| Size | Price | Stock | Qty |
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| 100mg |
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| 250mg |
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| Other Sizes |
| Targets |
Azido-PEG9-acid is a heterobifunctional PEG linker used in the synthesis of ADCs and PROTACs. The azide group enables copper-catalyzed azide-alkyne cycloaddition (CuAAC) click chemistry with alkyne-containing molecules. The terminal carboxylic acid enables amide bond formation with amine-containing molecules. The PEG9 spacer provides enhanced solubility in aqueous media.
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| ln Vitro |
An ADC cytotoxin is connected to an antibody by use of an ADC linker to form an ADC. 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-PEG9-acid is used as a building block for the synthesis of ADCs and PROTACs. Its primary in vitro application is in bioconjugation chemistry, where it serves as a versatile linker to connect antibodies to cytotoxic payloads (ADCs) or target protein ligands to E3 ligase ligands (PROTACs). The PEG spacer enhances the solubility and stability of the resulting conjugates. |
| ln Vivo |
In vivo, Azido-PEG9-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, stability, and bioavailability of the resulting conjugates. The compound's role as a linker in ADC and PROTAC synthesis enables targeted drug delivery and protein degradation. Its utility has been validated in various preclinical studies.
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| Enzyme Assay |
In cell-free biochemical assays, Azido-PEG9-acid is characterized for its chemical properties and conjugation efficiency. Its molecular weight and molecular formula are determined using analytical techniques. Its reactivity with alkyne-containing molecules and amine-containing molecules is assessed. Its solubility in DCM, DMF, DMSO, methanol, and water is evaluated. Its stability under various storage conditions is assessed.
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| Cell Assay |
Cellular assays for Azido-PEG9-acid 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.
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| Animal Protocol |
Animal models for Azido-PEG9-acid involve evaluating the ADCs or PROTACs synthesized using this linker in preclinical studies. The resulting conjugates are tested in tumor xenograft models or disease models relevant to the target. The PEG linker's effect on pharmacokinetics, biodistribution, and efficacy is assessed.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for Azido-PEG9-acid are not typically reported, as the compound is a linker rather than a therapeutic agent. The compound has a molecular formula of C21H41N3O11. The CAS number is 1670249-37-2. The compound appears as a pale yellow oily matter. It is soluble in DCM, DMF, DMSO, methanol, and water. Standard handling procedures for PEG linkers apply.
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| Toxicity/Toxicokinetics |
The toxicity profile of Azido-PEG9-acid has not been extensively documented, as the compound is a linker rather than a pharmacologically active agent. The compound is intended for research use only. Standard safety precautions for handling laboratory chemicals apply. The azide group may pose a hazard if heated or subjected to shock.
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| References |
[1]. An S, et al. Small-molecule PROTACs: An emerging and promising approach for the development of targeted therapy drugs. EBioMedicine. 2018 Oct;36:553-562.
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| Additional Infomation |
Azido-PEG9-acid is a non-cleavable 9-unit PEG ADC linker used in the synthesis of ADCs and PROTACs. It contains an azide group for click chemistry and a terminal carboxylic acid. The CAS number is 1670249-37-2.
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| Molecular Formula |
C21H41N3O11
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| Molecular Weight |
511.563747167587
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| Exact Mass |
511.274
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| CAS # |
1670249-37-2
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| PubChem CID |
77078357
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| Appearance |
Colorless to light yellow liquid
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| LogP |
-2.86
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
13
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| Rotatable Bond Count |
30
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| Heavy Atom Count |
35
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| Complexity |
497
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O(CCOCCOCCOCCOCCN=[N+]=[N-])CCOCCOCCOCCOCCC(=O)O
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| InChi Key |
SITPDBHRMHFFHS-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C21H41N3O11/c22-24-23-2-4-28-6-8-30-10-12-32-14-16-34-18-20-35-19-17-33-15-13-31-11-9-29-7-5-27-3-1-21(25)26/h1-20H2,(H,25,26)
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| Chemical Name |
3-[2-[2-[2-[2-[2-[2-[2-[2-(2-azidoethoxy)ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]propanoic acid
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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 | 1.9548 mL | 9.7740 mL | 19.5480 mL | |
| 5 mM | 0.3910 mL | 1.9548 mL | 3.9096 mL | |
| 10 mM | 0.1955 mL | 0.9774 mL | 1.9548 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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