| Size | Price | Stock | Qty |
|---|---|---|---|
| 500mg |
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| 1g |
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| Other Sizes |
| Targets |
Azido-PEG3-azide does not possess a specific pharmacological target of its own. Its function is chemical rather than biological—the two terminal azide groups provide reactive handles for click chemistry conjugation. The compound's role in PROTAC synthesis is structural: it serves as a linker that connects two ligands via azide-alkyne cycloaddition. The PEG3 spacer provides flexibility.
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|---|---|
| ln Vitro |
One ligand is for an E3 ubiquitin ligase, and the other is for the target protein; these two ligands are joined by a linker to form PROTACs. The intracellular ubiquitin-proteasome system is utilized by PROTACs to specifically destroy target proteins[1].
Azido-PEG3-azide itself does not exhibit intrinsic biological activity in vitro. Its activity is evaluated in the context of the complete PROTAC molecule. The azide groups enable efficient click chemistry conjugation. |
| ln Vivo |
As a non-therapeutic linker, Azido-PEG3-azide does not exhibit intrinsic in vivo activity. Its applications in vivo are realized through the conjugates prepared using this reagent.
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| Enzyme Assay |
Characterization involves HPLC, NMR, and MS. The azide groups can be detected by FTIR. Storage: appropriate conditions for azide-containing compounds.
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| Cell Assay |
Cell-based studies are conducted in the context of PROTAC-mediated protein degradation. Cells are treated with PROTACs incorporating this linker, and target protein degradation is assessed by Western blot.
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| Animal Protocol |
In vivo studies are performed using PROTAC molecules that incorporate this linker in mouse xenograft models.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties are characterized in the context of the complete PROTAC molecule.
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| Toxicity/Toxicokinetics |
Azido-PEG3-azide is not intended for human or veterinary use. Azide-containing compounds should be handled with care. Standard laboratory safety precautions should be followed.
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| References |
[1]. An S, et al. Small-molecule PROTACs: An emerging and promising approach for the development of targeted therapy drugs. EBioMedicine. 2018 Oct;36:553-562
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| Additional Infomation |
Azido-PEG3-azide is a PEG-based PROTAC linker and click chemistry reagent used in the synthesis of targeted protein degraders. The compound is not approved for clinical use.
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| Molecular Formula |
C₈H₁₆N₆O₃
|
|---|---|
| Molecular Weight |
244.25
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| Exact Mass |
244.128
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| CAS # |
101187-39-7
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| PubChem CID |
4157492
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| Appearance |
Colorless to light yellow liquid（Density：1.17 g/cm3）
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| Density |
1.1703g/mL
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| Boiling Point |
163-196°C
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| LogP |
0.562
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
12
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| Heavy Atom Count |
17
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| Complexity |
236
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C(COCCOCCOCCN=[N+]=[N-])N=[N+]=[N-]
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| InChi Key |
SFMMXKLNFMIUCH-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C8H16N6O3/c9-13-11-1-3-15-5-7-17-8-6-16-4-2-12-14-10/h1-8H2
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| Chemical Name |
1-azido-2-[2-[2-(2-azidoethoxy)ethoxy]ethoxy]ethane
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| Synonyms |
AzidoPEG3azide; Azido PEG3 azide
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~409.42 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (10.24 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (10.24 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (10.24 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.0942 mL | 20.4708 mL | 40.9417 mL | |
| 5 mM | 0.8188 mL | 4.0942 mL | 8.1883 mL | |
| 10 mM | 0.4094 mL | 2.0471 mL | 4.0942 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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