| Size | Price | Stock | Qty |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg |
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| Other Sizes |
| Targets |
The primary target of m-PEG5-Ms is not a biological receptor but nucleophilic functional groups. The mesylate group serves as an excellent leaving group for SN2 nucleophilic substitution reactions, enabling the attachment of various nucleophiles (amines, thiols, alcohols) to the PEG chain. In PROTACs and ADCs, it acts as a linker component.
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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 targets and selectively degrades target proteins by means of the intracellular ubiquitin-proteasome system. An ADC cytotoxin is connected to an antibody by use of an ADC linker to form an ADC.
As a chemical linker, m-PEG5-Ms does not exhibit intrinsic biological activity. Its utility is defined by its reactivity as an alkylating agent. The mesylate group can be displaced by nucleophiles to form new chemical bonds. The PEG5 spacer provides a balance between solubility and compactness. The compound is highly soluble in water and organic solvents. |
| ln Vivo |
No direct in vivo activity is attributed to m-PEG5-Ms. It functions exclusively as a synthetic intermediate or linker. Its in vivo relevance stems from its use in constructing ADCs and PROTACs, where the PEG5 spacer enhances solubility and reduces immunogenicity. The mesylate group is typically consumed during conjugation and does not persist in the final therapeutic molecule.
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| Enzyme Assay |
For non-cell-based assays, m-PEG5-Ms is characterized by NMR and HPLC (≥98% purity). The mesylate group's reactivity can be tested by reacting with a model nucleophile (e.g., benzylamine) and monitoring reaction progress by TLC or HPLC. Purity is assessed by GC or HPLC. The compound's solubility in various solvents can be determined.
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| Cell Assay |
Cell-based assays are not performed on m-PEG5-Ms alone. It is used as a building block to synthesize PROTACs or ADCs, which are then evaluated in cell culture. Standard protocols involve treating cancer cell lines with the conjugate at varying concentrations (0.001-10 µM) for 24-72 hours, followed by assessment of target protein degradation or cell viability.
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| Animal Protocol |
In vivo studies with m-PEG5-Ms are conducted using the final conjugate. Typical protocols involve administering the construct to rodent models via intravenous injection at doses of 1-10 mg/kg. The PEG5 spacer contributes to prolonged circulation half-life and reduced immunogenicity. Efficacy is assessed by tumor volume measurements or biomarker analysis.
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| ADME/Pharmacokinetics |
As a linker intermediate, m-PEG5-Ms does not have independent PK properties. The computed XLogP3-AA value is -0.9, indicating hydrophilicity. When incorporated into a final conjugate, the PEG5 spacer improves aqueous solubility and reduces clearance. The defined molecular weight ensures batch-to-batch consistency.
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| Toxicity/Toxicokinetics |
Toxicology data specific to m-PEG5-Ms are limited. The compound is handled with standard safety precautions. The mesylate group is an alkylating agent and may be reactive; however, at research concentrations, significant toxicity is unlikely. Store at -20°C for long-term stability. The compound is stable at room temperature for short periods.
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| References | |
| Additional Infomation |
m-PEG5-Ms is a PEG-based PROTAC linker. Synonyms include 2,5,8,11-tetraoxatridecan-13-yl methanesulfonate and m-PEG5-MS. It is a monodisperse compound with a polydispersity index of 1.0. The compound is used in the synthesis of ADCs and PROTACs. No clinical trials exist.
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| Molecular Formula |
C10H24O8S
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|---|---|
| Molecular Weight |
304.357763290405
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| Exact Mass |
286.108
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| CAS # |
130955-37-2
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| PubChem CID |
14763679
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| Appearance |
Colorless to light yellow liquid
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| LogP |
-0.9
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
13
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| Heavy Atom Count |
18
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| Complexity |
260
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
GXMYCEJMFZMVSC-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C10H22O7S/c1-13-3-4-14-5-6-15-7-8-16-9-10-17-18(2,11)12/h3-10H2,1-2H3
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| Chemical Name |
2-[2-[2-(2-methoxyethoxy)ethoxy]ethoxy]ethyl methanesulfonate
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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 | 3.2856 mL | 16.4279 mL | 32.8558 mL | |
| 5 mM | 0.6571 mL | 3.2856 mL | 6.5712 mL | |
| 10 mM | 0.3286 mL | 1.6428 mL | 3.2856 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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