| Size | Price | Stock | Qty |
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| 10mg |
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| 25mg |
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| 50mg | |||
| Other Sizes |
| Targets |
(2E)-TCO-PEG4-NHS ester targets proteins for degradation via the PROTAC mechanism. The NHS ester reacts with primary amines on target proteins or ligands, while the TCO group enables bioorthogonal click chemistry with tetrazine-modified partners. The PEG4 spacer provides water solubility and flexibility.
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| ln Vitro |
One ligand is for an E3 ubiquitin ligase, and the other is for the target protein; these two ligands are joined by a linker to form PROTACs. The intracellular ubiquitin-proteasome system is utilized by PROTACs to specifically destroy target proteins[1].
In vitro, (2E)-TCO-PEG4-NHS ester is used to synthesize PROTAC molecules that induce targeted protein degradation. The NHS ester reacts with amine groups on proteins or small molecules to form stable amide bonds. The TCO group enables subsequent conjugation via inverse electron demand Diels-Alder reaction with tetrazines. |
| ln Vivo |
In vivo, (2E)-TCO-PEG4-NHS ester is used as a linker in the preparation of PROTACs for therapeutic applications. The resulting PROTACs can be administered to animals to induce degradation of target proteins. Its utility depends on the specific PROTAC construct.
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| Enzyme Assay |
The non-cellular assay for (2E)-TCO-PEG4-NHS ester involves standard chemical characterization to confirm its identity and purity. Techniques include HPLC, NMR, and mass spectrometry. The NHS ester functionality is confirmed by reaction with amine-containing compounds and monitoring by HPLC.
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| Cell Assay |
In vitro cell-based assays for (2E)-TCO-PEG4-NHS ester are not typically performed, as it is a linker rather than a biologically active compound. The PROTACs synthesized using this linker are evaluated in cell-based degradation assays using Western blotting to measure target protein levels.
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| Animal Protocol |
In vivo animal study protocols for (2E)-TCO-PEG4-NHS ester are not applicable, as it is a linker used in PROTAC synthesis. The resulting PROTACs are evaluated in animal models for efficacy and pharmacokinetics.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of (2E)-TCO-PEG4-NHS ester are not characterized as it is a linker rather than a therapeutic agent. The PEG4 spacer provides water solubility. When used in PROTACs, the PK properties are determined by the overall PROTAC molecule.
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| Toxicity/Toxicokinetics |
Toxicological data for (2E)-TCO-PEG4-NHS ester are not extensively reported. As a research compound, it is intended for laboratory use only. Standard safety precautions should be observed during handling.
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| References |
[1]. Nalawansha DA, et al. PROTACs: An Emerging Therapeutic Modality in Precision Medicine. Cell Chem Biol. 2020;27(8):998-1013.
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| Additional Infomation |
(2E)-TCO-PEG4-NHS ester is a heterobifunctional PEG linker used in PROTAC synthesis and protein modification. It contains a TCO group for click chemistry, a PEG4 spacer, and an NHS ester for amine coupling. It is not a therapeutic drug and has no clinical trial status.
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| Molecular Formula |
C24H38N2O10
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|---|---|
| Molecular Weight |
514.57
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| CAS # |
2269467-44-7
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| Related CAS # |
1621096-79-4;1613439-69-2
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| Appearance |
Pale Yellow Oily
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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 | 1.9434 mL | 9.7169 mL | 19.4337 mL | |
| 5 mM | 0.3887 mL | 1.9434 mL | 3.8867 mL | |
| 10 mM | 0.1943 mL | 0.9717 mL | 1.9434 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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