS-VHL720 recruits CDO1 to the VHL E3 ligase complex, driving ubiquitin-dependent proteasomal degradation of CDO1. NVS-VHL720 can be used for the research of cancer.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Pureté: 98.63%
- Formule: C27H33N5O4
- Masse moléculaire:491.58
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Stockage: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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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
Cysteine dioxygenase (CDO1)[1]
NVS-VHL720 (Compound 8) binds directly to VHL with a Kd of 0.072 μM, and mediates formation of a high-affinity ternary VBC-CDO1 complex with a Kd of 0.10 μM, which is drastically reduced by mutation of CDO1 residue Q99[1].
NVS-VHL720 (60 min) potently induces ternary VBC-CDO1 complex formation in a TR-FRET assay with an AC50 of 0.071 μM, and this activity is significantly reduced by mutation of CDO1 residue Q99[1].
NVS-VHL720 (2 h) induces VHL-CDO1 ternary complex formation in HEK293T cells with an AC50 of 0.306 μM, as measured by the NanoBiT assay[1].
NVS-VHL720 (17 h) potently degrades CDO1 in HEK293T cells with an absDC50 of 0.008 μM and 98.46% maximum degradation, and this activity is dependent on CDO1 residue Q99[1].
NVS-VHL720 (0.05-0.1 μM; 24 h) selectively degrades endogenous CDO1 in Huh-7 cells, with 62% degradation at 0.05 μM and 72% degradation at 0.1 μM, without affecting other quantified proteins[1].
NVS-VHL720 (0.01 nM-100 μM) does not affect the viability of HEK293T cells at tested concentrations[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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Appearance Solid
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Masse moléculaire 491.58
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Formule C27H33N5O4
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Color White to off-white
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SMILES
O=C(NCC1=CC=C(C2=CC=NN2)C3=C1C=CC=C3)[C@H]4N(C([C@@H](NC(C)=O)C(C)(C)C)=O)C[C@H](O)C4
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvant et solubilité
DMSO : 100 mg/mL (203.43 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 (10.17 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 5 mg/mL (10.17 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 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.
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.
Pureté et documentation
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Fiche technique (274 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Instruction de manipulation (2659 KB)
Références
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 | 2.0343 mL | 10.1713 mL | 20.3426 mL | 50.8564 mL |
| 5 mM | 0.4069 mL | 2.0343 mL | 4.0685 mL | 10.1713 mL | |
| 10 mM | 0.2034 mL | 1.0171 mL | 2.0343 mL | 5.0856 mL | |
| 15 mM | 0.1356 mL | 0.6781 mL | 1.3562 mL | 3.3904 mL | |
| 20 mM | 0.1017 mL | 0.5086 mL | 1.0171 mL | 2.5428 mL | |
| 25 mM | 0.0814 mL | 0.4069 mL | 0.8137 mL | 2.0343 mL | |
| 30 mM | 0.0678 mL | 0.3390 mL | 0.6781 mL | 1.6952 mL | |
| 40 mM | 0.0509 mL | 0.2543 mL | 0.5086 mL | 1.2714 mL | |
| 50 mM | 0.0407 mL | 0.2034 mL | 0.4069 mL | 1.0171 mL | |
| 60 mM | 0.0339 mL | 0.1695 mL | 0.3390 mL | 0.8476 mL | |
| 80 mM | 0.0254 mL | 0.1271 mL | 0.2543 mL | 0.6357 mL | |
| 100 mM | 0.0203 mL | 0.1017 mL | 0.2034 mL | 0.5086 mL |
NVS-VHL720 Related Classifications
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