| Size | Price | Stock | Qty |
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| 50mg |
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| 100mg |
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| Other Sizes |
| Targets |
PEGs
This linker itself does not have a biological target. Its purpose is to connect two ligands: one that binds to a target protein and another that recruits an E3 ubiquitin ligase to form a PROTAC, or to connect multiple functional moieties for bioconjugation. The "target" is a chemical reaction (click chemistry), not a biological protein. |
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| ln Vitro |
A linker separates the two ligands that make up PROTACs; one ligand is for an E3 ubiquitin ligase, and the other is for the target protein. Target proteins are selectively degraded by PROTACs by taking advantage of the intracellular ubiquitin-proteasome system[1].
This compound is a chemical reagent, not a bioactive drug candidate, and thus is not tested for in vitro biological activity on cells. Its utility lies in its chemical reactivity. The azide groups are highly reactive with alkyne-functionalized molecules via copper-catalyzed azide-alkyne cycloaddition (CuAAC) or strain-promoted alkyne-nitrone cycloaddition (SPAAC) click chemistry, allowing for efficient and specific conjugation. |
| ln Vivo |
This compound is not used for in vivo efficacy studies. It is a building block for creating molecules (such as PROTACs) that are then tested in vivo. For example, a PROTAC synthesized using this linker could be administered to mice to induce the degradation of a specific oncogenic protein, leading to tumor growth inhibition. The linker's modularity makes it a critical tool for in vivo target validation.
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| Enzyme Assay |
This compound is a chemical intermediate, so it is not used in biological assays such as enzyme/receptor binding. Instead, its reactivity can be demonstrated in a non-cellular chemical assay. The azide groups are shown to undergo click chemistry reactions with terminal alkynes. For example, N-(Amino-PEG2)-N-bis(PEG3-azide) is incubated with a fluorescently labeled alkyne in the presence of a copper catalyst. The reaction mixture is analyzed by LC-MS or gel electrophoresis, and the appearance of a new product with a molecular weight corresponding to the conjugation of both molecules is monitored.
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| Cell Assay |
This compound is a chemical reagent, so it has no inherent activity in a standard cell-based assay. Its utility is demonstrated by using it to synthesize a molecule (like a PROTAC or a fluorescent probe) and then testing that molecule in cells. A typical cellular assay for a PROTAC built with this linker would involve treating cells with the PROTAC, then lysing the cells and measuring the level of the target protein by Western blotting to determine the DC50 (concentration for 50% protein degradation).
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| Animal Protocol |
N/A - Not applicable for the linker itself. However, as an example of an in vivo study that a PROTAC made with this linker would be used for: Female athymic nude mice bearing subcutaneous xenografts (e.g., with target protein-expressing cancer cells) are administered the PROTAC intraperitoneally (i.p.) or intravenously (i.v.) at various doses (e.g., 10-100 mg/kg). Tumor volumes are measured every 2-3 days. At the end of the study, tumor and tissue lysates are analyzed by Western blot to quantify the degradation of the target protein.
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| ADME/Pharmacokinetics |
N/A for the linker alone. The linker is a synthetic polymer (PEG) and is considered to be biologically inert and non-immunogenic. It is used specifically to improve the aqueous solubility, stability, and pharmacokinetic (PK) properties of the final PROTAC or conjugate. The presence of the PEG units can increase the hydrodynamic radius of a molecule, potentially reducing its clearance and extending its plasma half-life (t1/2).
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| Toxicity/Toxicokinetics |
This compound is designed to be as non-toxic as possible. PEG is a biocompatible polymer, and the terminal functional groups (amine, azide) are generally considered safe for laboratory handling. The primary toxicity concerns would arise not from the linker itself, but from the final bioactive molecule (e.g., a PROTAC) it is used to build. Standard lab safety precautions should be followed.
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| References | |
| Additional Infomation |
N-(Amino-PEG2)-N-bis(PEG3-azide) is an advanced chemical tool for the field of chemical biology. Its design, containing three functional groups (one amine, two azides), allows for the creation of branched or multi-specific conjugates. It is particularly valuable for the synthesis of PROTACs that require a branched linker to connect one target-binding ligand and two E3 ligase-binding ligands (known as a "homo-PROTAC") or for creating "tandem" molecules.
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| Molecular Formula |
C22H46N8O8
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|---|---|
| Appearance |
Light yellow to yellow liquid
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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 Note: (1). This product requires protection from light (avoid light exposure) during transportation and storage. (2). Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture. |
| 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 (~181.60 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.54 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 (4.54 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 (4.54 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
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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