| Size | Price | Stock | Qty |
|---|---|---|---|
| 50mg |
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| 100mg |
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| 250mg |
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| 500mg |
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| Other Sizes |
| Targets |
m-PEG8-NHS ester targets primary amine groups (-NH₂) on proteins, peptides, and other biomolecules. The NHS ester reacts with amines to form stable amide bonds. In ADCs, it connects the antibody to the cytotoxic payload. The non-cleavable nature ensures stable payload attachment.
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|---|---|
| ln Vitro |
An ADC cytotoxin is connected to an antibody by use of an ADC linker to form an ADC.
As a chemical linker, m-PEG8-NHS ester has no intrinsic pharmacological activity. Its utility is defined by its amine-reactive NHS ester group. The PEG8 spacer provides excellent water solubility and flexibility. The monodisperse PEG structure allows precise control over conjugation. |
| ln Vivo |
No direct in vivo activity is attributed to m-PEG8-NHS ester. It functions as a linker in ADCs. The NHS ester group reacts with amines on antibodies to form stable amide linkages. The PEG8 spacer improves solubility and reduces immunogenicity of the final conjugate.
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| Enzyme Assay |
For non-cell-based assays, m-PEG8-NHS ester is characterized by NMR and HPLC. The NHS ester reactivity can be assessed by reacting with a model amine and monitoring by HPLC or LC-MS. Purity is confirmed by elemental analysis (nitrogen content 2.50-3.00%).
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| Cell Assay |
Cell-based assays are not performed on m-PEG8-NHS ester alone. It is used to synthesize ADCs, which are then evaluated in cell culture. Standard protocols involve treating cancer cell lines with the ADC at 0.001-10 µM for 24-72 hours. Cytotoxicity is measured by MTT or CellTiter-Glo assays.
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| Animal Protocol |
In vivo studies with m-PEG8-NHS ester are conducted using the final ADC construct. Typical protocols involve administering the ADC to tumor-bearing mouse models via intravenous injection at 1-10 mg/kg. The PEG8 spacer contributes to prolonged circulation and enhanced efficacy.
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| ADME/Pharmacokinetics |
As a linker, m-PEG8-NHS ester does not have independent PK properties. The PEG8 spacer improves aqueous solubility and reduces clearance. The compound has a molecular weight of 509.55. Storage frozen below 0°C under inert gas is recommended (moisture sensitive).
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| Toxicity/Toxicokinetics |
Toxicology data specific to m-PEG8-NHS ester are limited. The NHS ester is reactive and may hydrolyze; standard safety precautions apply. The PEG8 moiety is biocompatible.
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| References | |
| Additional Infomation |
m-PEG8-NHS ester is a non-cleavable 8-unit PEG ADC linker. It is used in the synthesis of antibody-drug conjugates (ADCs). The NHS ester labels primary amines of proteins. No clinical trials exist.
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| Molecular Formula |
C22H39NO12
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|---|---|
| Molecular Weight |
509.5446
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| Exact Mass |
509.247
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| CAS # |
756525-90-3
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| PubChem CID |
51340981
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| Appearance |
Colorless to light yellow liquid
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| LogP |
-2
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
12
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| Rotatable Bond Count |
26
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| Heavy Atom Count |
35
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| Complexity |
547
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O(C(C([H])([H])C([H])([H])OC([H])([H])C([H])([H])OC([H])([H])C([H])([H])OC([H])([H])C([H])([H])OC([H])([H])C([H])([H])OC([H])([H])C([H])([H])OC([H])([H])C([H])([H])OC([H])([H])C([H])([H])OC([H])([H])[H])=O)N1C(C([H])([H])C([H])([H])C1=O)=O
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| InChi Key |
IBZNTYBFTKFSMU-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C22H39NO12/c1-27-6-7-29-10-11-31-14-15-33-18-19-34-17-16-32-13-12-30-9-8-28-5-4-22(26)35-23-20(24)2-3-21(23)25/h2-19H2,1H3
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| Chemical Name |
(2,5-dioxopyrrolidin-1-yl) 3-[2-[2-[2-[2-[2-[2-(2-methoxyethoxy)ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]propanoate
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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 | 1.9626 mL | 9.8128 mL | 19.6255 mL | |
| 5 mM | 0.3925 mL | 1.9626 mL | 3.9251 mL | |
| 10 mM | 0.1963 mL | 0.9813 mL | 1.9626 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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