| Size | Price | Stock | Qty |
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| 500mg |
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| 1g |
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| Other Sizes |
Purity: ≥98%
| Targets |
Azido-PEG5-alcohol is a heterobifunctional PEG linker used in the synthesis of ADCs and PROTACs. The azide group can react with alkyne, BCN, and DBCO via click chemistry to yield a stable triazole linkage. The terminal hydroxyl group enables further derivatization or replacement with other reactive functional groups. The PEG5 spacer provides a balance of properties between shorter and longer PEG linkers, enhancing solubility and stability of the resulting conjugates. The compound is extensively utilized in bioconjugation techniques, particularly for labeling and imaging applications.
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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, Azido-PEG5-alcohol is used as a building block for the synthesis of ADCs and PROTACs. ADCs consist of an antibody linked to a cytotoxic payload via an ADC linker. PROTACs contain two distinct ligands connected by a linker: one for an E3 ubiquitin ligase and the other for the target protein, utilizing the intracellular ubiquitin-proteasome system to selectively degrade target proteins. The PEG spacer enhances the solubility and stability of the resulting conjugates in aqueous solutions. The azide group enables precise attachment to alkyne-modified biomolecules. |
| ln Vivo |
In vivo, Azido-PEG5-alcohol is not administered directly but is used to synthesize ADCs and PROTACs that are evaluated in animal models. The PEG spacer enhances the solubility, stability, and bioavailability of the resulting conjugates. The compound's role as a linker in ADC synthesis enables targeted delivery of chemotherapeutics with reduced systemic toxicity. In PROTAC development, the PEG linker facilitates the formation of chimeric molecules that induce degradation of disease-relevant proteins. Its utility in drug development has been validated in various preclinical studies involving ADC and PROTAC-based therapeutics.
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| Enzyme Assay |
In cell-free biochemical assays, Azido-PEG5-alcohol is characterized for its chemical properties and conjugation efficiency. The compound's purity (>98%) is determined using analytical techniques such as HPLC. Its reactivity with alkyne-containing molecules via click chemistry is assessed. The compound's solubility in DMSO (10 mM) and aqueous media is evaluated. Its stability under various storage conditions is assessed to ensure the integrity of the linker for long-term research use. The compound's LogP of -1.59 indicates high hydrophilicity.
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| Cell Assay |
Cellular assays for Azido-PEG5-alcohol are evaluated indirectly through the biological activity of the ADCs or PROTACs synthesized using this linker. The resulting ADCs are tested for their ability to bind to target antigens and deliver cytotoxic payloads to cancer cells. The resulting PROTACs are tested for their ability to degrade target proteins. The PEG linker's effect on cellular uptake, intracellular trafficking, and biological activity is assessed. The compound itself is not biologically active and serves only as a structural component.
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| Animal Protocol |
Animal models for Azido-PEG5-alcohol 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 and protein degradation has been demonstrated in various preclinical studies. Its utility in drug development continues to be explored.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for Azido-PEG5-alcohol are not typically reported, as the compound is a linker rather than a therapeutic agent. The compound has a molecular weight of 263.29 g/mol with a molecular formula of C10H21N3O5. The CAS number is 86770-68-5. The compound appears as a colorless to light orange to yellow clear liquid. It has a LogP of -1.59, indicating high water solubility. It is soluble in DMSO (10 mM). The compound should be stored at -20°C and kept in a dry place away from sunlight.
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| Toxicity/Toxicokinetics |
The toxicity profile of Azido-PEG5-alcohol indicates that it has low toxicity and high water solubility, making it an ideal candidate for drug delivery applications. The compound is supplied at >97% purity and is intended for research use only. Standard safety precautions for handling laboratory chemicals apply, including the use of appropriate personal protective equipment. The azide group may pose a hazard if heated or subjected to shock, as azides can be explosive. The compound is not intended for human use or therapeutic applications.
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| References | |
| Additional Infomation |
Azido-PEG5-alcohol is a non-cleavable 5-unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs) and PROTACs. It contains an azide group for click chemistry and a terminal hydroxyl group for further derivatization. The hydrophilic PEG spacer increases solubility in aqueous media. The compound is extensively utilized in bioconjugation techniques for labeling and imaging applications. It has low toxicity and high water solubility. The compound has a molecular weight of 263.29 g/mol and formula C10H21N3O5. The CAS number is 86770-68-5.
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| Molecular Formula |
C10H21N3O5
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|---|---|
| Molecular Weight |
263.2908
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| Exact Mass |
263.148
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| CAS # |
86770-68-5
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| Related CAS # |
86770-68-5;
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| PubChem CID |
70702325
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| Appearance |
Colorless to light yellow liquid
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| Flash Point |
100 °C
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| Index of Refraction |
1.47
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| LogP |
-1.59
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
14
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| Heavy Atom Count |
18
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| Complexity |
212
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| Defined Atom Stereocenter Count |
0
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| SMILES |
[N-]=[N+]=NCCOCCOCCOCCOCCO
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| InChi Key |
JTGGTGKXQQGEHB-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C10H21N3O5/c11-13-12-1-3-15-5-7-17-9-10-18-8-6-16-4-2-14/h14H,1-10H2
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| Chemical Name |
2-[2-[2-[2-(2-azidoethoxy)ethoxy]ethoxy]ethoxy]ethanol
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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 | 3.7981 mL | 18.9905 mL | 37.9809 mL | |
| 5 mM | 0.7596 mL | 3.7981 mL | 7.5962 mL | |
| 10 mM | 0.3798 mL | 1.8990 mL | 3.7981 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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