Tri-GalNAc-DBCO
Based on 1 Customer Validation
Tri-GalNAc-DBCO is a synthetic ligand composed of three GalNAc units connected to DBCO. Tri-GalNAc-DBCO can act as a ligand for the sialic acid-degrading protein receptor (ASGPR), and can be coupled with targeting proteins or small molecules to form GalNAc-LYTACs. Tri-GalNAc-DBCO specifically binds to ASGPR and, through receptor-mediated endocytosis, guides the coupled molecules to lysosomes for degradation.
For research use only. We do not sell to patients.
- Purity: 99.97%
- CAS No.: 2999748-27-3
- Formula: C82H127N11O29
- Molecular Weight:1730.94
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Biological Activity
Tri-GalNAc-DBCO is conjugated with the anti-EGFR antibody (Cetuximab (HY-P9905)), the anti-HER2 antibody (Pertuzumab (HY-P9912)), and the anti-PCSK9 antibody (Alirocumab (HY-P9928)), forming homogeneous conjugates. The conjugated LYTACs can efficiently degrade membrane proteins[1][2][3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 2999748-27-3
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Appearance Solid
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Molecular Weight 1730.94
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Formula C82H127N11O29
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Color White to off-white
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SMILES
O=C(NCCCNC(CCCCO[C@H](O[C@@H]1CO)[C@@H]([C@H]([C@H]1O)O)NC(C)=O)=O)CCOCC(COCCC(NCCCNC(CCCCO[C@H](O[C@@H]2CO)[C@@H]([C@H]([C@H]2O)O)NC(C)=O)=O)=O)(NC(CCCCC(N3CC4=CC=CC=C4C#CC5=CC=CC=C53)=O)=O)COCCC(NCCCNC(CCCCO[C@H](O[C@@H]6CO)[C@@H]([C@H]([C@H]6O)O)NC(C)=O)=O)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
H2O : 100 mg/mL (57.77 mM; Need ultrasonic)
DMSO : 100 mg/mL (57.77 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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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: ≥ 2.5 mg/mL (1.44 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: ≥ 2.5 mg/mL (1.44 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
Working solution concentration: 0.22 mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
Purity & Documentation
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Data Sheet (275 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
[1]. Green Ahn, et al. LYTACs that engage the asialoglycoprotein receptor for targeted protein degradation. Nat Chem Biol. 2021 Sep;17(9):937-946. [Content Brief]
[2]. Maity P , et al. Targeting the Epidermal Growth Factor Receptor with Molecular Degraders: State-of-the-Art and Future Opportunities. J Med Chem. 2023 Mar 9;66(5):3135-3172. [Content Brief]
[3]. Donahue TC, et al. Synthetic Site-Specific Antibody-Ligand Conjugates Promote Asialoglycoprotein Receptor-Mediated Degradation of Extracellular Human PCSK9. ACS Chem Biol. 2023 Jul 21;18(7):1611-1623. [Content Brief]
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 (sealed storage, away from moisture). 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 |
|---|---|---|---|---|---|
| H2O / DMSO | 1 mM | 0.5777 mL | 2.8886 mL | 5.7772 mL | 14.4430 mL |
| 5 mM | 0.1155 mL | 0.5777 mL | 1.1554 mL | 2.8886 mL | |
| 10 mM | 0.0578 mL | 0.2889 mL | 0.5777 mL | 1.4443 mL | |
| 15 mM | 0.0385 mL | 0.1926 mL | 0.3851 mL | 0.9629 mL | |
| 20 mM | 0.0289 mL | 0.1444 mL | 0.2889 mL | 0.7222 mL | |
| 25 mM | 0.0231 mL | 0.1155 mL | 0.2311 mL | 0.5777 mL | |
| 30 mM | 0.0193 mL | 0.0963 mL | 0.1926 mL | 0.4814 mL | |
| 40 mM | 0.0144 mL | 0.0722 mL | 0.1444 mL | 0.3611 mL | |
| 50 mM | 0.0116 mL | 0.0578 mL | 0.1155 mL | 0.2889 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.