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| Targets |
As a chemical linker, m-PEG6-azide does not bind to biological targets. Its functional "targets" are the chemical groups on molecules to which it conjugates. In ADC applications, the linker attaches cytotoxic payloads to monoclonal antibodies. The azide group enables Click Chemistry reactions (CuAAc or SPAAC) with alkyne-bearing compounds. The PEG6 spacer enhances aqueous solubility and reduces aggregation of the final conjugates. This linker does not bind to biological receptors or enzymes but serves as a structural bridge for bioconjugation. The compound is non-cleavable.
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| ln Vitro |
An ADC cytotoxin is connected to an antibody by use of an ADC linker to form an ADC.
As a synthetic linker molecule, m-PEG6-azide does not exhibit pharmacological activity in cell-based assays. Its in vitro utility is demonstrated through the successful synthesis and characterization of ADC constructs incorporating this linker. Researchers evaluate the linker's performance by assessing conjugation efficiency (via HPLC, LC-MS, or NMR), the stability of resulting conjugates in cell culture media, and the biological activity of final ADC constructs in target cell lines. For ADCs, cytotoxicity is assessed using cell viability assays such as MTT or CellTiter-Glo. The compound is soluble in DMSO and other organic solvents. The azide group is stable under standard storage conditions. |
| ln Vivo |
No direct in vivo pharmacological activity is attributed to m-PEG6-azide. Its in vivo relevance is demonstrated through the performance of ADC constructs synthesized using this linker in animal models. For in vivo administration, ADCs are typically formulated in vehicles such as saline or buffer. The linker's stability in biological matrices, its contribution to the construct's pharmacokinetic profile, and its ability to maintain construct integrity are key parameters evaluated in preclinical studies. The azide group is stable under physiological conditions, ensuring that the construct remains intact during circulation.
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| Enzyme Assay |
In vitro enzyme/receptor binding assays are not applicable to m-PEG6-azide as it is a chemical linker with no intrinsic affinity for biological macromolecules. Quality control and characterization are performed using standard analytical methods. Purity is assessed by HPLC and structural integrity is confirmed by ¹H NMR, ¹³C NMR, and mass spectrometry. The azide group content is verified through spectroscopic analysis (e.g., IR spectroscopy). For researchers using this linker, Click Chemistry reactions are monitored by TLC, HPLC, or LC-MS. Solubility testing in various solvents is performed to guide formulation development.
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| Cell Assay |
Cell-based assays are not performed directly on m-PEG6-azide because it is a synthetic linker lacking biological activity. However, the biological activity of ADC constructs containing this linker is evaluated in relevant cell lines. Typical protocols involve treating cells with the ADC construct for 48-72 hours, then assessing cytotoxicity using cell viability assays such as MTT, CellTiter-Glo, or flow cytometry-based viability staining. The linker's contribution to the construct's cellular uptake, stability, and efficacy is inferred from comparative studies. DMSO stock solutions are prepared and diluted in cell culture media.
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| Animal Protocol |
In vivo animal studies are conducted with ADC constructs incorporating m-PEG6-azide, not with the linker alone. Typical protocols utilize rodent models (e.g., mice bearing tumor xenografts). The ADC is administered via intravenous injection at doses determined by the payload's maximum tolerated dose. Efficacy is assessed by measuring tumor volumes with calipers every 2-3 days, body weight monitoring, and survival analysis. Pharmacodynamic endpoints include tumor growth inhibition. The linker's stability in circulation is evaluated through plasma sampling and LC-MS/MS analysis of intact ADC concentrations.
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| ADME/Pharmacokinetics |
As a chemical linker, m-PEG6-azide does not have a conventional pharmacokinetic profile. However, the pharmacokinetic properties of ADC constructs incorporating this linker are evaluated in preclinical studies. Following intravenous administration in rodents, key parameters such as half-life, clearance, volume of distribution, and AUC are determined from plasma concentration-time data. The PEG6 spacer contributes to enhanced aqueous solubility, reduced protein binding, and potentially prolonged circulation time of the conjugate. Linker stability in plasma is assessed by measuring free payload release over time using LC-MS/MS.
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| Toxicity/Toxicokinetics |
Standard laboratory safety precautions should be followed when handling m-PEG6-azide: use of personal protective equipment (gloves, safety goggles, lab coat) and handling in a well-ventilated fume hood. The compound should be stored at -20°C for long-term stability. Azides are potentially explosive and should be handled with care; avoid heating, friction, or shock. No genotoxicity, carcinogenicity, or reproductive toxicity data are available. Researchers should consult the safety data sheet (SDS) before handling and follow institutional chemical safety guidelines.
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| References |
[1]. Gauzy, Laurence, et al. Cytotoxic agents comprising new tomaymycin derivatives and their therapeutic use. Patent WO2007085930A1.
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| Additional Infomation |
Additional information for m-PEG6-azide: The compound has a CAS number of 1043884-49-6. Its molecular formula is C₁₃H₂₇N₃O₆ and molecular weight is 321.37 g/mol. It is a non-cleavable 6-unit PEG ADC linker. It is a click chemistry reagent with an azide group for CuAAc reactions. It is for research use only and is not approved for clinical applications. No FDA approvals exist.
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| Molecular Formula |
C13H27N3O6
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|---|---|
| Molecular Weight |
321.369983911514
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| Exact Mass |
321.19
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| CAS # |
1043884-49-6
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| PubChem CID |
60146162
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| Appearance |
Colorless to light yellow liquid
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| LogP |
0.478
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
18
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| Heavy Atom Count |
22
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| Complexity |
264
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O(CCOCCOCCN=[N+]=[N-])CCOCCOCCOC
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| InChi Key |
MACROZUHOZGXJL-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C13H27N3O6/c1-17-4-5-19-8-9-21-12-13-22-11-10-20-7-6-18-3-2-15-16-14/h2-13H2,1H3
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| Chemical Name |
1-azido-2-[2-[2-[2-[2-(2-methoxyethoxy)ethoxy]ethoxy]ethoxy]ethoxy]ethane
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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 | 3.1117 mL | 15.5584 mL | 31.1168 mL | |
| 5 mM | 0.6223 mL | 3.1117 mL | 6.2234 mL | |
| 10 mM | 0.3112 mL | 1.5558 mL | 3.1117 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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