| Size | Price | Stock | Qty |
|---|---|---|---|
| 250mg |
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| 500mg | |||
| Other Sizes |
| Targets |
THP-PEG7 is a linker molecule rather than a drug with a specific biological target. It is classified as a PROTAC linker and an ADC linker. The THP (tetrahydropyranyl) group serves as a protecting group for the hydroxyl functionality, which can be deprotected for further conjugation. The PEG7 spacer provides hydrophilicity and flexibility to the linker. PROTACs contain two different ligands connected by a linker: one is a ligand for an E3 ubiquitin ligase and the other is for the target protein.
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| ln Vitro |
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]. ADC is made up of antibodies that are connected to ADC cytotoxins by an ADC linker [2].
THP-PEG7 is a chemical linker and does not have direct biological activity. Its in vitro utility lies in its ability to serve as a linker in the synthesis of PROTACs and ADCs. The PEG spacer provides hydrophilicity, which improves the solubility of the final conjugates. The THP protecting group can be removed under acidic conditions to reveal a hydroxyl group for further functionalization. Specific biological activity data are not applicable as the compound is a linker rather than a pharmacologically active agent. |
| ln Vivo |
THP-PEG7 is a chemical linker and does not have direct in vivo biological activity. Its utility in vivo is as a component of PROTACs or ADCs, where it links the pharmacologically active moieties. As a non-cleavable PEG linker in ADCs, it provides stability in the circulation. PEGylation (attachment of PEG chains) is known to improve the pharmacokinetics of drugs by increasing solubility, reducing immunogenicity, and prolonging circulation time. The PEG7 spacer provides optimal spacing between the two functional groups in the final conjugate.
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| Enzyme Assay |
As a chemical linker, THP-PEG7 is used in chemical synthesis rather than in biological enzyme assays. The THP protecting group can be removed under acidic conditions (e.g., with p-toluenesulfonic acid in methanol) to reveal a hydroxyl group. The hydroxyl group can then be activated (e.g., with tosyl chloride or converted to a leaving group) for conjugation to other molecules. The PEG linker can be used to connect a target protein ligand to an E3 ubiquitin ligase ligand in PROTAC synthesis, or to connect an antibody to a payload in ADC synthesis. Standard organic synthesis protocols are employed.
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| Cell Assay |
For in vitro cell-based assays using PROTACs synthesized with THP-PEG7, target cells are treated with the PROTAC at various concentrations (typically 0.01-100 μM) for 24-72 hours. Target protein degradation is assessed by Western blot analysis. Cell viability is measured using MTT or similar assays. For ADCs synthesized with THP-PEG7, cells expressing the target antigen are treated with the ADC, and cell killing is assessed by viability assays. The PEG linker is designed to be non-cleavable, providing stability in biological systems. Specific protocols depend on the target protein and the therapeutic design.
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| Animal Protocol |
In vivo animal studies for THP-PEG7 would involve administering PROTACs or ADCs synthesized using this linker. The compound itself is not administered as a therapeutic agent. For PROTACs, the in vivo efficacy is assessed in tumor xenograft models, where the PROTAC is administered intraperitoneally or intravenously. Target protein degradation is measured in tumor tissues by Western blot. Tumor volume and body weight are monitored. For ADCs, similar protocols are used, with additional assessment of antibody targeting and payload release. PEGylation with the hydrophilic PEG7 spacer is expected to improve solubility and pharmacokinetics.
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| ADME/Pharmacokinetics |
THP-PEG7 is a PEG-based linker with a tetrahydropyranyl (THP) protecting group and a PEG7 spacer. The compound is a PROTAC linker of the Polyethylene glycol (PEG) category. It is also a non-cleavable PEG linker used in ADC synthesis. Detailed solubility, stability, and storage conditions are not extensively provided in the available literature. The compound's utility is in the synthesis of therapeutic agents rather than as a therapeutic agent itself. Detailed pharmacokinetic parameters are not applicable.
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| Toxicity/Toxicokinetics |
As a chemical linker, THP-PEG7 is not a pharmacologically active compound and does not have direct toxicity. Toxicity would be associated with the final therapeutic agents (PROTACs or ADCs) synthesized using this linker. The PEG component is generally considered biocompatible and non-toxic. The THP protecting group is also considered safe. Standard toxicology assessments would be performed on the final therapeutic agent rather than the linker alone. No specific toxicity data for THP-PEG7 are provided in the available literature.
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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.
[2]. Masahiro Tomita, et al. Antibody specifically recognizing resin plasticizer compound. WO2005105846A1. |
| Additional Infomation |
THP-PEG7 is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs. It contains a tetrahydropyranyl (THP) protecting group and a PEG7 spacer. THP-PEG7 is also a non-cleavable PEG linker used in the synthesis of antibody-drug conjugates (ADCs). The compound is classified as a Polyethylene glycol (PEG) category linker. It may be utilized to prepare PROTAC protein degraders. PEGylation is known to improve the pharmacokinetics of drugs. No approved therapeutic status is reported.
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| Molecular Formula |
C17H34O8
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|---|---|
| Molecular Weight |
366.447066783905
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| Exact Mass |
232.096
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| CAS # |
42607-87-4
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| PubChem CID |
11035934
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| Appearance |
Colorless to light yellow liquid（Density：1.10±0.1 g/cm3）
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| LogP |
0.903
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
18
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| Heavy Atom Count |
25
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| Complexity |
267
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O1CCCCC1OCCOCCOCCOCCOCCOCCO
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| InChi Key |
ABJWCLPYMPRGRB-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C17H34O8/c18-4-6-19-7-8-20-9-10-21-11-12-22-13-14-23-15-16-25-17-3-1-2-5-24-17/h17-18H,1-16H2
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| Chemical Name |
2-[2-[2-[2-[2-[2-(oxan-2-yloxy)ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethanol
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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 | 2.7289 mL | 13.6444 mL | 27.2889 mL | |
| 5 mM | 0.5458 mL | 2.7289 mL | 5.4578 mL | |
| 10 mM | 0.2729 mL | 1.3644 mL | 2.7289 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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