| Size | Price | Stock | Qty |
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| 50mg |
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| 100mg |
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| 250mg |
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| Other Sizes |
| Targets |
Azido-PEG8-NHS ester itself does not bind to a specific biological target. The NHS ester group reacts with primary amines (-NH2) on proteins, antibodies, or other amine-containing molecules to form stable amide bonds. The azide group enables copper-catalyzed azide-alkyne cycloaddition (CuAAc) with alkyne-containing molecules. As an ADC linker, it connects an antibody to a cytotoxic payload.
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| ln Vitro |
ADC cytotoxins are connected to antibodies through an ADC connector to form ADCs [1]. 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 selectively degrades target proteins by means of the intracellular ubiquitin-proteasome system [2].
In vitro activity is primarily related to its function as a bioconjugation reagent. It enables the efficient labeling of primary amine-containing molecules with an azide handle. The NHS ester reacts rapidly with amines at pH 7-9. The PEG spacer improves aqueous solubility and reduces nonspecific interactions. No direct pharmacological activity is attributed to the linker itself. |
| ln Vivo |
In vivo activity is inferred from the performance of ADCs synthesized using this linker. The cleavable nature of the linker allows for payload release at the target site. 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-PEG8-NHS ester typically involve evaluating the efficiency of bioconjugation. The NHS ester is reacted with primary amine-containing molecules at pH 7-9. Reaction efficiency is assessed by mass spectrometry, HPLC, or gel electrophoresis. Biotin incorporation is confirmed by streptavidin-binding assays. Purity is assessed by HPLC (>95% 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 molecule. Cells expressing the target antigen are treated with the ADC, and cytotoxicity is measured by MTT or CellTiter-Glo assays. Antigen-specific cell killing is compared to non-targeting controls. Internalization and trafficking of the ADC are assessed by immunofluorescence microscopy using fluorophore-labeled versions of the linker.
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| Animal Protocol |
In vivo animal studies are performed with ADCs containing this linker. Tumor-bearing mice are treated with the ADC, and tumor growth inhibition is monitored. Pharmacokinetic parameters are evaluated by measuring ADC levels in blood and tissues. Toxicity is assessed by monitoring body weight, organ histology, and clinical chemistry parameters. The cleavable nature of the linker is evaluated for payload release at the tumor site.
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| ADME/Pharmacokinetics |
As a PEG-based linker (molecular weight 564.58, formula C23H40N4O12), Azido-PEG8-NHS ester has favorable aqueous solubility due to the hydrophilic PEG spacer. The NHS ester is hydrolytically unstable and should be used fresh. No specific PK data are available for the linker alone; its PK profile is determined by the conjugated molecule.
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| Toxicity/Toxicokinetics |
No detailed toxicology data are specifically available for Azido-PEG8-NHS ester. The compound is for research use only and not intended for therapeutic use. Standard laboratory safety precautions should be followed. The NHS ester may cause mild irritation upon contact. Comprehensive toxicological evaluation has not been reported.
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| References | |
| Additional Infomation |
Azido-PEG8-NHS ester (CAS#: 1204834-00-3) is a cleavable, 8-unit PEG-based ADC linker. It contains an azide group for click chemistry and an NHS ester for amine coupling. It is used in bioconjugation and ADC synthesis. Molecular weight: 564.58, formula: C23H40N4O12.
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| Molecular Formula |
C23H40N4O12
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|---|---|
| Molecular Weight |
564.583307266235
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| Exact Mass |
564.264
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| CAS # |
1204834-00-3
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| PubChem CID |
51340932
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| Appearance |
Colorless to light yellow liquid
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| LogP |
-1.1
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
14
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| Rotatable Bond Count |
29
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| Heavy Atom Count |
39
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| Complexity |
693
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O(C(CCOCCOCCOCCOCCOCCOCCOCCOCCN=[N+]=[N-])=O)N1C(CCC1=O)=O
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| InChi Key |
AZXJVYAMFTUKFC-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C23H40N4O12/c24-26-25-4-6-32-8-10-34-12-14-36-16-18-38-20-19-37-17-15-35-13-11-33-9-7-31-5-3-23(30)39-27-21(28)1-2-22(27)29/h1-20H2
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| Chemical Name |
(2,5-dioxopyrrolidin-1-yl) 3-[2-[2-[2-[2-[2-[2-[2-(2-azidoethoxy)ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]propanoate
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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 (~177.12 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.43 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 (4.43 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 (4.43 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 | 1.7712 mL | 8.8561 mL | 17.7123 mL | |
| 5 mM | 0.3542 mL | 1.7712 mL | 3.5425 mL | |
| 10 mM | 0.1771 mL | 0.8856 mL | 1.7712 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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