| Size | Price | Stock | Qty |
|---|---|---|---|
| 500mg |
|
||
| 1g | |||
| Other Sizes |
Purity: ≥98%
| Targets |
Non-cleavable PEG Linker; PROTAC linker
Azido-PEG3-acid is classified as a PROTAC linker, an ADC linker, and a click chemistry reagent. The azide group can react with alkyne, BCN, or DBCO via click chemistry. The carboxylic acid group can be used for conjugation to primary amines. |
|---|---|
| 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 targets and selectively degrades target proteins by means of the intracellular ubiquitin-proteasome system. An ADC cytotoxin is connected to an antibody by use of an ADC linker to form an ADC.
Azido-PEG3-acid is used as a linker in the synthesis of PROTACs such as BI-3663, BI-4216, and BI-0319. It is also used in ADC synthesis. It is not typically evaluated for direct biological activity as a standalone compound. |
| ln Vivo |
Azido-PEG3-acid is not typically evaluated for in vivo activity as a standalone compound. Its role is in the synthesis of PROTACs or ADCs, which are then evaluated in vivo. The PEG spacer can improve the pharmacokinetic properties of the conjugated molecules.
|
| Enzyme Assay |
Azido-PEG3-acid is a chemical reagent, and its purity and identity are confirmed using analytical techniques such as NMR and HPLC. It is not typically used in enzyme or receptor binding assays. Its reactivity can be assessed by reacting it with amines or alkyne-containing compounds.
|
| Cell Assay |
Azido-PEG3-acid is not typically used in cell-based assays as a standalone compound. Its primary application is in the synthesis of PROTACs or ADCs, which are then tested in cell-based assays for their activity.
|
| Animal Protocol |
Azido-PEG3-acid is not typically used in in vivo animal studies as a standalone compound. It is used to synthesize PROTACs or ADCs, which are then evaluated in animal models. The PEG spacer can influence the pharmacokinetics of the conjugated molecules.
|
| ADME/Pharmacokinetics |
Azido-PEG3-acid has a molecular weight of 261.28 and a formula of C9H17N3O5. It contains an azide group and a terminal carboxylic acid. It is a monodisperse PEG molecule that is soluble in aqueous media.
|
| Toxicity/Toxicokinetics |
Specific toxicology data for Azido-PEG3-acid are not detailed in the available literature. As a linker used in PROTAC or ADC research, its toxicity is typically assessed as part of the final conjugated product. Standard safety precautions should be taken when handling this compound.
|
| References | |
| Additional Infomation |
3-{2-[2-(2-azidoethoxy)ethoxy]ethoxy}propionic acid is an organic nitrogen compound.
Azido-PEG3-acid is a PEG-based linker used in the synthesis of PROTACs and ADCs. It is a click chemistry reagent containing an azide group, which can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAC) with alkyne-containing molecules. It is a research tool for targeted protein degradation and cancer therapy. |
| Molecular Formula |
C9H17N3O5
|
|---|---|
| Molecular Weight |
247.248
|
| Exact Mass |
247.116
|
| Elemental Analysis |
C, 43.72; H, 6.93; N, 17.00; O, 32.35
|
| CAS # |
1056024-94-2
|
| Related CAS # |
2341740-84-7 (PROTAC BI-3663)
|
| PubChem CID |
59542208
|
| Appearance |
Colorless to light yellow liquid
|
| LogP |
-0.71
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
7
|
| Rotatable Bond Count |
12
|
| Heavy Atom Count |
17
|
| Complexity |
243
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
C(COCCOCCOCCN=[N+]=[N-])C(=O)O
|
| InChi Key |
VWJGWKZZFZMGGY-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C9H17N3O5/c10-12-11-2-4-16-6-8-17-7-5-15-3-1-9(13)14/h1-8H2,(H,13,14)
|
| Chemical Name |
3-[2-[2-(2-azidoethoxy)ethoxy]ethoxy]propanoic acid
|
| Synonyms |
Azido-PEG3-acid; 1056024-94-2; N3-PEG3-CH2CH2COOH; Azido-dPEG4-acid; 3-(2-(2-(2-azidoethoxy)ethoxy)ethoxy)propanoic acid; MFCD23726617; 3-[2-[2-(2-azidoethoxy)ethoxy]ethoxy]propanoic acid; 3-{2-[2-(2-AZIDOETHOXY)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: 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) |
DMSO : ~100 mg/mL (~404.45 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (10.11 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 (10.11 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 (10.11 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 | 4.0445 mL | 20.2224 mL | 40.4449 mL | |
| 5 mM | 0.8089 mL | 4.0445 mL | 8.0890 mL | |
| 10 mM | 0.4044 mL | 2.0222 mL | 4.0445 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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