| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg | |||
| Other Sizes |
| Targets |
Not applicable. N-(NHS ester-PEG2)-N-bis(PEG3-azide) is a PROTAC linker and PEG-based chemical reagent. It has no direct biological target. The NHS ester group reacts with primary amines (e.g., lysine residues on proteins) to form stable amide bonds. The two terminal azide groups can participate in copper-catalyzed azide-alkyne cycloaddition (CuAAC) click chemistry reactions, allowing conjugation to alkyne-containing molecules. The PEG spacers (PEG2 and PEG3) increase water solubility and flexibility.
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| ln Vitro |
The compound itself has no direct in vitro biological activity. It is a building block for PROTAC synthesis and bioconjugation. Its activity is assessed after conjugation to an E3 ligase ligand and a target protein ligand. The resulting PROTAC is then evaluated for its ability to induce target protein degradation in cells. The NHS ester group reacts with primary amines under mild conditions (pH 7-8), and the azide groups are stable and biocompatible.
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| ln Vivo |
The compound is not a drug; it is a PROTAC linker and bioconjugation reagent. PROTACs synthesized using this linker can have potent in vivo activity. In xenograft mouse models, PROTACs are administered intraperitoneally or intravenously (10-100 mg/kg) once daily for 2-4 weeks. They induce sustained degradation of target proteins in tumors (>80% reduction) and inhibit tumor growth. This linker can be used for the synthesis of PROTACs and other conjugates.
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| Enzyme Assay |
Not applicable. N-(NHS ester-PEG2)-N-bis(PEG3-azide) is a PROTAC linker and bioconjugation reagent, not a standard enzyme inhibitor. Its purity (>98%) is assessed by HPLC. The structure is confirmed by ¹H NMR, ¹3C NMR, and mass spectrometry (ESI-MS, expected [M+H]+ m/z 705). Physicochemical properties: MW 704.73, colorless to light yellow liquid, soluble in DMSO. The NHS ester is reactive with primary amines; the azide groups are stable.
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| Cell Assay |
Not applicable. N-(NHS ester-PEG2)-N-bis(PEG3-azide) is not used directly in cell-based assays; it is a building block for PROTAC synthesis. For PROTAC evaluation, cells expressing the target protein are seeded in 6-well plates (3×10⁵ cells/well) and treated with the PROTAC (0.1-1000 nM) for 4-24 h. Target protein degradation is assessed by Western blotting. DC₅0 is calculated from the dose-response curve. Cell viability is measured by MTT or CellTiter-Glo.
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| Animal Protocol |
In vivo efficacy of PROTACs incorporating this linker can be evaluated in xenograft mouse models. Female BALB/c nude mice (6-8 wk) are subcutaneously inoculated with 5×10⁶ cancer cells. When tumors reach ~100-150 mm3, mice are randomized into treatment groups (n=6-8/group). The PROTAC is formulated in 10% DMSO + 40% PEG300 + 5% Tween 80 + 45% saline and administered intraperitoneally at 10-100 mg/kg once daily or every other day for 2-4 weeks. Tumor volume is measured every 3 days, and tumors are excised for Western blot analysis.
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| ADME/Pharmacokinetics |
No specific PK data is available for N-(NHS ester-PEG2)-N-bis(PEG3-azide) alone. When incorporated into a PROTAC (MW 800-1200), the overall PK properties are determined by the full PROTAC molecule. PROTACs generally have moderate to low oral bioavailability (<20%), short plasma half-life (1-4 h), high plasma protein binding (>90%), and rapid clearance. The PEG2 and PEG3 linkers improve solubility and may reduce aggregation.
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| Toxicity/Toxicokinetics |
For N-(NHS ester-PEG2)-N-bis(PEG3-azide), hazard statements: H315 (Causes skin irritation), H319 (Causes serious eye irritation), H335 (May cause respiratory irritation). Signal word: Warning. Precautionary statements: P261 (Avoid breathing dust/fume/gas/mist/vapors/spray), P280 (Wear protective gloves/protective clothing/eye protection/face protection), P305+P351+P338 (IF IN EYES: Rinse cautiously with water for several minutes). Storage: at -20degC, sealed, under inert gas (nitrogen), protect from light and moisture.
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| References | |
| Additional Infomation |
N-(NHS ester-PEG2)-N-bis(PEG3-azide) (MW 704.73) is a research-grade PEG-based PROTAC linker and click chemistry reagent. It is not an FDA-approved drug. It is used for the synthesis of PROTACs and bioconjugates via NHS ester-amine coupling and CuAAC click chemistry. For research use only, not for diagnostic or therapeutic applications.
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| Molecular Formula |
C28H48N8O13
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|---|---|
| Molecular Weight |
704.73
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| Appearance |
Colorless to light yellow liquid
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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 Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
| 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 | 1.4190 mL | 7.0949 mL | 14.1898 mL | |
| 5 mM | 0.2838 mL | 1.4190 mL | 2.8380 mL | |
| 10 mM | 0.1419 mL | 0.7095 mL | 1.4190 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
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