GNE7599
Based on 1 Customer Validation
GNE7599 is a high-affinity VHL ligand with a Kd value of 540 pM, which binds to the VHL substrate receptor of the CRL2VHL E3 ligase. GNE7599 is cell-permeable and exhibits moderate stability in liver microsomes and hepatocytes. GNE7599 can be used in cancer-related research.
For research use only. We do not sell to patients.
- Purity : 99.19%
- CAS No.: 2771069-76-0
- Formula: C31H40N6O3S
- Molecular Weight:576.75
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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
Biological Activity
Description
IC50 & Target
[1]|
VHL 540 pM (Kd) |
In Vitro
GNE7599 (33-100 nM) binds VHL-Elongin B/C in SPR with KD = 540 pM[1].
GNE7599 (0.5-2 h) binds VHL in HEK293 VHL-NanoLuc cells, with KDapp <2.5 nM both in the absence and presence of Digitonin (HY-N4000)[1].
GNE7599 shows a gMDCK Papp A-to-B of 8.9 × 10-6 cm/s[1].
GNE7599 shows a hepatocellular CLhep of 64 mL/min/kg[1].
GNE7599 exhibits 99.7% binding in human plasma and mouse plasma[1].
GNE7599 shows a FaSSIF solubility of 190 μM[1].
GNE7599 shows a hepatic microsomal CLhep of 59.8 mL/min/kg[1].
GNE7599 binds VHL in the nanoBRET cellular assay and is a VHL ligand, with IC50 <5 nM[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Parmacokinetics
Chemical Information
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CAS No. 2771069-76-0
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Appearance Solid
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Molecular Weight 576.75
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Formula C31H40N6O3S
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Color White to off-white
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SMILES
O=C([C@@H](N1N=NC(C2CC2)=C1)C(C)(C)C)N3C[C@H](O)C[C@H]3C(N[C@H]4CCCCC5=C4C=CC(C6=C(C)N=CS6)=C5)=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
In Vitro:
DMSO : 200 mg/mL (346.77 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)
In Vivo:
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 (8.67 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 (8.67 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.
In Vivo Dissolution Calculator
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 (291 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 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 |
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| DMSO | 1 mM | 1.7339 mL | 8.6693 mL | 17.3385 mL | 43.3463 mL |
| 5 mM | 0.3468 mL | 1.7339 mL | 3.4677 mL | 8.6693 mL | |
| 10 mM | 0.1734 mL | 0.8669 mL | 1.7339 mL | 4.3346 mL | |
| 15 mM | 0.1156 mL | 0.5780 mL | 1.1559 mL | 2.8898 mL | |
| 20 mM | 0.0867 mL | 0.4335 mL | 0.8669 mL | 2.1673 mL | |
| 25 mM | 0.0694 mL | 0.3468 mL | 0.6935 mL | 1.7339 mL | |
| 30 mM | 0.0578 mL | 0.2890 mL | 0.5780 mL | 1.4449 mL | |
| 40 mM | 0.0433 mL | 0.2167 mL | 0.4335 mL | 1.0837 mL | |
| 50 mM | 0.0347 mL | 0.1734 mL | 0.3468 mL | 0.8669 mL | |
| 60 mM | 0.0289 mL | 0.1445 mL | 0.2890 mL | 0.7224 mL | |
| 80 mM | 0.0217 mL | 0.1084 mL | 0.2167 mL | 0.5418 mL | |
| 100 mM | 0.0173 mL | 0.0867 mL | 0.1734 mL | 0.4335 mL |
GNE7599 Related Classifications
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