| Size | Price | Stock | Qty |
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| 100mg |
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| 250mg |
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| Targets |
Azido-PEG9-amine itself does not bind to a specific biological target. Its "target" is defined by the molecules it links together in PROTAC and ADC applications. In PROTACs, it joins a ligand for an E3 ubiquitin ligase to a ligand for a target protein. In ADCs, it connects an antibody to a cytotoxic payload. The azide group enables click chemistry reactions.
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| ln Vitro |
An ADC cytotoxin is connected to an antibody by use of an ADC linker to form an ADC. Two distinct ligands, one for the E3 ubiquitin ligase and the other for the target protein, are present in PROTAC and are joined by a linker. PROTAC targets and selectively degrades target proteins by means of the intracellular ubiquitin-proteasome system.
In vitro activity is primarily related to its function as a linker. It enables the formation of stable conjugates via copper-catalyzed or copper-free click chemistry. The amino group can be coupled to carboxylic acids or activated esters. The PEG spacer reduces nonspecific binding and aggregation. No direct pharmacological activity is attributed to the linker itself. |
| ln Vivo |
In vivo activity is inferred from the performance of ADCs or PROTACs synthesized using this linker. The non-cleavable nature of the linker provides stability in circulation. The PEG spacer improves the pharmacokinetic properties of the conjugate by increasing solubility and reducing immunogenicity. No direct in vivo activity is associated with the linker alone.
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| Enzyme Assay |
In vitro assays for Azido-PEG9-amine typically involve evaluating the efficiency of conjugation. The amine group is reacted with carboxylic acids using EDC/NHS coupling chemistry, or the azide group is reacted with alkyne-containing molecules via click chemistry. Reaction progress is monitored by HPLC, mass spectrometry, or NMR. Purity is assessed by HPLC (>98% typical). Solubility is evaluated in aqueous and organic solvents.
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| Cell Assay |
Cell-based assays are conducted in the context of the final ADC or PROTAC molecule. Cells are treated with the conjugate and evaluated for target-specific cytotoxicity (for ADCs) or protein degradation (for PROTACs). Biotinylated or fluorophore-labeled versions of the linker may be used to track cellular uptake and localization via flow cytometry or fluorescence microscopy. Cytotoxicity is measured by MTT or CellTiter-Glo assays.
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| Animal Protocol |
In vivo animal studies are performed with ADCs or PROTACs containing this linker. Tumor-bearing mice are treated with the conjugate, and tumor growth inhibition is monitored. Pharmacokinetic parameters are evaluated by measuring conjugate levels in blood and tissues. Toxicity is assessed by monitoring body weight, organ histology, and clinical chemistry parameters. The linker's stability in circulation is a key parameter evaluated in these studies.
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| ADME/Pharmacokinetics |
As a PEG-based linker (molecular weight 482.57, formula C20H42N4O9), Azido-PEG9-amine has favorable aqueous solubility due to the hydrophilic PEG spacer. No specific pharmacokinetic data are available for the linker alone; its PK profile is determined by the conjugated molecule. The non-cleavable nature contributes to conjugate stability in circulation.
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| Toxicity/Toxicokinetics |
No detailed toxicology data are specifically available for Azido-PEG9-amine. PEG-based compounds are generally considered to have low toxicity and good biocompatibility. The compound is for research use only and not intended for therapeutic use. Standard laboratory safety precautions should be followed when handling this compound.
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| References | |
| Additional Infomation |
Azido-PEG9-amine (CAS#: 1207714-69-9) is a non-cleavable, 9-unit PEG-based ADC and PROTAC linker. It contains an azide group for click chemistry and a primary amine for conjugation. Molecular weight: 482.57, formula: C20H42N4O9.
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| Molecular Formula |
C20H42N4O9
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|---|---|
| Molecular Weight |
482.569
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| Exact Mass |
482.295
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| CAS # |
1207714-69-9
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| PubChem CID |
59202801
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| Appearance |
Colorless to light yellow liquid
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| LogP |
-3.23
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
12
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| Rotatable Bond Count |
29
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| Heavy Atom Count |
33
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| Complexity |
419
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| Defined Atom Stereocenter Count |
0
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| SMILES |
N(CCOCCOCCOCCOCCOCCOCCOCCOCCOCCN)=[N+]=[N-]
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| InChi Key |
QECAUUOGHAUEDJ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C20H42N4O9/c21-1-3-25-5-7-27-9-11-29-13-15-31-17-19-33-20-18-32-16-14-30-12-10-28-8-6-26-4-2-23-24-22/h1-21H2
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| Chemical Name |
2-[2-[2-[2-[2-[2-[2-[2-[2-(2-azidoethoxy)ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethanamine
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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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.0722 mL | 10.3612 mL | 20.7224 mL | |
| 5 mM | 0.4144 mL | 2.0722 mL | 4.1445 mL | |
| 10 mM | 0.2072 mL | 1.0361 mL | 2.0722 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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