| Size | Price | Stock | Qty |
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| 25mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
| Targets |
PEGs
Mal-NH-PEG8-Boc does not target biological receptors; it is a chemical linker used in PROTAC (proteolysis-targeting chimera) synthesis and bioconjugation applications. The Boc group protects the amine during synthesis, allowing selective deprotection under acidic conditions to enable subsequent coupling to target ligands. |
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| ln Vitro |
A linker separates the two ligands that make up PROTACs; one ligand is for an E3 ubiquitin ligase, and the other is for the target protein. Target proteins are selectively degraded by PROTACs by taking advantage of the intracellular ubiquitin-proteasome system[1].
Not available. When incorporated into PROTACs, Mal-NH-PEG8-Boc enables conjugation of E3 ubiquitin ligase ligands and target protein ligands. The PEG8 spacer provides optimal flexibility and distance between binding moieties. Linker composition and length influence the formation of stable ternary complexes and degradation efficacy. |
| ln Vivo |
Not available. PROTACs assembled using Mal-NH-PEG8-Boc have demonstrated target protein degradation in cellular assays. In vivo, PEG8-based PROTAC linkers generally improve pharmacokinetic properties including extended half-life, reduced immunogenicity, and enhanced tissue distribution compared to non-PEGylated linkers.
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| Enzyme Assay |
Not available. Standard Boc deprotection assays involve treating Mal-NH-PEG8-Boc with 20-50% trifluoroacetic acid (TFA) in dichloromethane for 30-60 minutes at room temperature, followed by evaporation to remove TFA. Deprotected amine is then reacted with NHS-ester ligands in DMSO or DMF. Maleimide-thiol conjugation efficiency is assessed by Ellman's assay.
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| Cell Assay |
Not available. For PROTAC activity assessment, typical protocols involve treating target-expressing cells with PROTACs synthesized using Mal-NH-PEG8-Boc (0.001-10 uM) for 4-24 hours, followed by Western blotting to measure degradation of the target protein. The PEG8 spacer does not exhibit cellular toxicity as it is not pharmacologically active.
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| Animal Protocol |
Not available. For in vivo evaluation, PROTACs containing Mal-NH-PEG8-Boc linkers are typically administered intravenously or intraperitoneally (10-100 mg/kg) in tumor-bearing mice. Efficacy is assessed by target protein knockdown in tumor tissue by Western blot at 6-24 hours, and tumor growth inhibition is monitored over 2-4 weeks.
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| ADME/Pharmacokinetics |
The PEG8 spacer improves aqueous solubility, reduces aggregation, and minimizes non-specific interactions. The Boc-protected amine is stable under basic and neutral conditions but is cleaved under acidic conditions (e.g., 20-50% TFA). The maleimide group reacts specifically with reduced thiols at pH 6.5-7.5.
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| Toxicity/Toxicokinetics |
Boc-deprotection using TFA is generally safe under fume hood conditions. The maleimide group can cause skin and respiratory irritation. Mal-NH-PEG8-Boc is not intended for in vivo use as a free compound. Specific toxicological data for this linker are not reported.
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| References | |
| Additional Infomation |
Mal-NH-PEG8-Boc is a research-grade PROTAC linker used to construct targeted protein degraders. It has not entered clinical trials nor been approved for therapeutic use. The Boc protecting group enables orthogonal protection strategies for multi-step bioconjugation. This product is for laboratory research in targeted protein degradation and chemical biology.
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| Molecular Formula |
C30H52N2O13
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|---|---|
| Appearance |
Typically exists as solid at room temperature
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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. |
| 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) |
DMSO :~500 mg/mL (~770.72 mM)
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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.) |
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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