| Size | Price | Stock | Qty |
|---|---|---|---|
| 50mg |
|
||
| 100mg |
|
||
| 250mg |
|
||
| 500mg | |||
| Other Sizes |
| Targets |
As a linker, Aminooxy-PEG2-azide does not have a traditional biological target. It is a chemical tool used to connect two functional molecules. In PROTACs, it links a ligand for an E3 ubiquitin ligase to a ligand for a target protein. In ADCs, it connects an antibody to a cytotoxic payload. The PEG spacer enhances aqueous solubility and reduces steric hindrance.
|
|---|---|
| ln Vitro |
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]. ADC is made up of antibodies that are connected to ADC cytotoxins by an ADC linker [2].
In vitro, Aminooxy-PEG2-azide functions as a linker in the synthesis of PROTACs and ADCs. Its utility is demonstrated by the successful creation of these bioconjugates. The resulting PROTACs can induce targeted protein degradation, and the resulting ADCs can deliver cytotoxic payloads to cancer cells. The linker's bioorthogonal chemistry allows for site-specific conjugation. |
| ln Vivo |
In vivo applications of Aminooxy-PEG2-azide are realized through the PROTACs or ADCs it helps construct. These conjugates are designed to have therapeutic effects, such as targeted protein degradation or cancer cell killing. The linker's stability and the properties of the PEG spacer influence the conjugate's pharmacokinetics and efficacy.
|
| Enzyme Assay |
In vitro assays for Aminooxy-PEG2-azide typically involve demonstrating its reactivity in click chemistry and oxime ligation. The formation of an oxime bond can be confirmed by mass spectrometry or NMR. The CuAAc reaction with an alkyne-containing compound can be monitored by HPLC or by detecting the formation of a triazole product. These protocols are for research purposes only.
|
| Cell Assay |
In vitro cell-based assays for Aminooxy-PEG2-azide are performed on the final PROTAC or ADC, not the linker alone. For PROTACs, target protein degradation is assessed by Western blot. For ADCs, cytotoxicity is measured using cell viability assays on target antigen-expressing cells. The linker's contribution to the conjugate's solubility and cell permeability can be evaluated in these systems. Standard cell culture conditions are used.
|
| Animal Protocol |
In vivo animal studies for Aminooxy-PEG2-azide are conducted with the final PROTAC or ADC. Typical protocols involve xenograft mouse models to evaluate antitumor efficacy. The conjugate is administered intravenously, and tumor growth inhibition is monitored. Pharmacodynamic studies assess target degradation (for PROTACs) or target engagement (for ADCs). Pharmacokinetic studies evaluate the conjugate's half-life and distribution. All procedures must comply with institutional animal care guidelines.
|
| ADME/Pharmacokinetics |
The pharmacokinetic properties of Aminooxy-PEG2-azide are not characterized independently. The PEG2 spacer contributes to the overall conjugate's properties by increasing hydrophilicity and reducing aggregation. The linker's stability in biological fluids is an important factor for the conjugate's PK profile. The compound is for research use only.
|
| Toxicity/Toxicokinetics |
The toxicity profile of Aminooxy-PEG2-azide is evaluated as part of the final conjugate. The linker itself is designed to be non-toxic and stable. Its degradation products are expected to be biocompatible. The toxicity of the conjugate is primarily determined by the payload and the target.
|
| References | |
| Additional Infomation |
Additional information: Aminooxy-PEG2-azide has the CAS number 1043426-13-6. It is a heterobifunctional PEG linker. It is used in PROTAC and ADC synthesis. It contains an aminooxy group for oxime ligation and an azide group for click chemistry. This product is for research use only and is not approved for clinical or therapeutic applications.
|
| Molecular Formula |
C6H14N4O3
|
|---|---|
| Molecular Weight |
190.200360774994
|
| Exact Mass |
190.106
|
| CAS # |
1043426-13-6
|
| PubChem CID |
102474663
|
| Appearance |
Colorless to light yellow liquid
|
| LogP |
-0.1
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
6
|
| Rotatable Bond Count |
9
|
| Heavy Atom Count |
13
|
| Complexity |
149
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
C(COCCOCCON)N=[N+]=[N-]
|
| InChi Key |
GCURLNTZWQFVMK-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C6H14N4O3/c7-10-9-1-2-11-3-4-12-5-6-13-8/h1-6,8H2
|
| Chemical Name |
O-[2-[2-(2-azidoethoxy)ethoxy]ethyl]hydroxylamine
|
| 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: This product requires protection from light (avoid light exposure) during transportation and storage. |
| 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) |
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
|
|---|---|
| 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 | 5.2576 mL | 26.2881 mL | 52.5762 mL | |
| 5 mM | 1.0515 mL | 5.2576 mL | 10.5152 mL | |
| 10 mM | 0.5258 mL | 2.6288 mL | 5.2576 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
