| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
This compound does not have a biological target itself; it is a chemical linker used for bioconjugation. The azide group reacts with alkyne-functionalized molecules via click chemistry, enabling the covalent attachment of two entities. In ADC synthesis, it is used to connect an antibody (modified with an alkyne) to a cytotoxic payload (or vice versa). The Gly-Gly-Gly and PEG2 segments provide a hydrophilic and flexible spacer that improves the solubility and stability of the resulting conjugate. It is a chemical tool for ADC synthesis.
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| ln Vitro |
Gly-Gly-Gly-PEG2-azide itself is not evaluated for direct biological activity as it is a linker. Its activity is demonstrated through its use in synthesizing ADCs. The efficiency of the click chemistry conjugation reaction is assessed in vitro. The resulting ADC is then tested for its ability to bind to target antigens on cancer cells and exert cytotoxicity. The linker's stability and hydrophilicity contribute to the overall properties of the ADC. It is a chemical building block.
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| ln Vivo |
In vivo activity is not applicable to Gly-Gly-Gly-PEG2-azide itself as it is a linker for ADC synthesis. The in vivo efficacy would be attributed to the complete ADC molecule synthesized using this linker. Such ADCs would be evaluated in animal models for antitumor activity and pharmacokinetics. The compound itself is not administered to animals. Its role is confined to chemical synthesis. It is stored and handled based on its chemical properties.
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| Enzyme Assay |
In vitro enzyme/receptor binding assays are not applicable to Gly-Gly-Gly-PEG2-azide as it is a linker, not a drug candidate. The primary in vitro characterization involves the click chemistry conjugation reaction. The azide group is reacted with an alkyne-functionalized molecule in the presence of a copper catalyst. The progress of the reaction is monitored by HPLC or mass spectrometry. The efficiency of the conjugation is assessed. No receptor binding assays are performed on the linker itself.
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| Cell Assay |
Cell-based assays are not directly performed on Gly-Gly-Gly-PEG2-azide as it is a linker. However, the final ADC molecules synthesized using this linker are tested in cell-based assays. Typically, cancer cell lines expressing the target antigen are treated with the ADC, and cell viability is assessed using MTT or CellTiter-Glo assays. Antigen binding and internalization are measured by flow cytometry. These assays confirm the functional activity of the ADC. The linker itself is not tested in cell culture.
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| Animal Protocol |
In vivo animal experiments are not performed with Gly-Gly-Gly-PEG2-azide itself. This compound is a synthetic building block used to construct ADCs. Once an ADC is synthesized, it may be tested in animal models, typically xenograft models in mice. Tumor-bearing mice are administered the ADC, and tumor growth inhibition, pharmacokinetics, and toxicity are evaluated. However, the intermediate itself is not administered to animals.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties are not applicable to Gly-Gly-Gly-PEG2-azide as it is a linker for ADC synthesis. The compound's molecular weight is 345.35. It is stored at 2-8°C in a refrigerator. Its solubility and stability are characterized to facilitate its use in chemical synthesis. The PEG2 and peptide components are designed to improve the hydrophilicity of the resulting ADC. No ADME studies are performed on this intermediate.
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| Toxicity/Toxicokinetics |
Toxicological data for Gly-Gly-Gly-PEG2-azide are not available as it is a research chemical intermediate. Standard laboratory safety precautions for handling chemical reagents should be followed. The compound is not intended for human or animal consumption. Its specific toxicity profile has not been established. Any toxicological assessment would be performed on the final ADC drug candidate, not on this synthetic precursor. It is handled as a potentially hazardous material.
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| References | |
| Additional Infomation |
Gly-Gly-Gly-PEG2-azide is an ADC linker used in the synthesis of antibody-drug conjugates. Its molecular formula is C12H23N7O5, and its molecular weight is 345.35. It features a tri-glycine peptide chain, a PEG2 spacer, and a terminal azide group for click chemistry. The azide group enables efficient bioconjugation via copper-catalyzed azide-alkyne cycloaddition (CuAAC). It is available for research use only.
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| Exact Mass |
345.176
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|---|---|
| CAS # |
2222277-20-3
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| PubChem CID |
169494466
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| Appearance |
White to off-white solid powder
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
14
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| Heavy Atom Count |
24
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| Complexity |
440
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C(COCCOCCN=[N+]=[N-])NC(=O)CNC(=O)CNC(=O)CN
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| InChi Key |
CLBIQTQAFPDAKO-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C12H23N7O5/c13-7-10(20)16-9-12(22)17-8-11(21)15-1-3-23-5-6-24-4-2-18-19-14/h1-9,13H2,(H,15,21)(H,16,20)(H,17,22)
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| Chemical Name |
2-amino-N-[2-[[2-[2-[2-(2-azidoethoxy)ethoxy]ethylamino]-2-oxoethyl]amino]-2-oxoethyl]acetamide
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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 :~50 mg/mL (~144.78 mM; with sonication)
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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.) |
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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