| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| Other Sizes |
| Targets |
No specific biological target. Tetrazine-PEG7-amine hydrochloride is a chemical linker used in bioconjugation. The tetrazine group reacts with TCO via bioorthogonal click chemistry (iEDDA), enabling the selective conjugation of two molecules. The amine group serves as a handle for coupling to carboxylic acids or activated esters on targeting antibodies or cytotoxic payloads.
|
|---|---|
| ln Vitro |
ADCs are made up of an antibody and an ADC cytotoxin that are joined together by an ADC linker[1].
Tetrazine-PEG7-amine hydrochloride is not directly tested for biological activity. Instead, it is used to conjugate a targeting antibody to a cytotoxic payload to create an ADC. The ADC‘s in vitro potency is then tested on target-positive and target-negative cancer cells. The PEG7 linker contributes to the ADC's solubility, stability, and pharmacokinetic properties. |
| ln Vivo |
In vivo, when incorporated into an ADC, the tetrazine-PEG7-amine linker enables the targeted delivery of a cytotoxic payload to tumor cells. The ADC is internalized by target cancer cells, and the linker releases the payload, resulting in potent and selective tumor growth inhibition. The PEG7 spacer enhances the ADC's circulating half-life and reduces aggregation.
|
| Enzyme Assay |
Bioorthogonal click chemistry conjugation: A TCO-modified antibody or protein (1-10 mg/mL in PBS, pH 7.4) is incubated with Tetrazine-PEG7-amine hydrochloride (2-10 equivalents) for 2-24 h at 4degC or room temperature. The reaction is monitored by LC-MS or SDS-PAGE. The tetrazine-TCO iEDDA reaction proceeds rapidly without requiring catalysts, making it ideal for sensitive biomolecules.
|
| Cell Assay |
ADC internalization and potency assay: Target-positive cancer cells are seeded in 96-well plates and treated with an ADC synthesized using Tetrazine-PEG7-amine hydrochloride (0-100 nM, 72-96 h). Cell viability is assessed by CCK-8 or CellTiter-Glo. Internalization of the ADC is confirmed by confocal microscopy using a fluorescently labeled secondary reagent. IC50 values are calculated by non-linear regression.
|
| Animal Protocol |
Xenograft tumor model: Mice bearing target-positive tumor xenografts are treated with an ADC synthesized using Tetrazine-PEG7-amine hydrochloride (1-10 mg/kg, i.v., once weekly for 2-3 weeks). Tumor volume is measured twice weekly. At study termination, tumors are collected for immunohistochemistry to assess target engagement, payload release, and apoptosis (cleaved caspase-3, Ki-67).
|
| ADME/Pharmacokinetics |
Pharmacokinetic data for Tetrazine-PEG7-amine hydrochloride alone are not applicable. When used in an ADC, the PEG7 linker contributes to the conjugate's overall stability and prolonged circulation time (half-life of days). The molecular weight of the linker is 603.11 (hydrochloride salt). It is soluble in DMSO and aqueous buffers. For storage, keep at 4degC, sealed, away from moisture.
|
| Toxicity/Toxicokinetics |
Toxicity data for the linker alone are not applicable. When used in an ADC, toxicity is primarily driven by the cytotoxic payload and target expression. Tetrazine groups may be immunogenic, but PEGylation reduces this risk. The hydrochloride salt form improves aqueous solubility. The compound is for research use only and not for human therapeutic use.
|
| 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.
|
| Additional Infomation |
Tetrazine-PEG7-amine hydrochloride is a research-grade ADC linker and click chemistry reagent. It has not been approved for clinical use. The tetrazine-TCO iEDDA reaction is a powerful tool for the site-specific conjugation of biomolecules, enabling the creation of homogeneous ADCs and other bioconjugates. For research use only.
|
| Molecular Formula |
C26H43CLN6O8
|
|---|---|
| Appearance |
Purple to purplish red solid powder
|
| 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: Please store this product in a sealed and protected environment, 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)
|
| 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.) |
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
