| Size | Price | Stock | Qty |
|---|---|---|---|
| 50mg |
|
||
| 100mg |
|
||
| 250mg | |||
| Other Sizes |
| Targets |
Azido-PEG8-acid is a non-cleavable linker used in the synthesis of antibody-drug conjugates (ADCs). It is also a PEG-based PROTAC linker. The compound contains an azide (N3) group that enables copper-catalyzed azide-alkyne cycloaddition (CuAAC) click chemistry reactions. The PEG spacer enhances the solubility and stability of the ADC or PROTAC. As a linker, it connects the antibody to the cytotoxic payload in ADCs or the target protein ligand to the E3 ligase ligand in PROTACs.
|
|---|---|
| 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 [1].
In vitro, Azido-PEG8-acid is used as a building block for the synthesis of ADCs and PROTACs. ADCs consist of an antibody linked to an ADC cytotoxin via an ADC linker. The compound's PEG spacer enhances the solubility and stability of the resulting conjugates. As a non-cleavable linker, it provides stable conjugation between the antibody and payload, which may affect the pharmacokinetics and efficacy of the ADC. The compound's azide group enables efficient conjugation via click chemistry. |
| ln Vivo |
In vivo, Azido-PEG8-acid is not administered directly but is used to synthesize ADCs and PROTACs that are evaluated in animal models. The PEG spacer enhances the solubility and stability of the drug, rendering it an indispensable component in drug delivery systems. The resulting ADCs enable targeted delivery of chemotherapeutics with reduced systemic toxicity. The compound's role as a linker in ADC and PROTAC synthesis has been validated in various preclinical studies.
|
| Enzyme Assay |
In cell-free biochemical assays, Azido-PEG8-acid is evaluated for its ability to serve as a linker in conjugation reactions. The azide group enables efficient CuAAC click chemistry with alkyne-bearing molecules. The compound's purity (≥95%) and molecular weight (469.53 g/mol) are characterized using analytical techniques such as HPLC and mass spectrometry. The compound's solubility and stability in various solvents are assessed to ensure compatibility with conjugation reactions.
|
| Cell Assay |
Cellular assays for Azido-PEG8-acid involve evaluating the activity of the ADCs or PROTACs synthesized using this linker. The resulting conjugates are tested for their ability to bind to target antigens (for ADCs) or degrade target proteins (for PROTACs). The PEG linker's effect on cellular uptake, intracellular trafficking, and biological activity is assessed in relevant cell lines. The compound itself is not biologically active and serves only as a linker.
|
| Animal Protocol |
Animal models for Azido-PEG8-acid involve evaluating the ADCs or PROTACs synthesized using this linker in preclinical studies. The resulting conjugates are tested in tumor xenograft models (for ADCs) or disease models relevant to the target protein (for PROTACs). The PEG linker's effect on pharmacokinetics, biodistribution, and efficacy is assessed. The compound's role in enabling targeted drug delivery has been demonstrated in various animal models.
|
| ADME/Pharmacokinetics |
Pharmacokinetic data for Azido-PEG8-acid are not typically reported as the compound is a linker rather than a therapeutic agent. The compound's molecular weight is 469.53 g/mol with a formula of C19H37N3O10. It should be stored at -20°C. The CAS number is 1214319-92-2. The compound is soluble in organic solvents typical for PEG-containing molecules. Standard handling procedures for PEG linkers apply.
|
| Toxicity/Toxicokinetics |
Toxicity data for Azido-PEG8-acid are limited as the compound is a linker rather than a therapeutic agent. The compound is supplied at ≥95% purity. Standard safety precautions for handling laboratory chemicals apply. The azide group may pose a hazard if heated or subjected to shock, as azides can be explosive. Appropriate handling procedures should be followed. The compound is for research use only and not for human use.
|
| References |
[1]. Tan M, et al. Peptide-targeted Nanoglobular Gd-DOTA monoamide conjugates for magnetic resonance cancer molecular imaging. Biomacromolecules. 2010 Mar 8;11(3):754-61.
|
| Additional Infomation |
Azido-PEG8-acid is a non-cleavable 8-unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs). It is also a PEG-based PROTAC linker. The PEG spacer enhances the solubility and stability of the ADC or PROTAC. The azide group facilitates the attachment of bioactive molecules via click chemistry. The compound finds applications in cancer therapy (targeted delivery of chemotherapeutics) and gene therapy (delivery of nucleic acids). The CAS number is 1214319-92-2.
|
| Molecular Formula |
C19H37N3O10
|
|---|---|
| Molecular Weight |
467.511186361313
|
| Exact Mass |
467.247
|
| CAS # |
1214319-92-2
|
| PubChem CID |
75535109
|
| Appearance |
Colorless to light yellow viscous liquid
|
| LogP |
-0.6
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
12
|
| Rotatable Bond Count |
27
|
| Heavy Atom Count |
32
|
| Complexity |
453
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
C(COCCOCCOCCOCCOCCOCCOCCOCCN=[N+]=[N-])C(=O)O
|
| InChi Key |
URUGOEBULOZLBF-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C19H37N3O10/c20-22-21-2-4-26-6-8-28-10-12-30-14-16-32-18-17-31-15-13-29-11-9-27-7-5-25-3-1-19(23)24/h1-18H2,(H,23,24)
|
| Chemical Name |
3-[2-[2-[2-[2-[2-[2-[2-(2-azidoethoxy)ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]propanoic acid
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, 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)
|
| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~213.90 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.35 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 (5.35 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 (5.35 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 | 2.1390 mL | 10.6950 mL | 21.3899 mL | |
| 5 mM | 0.4278 mL | 2.1390 mL | 4.2780 mL | |
| 10 mM | 0.2139 mL | 1.0695 mL | 2.1390 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
