| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| Other Sizes |
| Targets |
No biological protein target. APN-PEG36-tetrazine is a chemical linker that reacts with trans-cyclooctene (TCO)-modified biomolecules (e.g., antibodies, nanoparticles). The tetrazine group undergoes highly specific and rapid iEDDA click chemistry with TCO under physiological conditions without copper catalysis.
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| ln Vitro |
ADCs are made up of an antibody and an ADC cytotoxin that are joined together by an ADC linker[1].
The iEDDA reaction between tetrazine and TCO is one of the fastest bioorthogonal ligations with rate constants up to 10⁶ M-¹s-¹. APN-PEG36-tetrazine reacts with TCO-modified antibodies or payloads to form stable covalent conjugates. The long PEG36 spacer reduces steric hindrance and enhances aqueous solubility. |
| ln Vivo |
In vivo, APN-PEG36-tetrazine can be used for pretargeted imaging or therapy. TCO-modified antibodies are administered first to localize to tumor targets, followed by injection of radiolabeled or drug-loaded tetrazine reagents (e.g., APN-PEG36-tetrazine conjugates). The rapid click reaction enables site-specific payload delivery.
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| Enzyme Assay |
To validate tetrazine reactivity, purified APN-PEG36-tetrazine is mixed with a TCO-containing small molecule (e.g., TCO-fluorophore) in PBS at 37degC. The reaction progress is monitored by HPLC or LC-MS to calculate the second-order rate constant. Conjugation efficiency is assessed by disappearance of starting materials and appearance of product.
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| Cell Assay |
Not applicable. APN-PEG36-tetrazine is a chemical reagent used for conjugation and not tested in cell-based functional assays in the traditional sense. However, cells expressing cell-surface TCO (via metabolic labeling or antibody binding) can be incubated with tetrazine-fluorophore to visualize and quantify click reaction efficiency by flow cytometry or fluorescence microscopy.
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| Animal Protocol |
In mouse xenograft models for pretargeted imaging: A TCO-modified tumor-targeting antibody is injected intravenously (e.g., 24-48 h prior). Then, a radiolabeled or fluorophore-labeled tetrazine probe (e.g., APN-PEG36-tetrazine conjugate) is administered. Tumor uptake is measured by PET/CT or fluorescence imaging. In therapeutic models, drug payloads are used.
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| ADME/Pharmacokinetics |
As a PEGylated linker with high molecular weight, APN-PEG36-tetrazine has prolonged circulation time and reduced immunogenicity compared to shorter PEG linkers. The tetrazine group is stable under physiological conditions for hours but can undergo slow hydrolysis. The compound is typically formulated in PBS or DMSO for in vivo use.
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| Toxicity/Toxicokinetics |
No toxicity data specific to APN-PEG36-tetrazine. PEG linkers are generally considered biocompatible and non-toxic at the doses used for pretargeting (typically ug to low mg range). Tetrazine groups have low acute toxicity. Standard safety precautions for handling chemical reagents apply.
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| References |
[1]. Beck A, et, al. Strategies and challenges for the next generation of antibody-drug conjugates. Nat Rev Drug Discov. 2017 May;16(5):315-337.
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| Additional Infomation |
APN-PEG36-tetrazine is a research-grade click chemistry linker, not approved for clinical use. The long PEG36 spacer (≈ 36 ethylene glycol units, ~1.5-2 kDa) provides excellent hydrophilicity and steric flexibility. It is commonly used in pretargeted radioimmunotherapy (PRIT) and ADC synthesis. Strictly for research applications.
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| Molecular Formula |
C94H161N7O38
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| Molecular Weight |
1997.30
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| Appearance |
Pink to red solid powder
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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: (1). This product requires protection from light (avoid light exposure) during transportation and storage. (2). Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture. |
| 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 | 0.5007 mL | 2.5034 mL | 5.0068 mL | |
| 5 mM | 0.1001 mL | 0.5007 mL | 1.0014 mL | |
| 10 mM | 0.0501 mL | 0.2503 mL | 0.5007 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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