| Size | Price | Stock | Qty |
|---|---|---|---|
| 50mg |
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| 100mg |
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| 500mg |
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| Other Sizes |
| Targets |
The two NHS ester groups react with primary amines (-NH2) on proteins, antibodies, or other amine-containing molecules to form stable amide bonds. This enables crosslinking of two amine-containing molecules. The non-degradable nature offers greater stability and longer circulation time in the body.
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|---|---|
| ln Vitro |
In vitro activity is primarily related to its function as an ADC linker or protein crosslinker. Bis-PEG1-NHS ester enables the conjugation of antibodies to cytotoxic payloads for ADC development. The short PEG spacer provides minimal flexibility between conjugated molecules. Crosslinking efficiency is assessed by SDS-PAGE or mass spectrometry.
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| ln Vivo |
In vivo activity of Bis-PEG1-NHS ester is primarily inferred from its use in ADC development. ADCs synthesized using this linker deliver cytotoxic payloads specifically to target cells. The non-degradable linker provides stability in circulation. No direct in vivo activity data are specifically available for this linker alone.
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| Enzyme Assay |
In vitro assays for Bis-PEG1-NHS ester typically involve evaluating crosslinking efficiency by reacting the NHS esters with primary amine-containing molecules at pH 7-9. Reaction efficiency is assessed by SDS-PAGE, mass spectrometry, or HPLC. Purity is assessed by HPLC. Solubility is evaluated in organic solvents (DMF, DMSO) and aqueous buffers.
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| Cell Assay |
Cell-based assays for Bis-PEG1-NHS ester are conducted in the context of ADC activity. Target cells expressing the antigen of interest are treated with ADCs synthesized using this linker. Cytotoxicity is measured by MTT or CellTiter-Glo assays. Antigen-specific cell killing is compared to non-targeting controls. Internalization and trafficking of ADCs are assessed by immunofluorescence microscopy.
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| Animal Protocol |
In vivo animal studies for Bis-PEG1-NHS ester are conducted in the context of ADC efficacy. Tumor-bearing mice are treated with ADCs synthesized using this linker, and tumor growth inhibition is monitored. Pharmacokinetic parameters are evaluated by measuring ADC levels in blood and tissues. Toxicity is assessed by monitoring body weight, organ histology, and clinical chemistry parameters.
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| ADME/Pharmacokinetics |
As a PEG-based linker (molecular weight ~300-350), Bis-PEG1-NHS ester has limited aqueous solubility due to the short PEG spacer. The NHS esters are hydrolytically unstable and should be used fresh. No specific PK data are available for this linker alone; its PK profile is determined by the conjugated molecule.
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| Toxicity/Toxicokinetics |
No detailed toxicology data are specifically available for Bis-PEG1-NHS ester. The compound is for research use only and not intended for therapeutic use. Standard laboratory safety precautions should be followed. The NHS ester may cause irritation upon contact. Comprehensive toxicological evaluation has not been reported.
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| Additional Infomation |
Bis-PEG1-NHS ester (CAS#: 65869-64-9) is a homobifunctional amine-reactive crosslinker and non-degradable ADC linker containing one PEG unit. It contains two NHS ester groups for protein crosslinking. It is used in ADC development and bioconjugation research. It is for research use only and not an approved therapeutic agent.
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| Molecular Formula |
C14H16N2O9
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|---|---|
| Molecular Weight |
356.284844398499
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| Exact Mass |
356.085
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| CAS # |
65869-64-9
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| PubChem CID |
13055591
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| Appearance |
Typically exists as solid at room temperature
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| Density |
1.5±0.1 g/cm3
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| Boiling Point |
511.4±60.0 °C at 760 mmHg
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| Flash Point |
263.1±32.9 °C
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| Vapour Pressure |
0.0±1.3 mmHg at 25°C
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| Index of Refraction |
1.564
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| LogP |
-3.51
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
9
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| Rotatable Bond Count |
10
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| Heavy Atom Count |
25
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| Complexity |
531
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O=C(ON1C(CCC1=O)=O)CCOCCC(ON2C(CCC2=O)=O)=O
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| InChi Key |
OWCYSDGIJAVHFQ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C14H16N2O9/c17-9-1-2-10(18)15(9)24-13(21)5-7-23-8-6-14(22)25-16-11(19)3-4-12(16)20/h1-8H2
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| Chemical Name |
(2,5-dioxopyrrolidin-1-yl) 3-[3-(2,5-dioxopyrrolidin-1-yl)oxy-3-oxopropoxy]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 | 2.8068 mL | 14.0339 mL | 28.0678 mL | |
| 5 mM | 0.5614 mL | 2.8068 mL | 5.6136 mL | |
| 10 mM | 0.2807 mL | 1.4034 mL | 2.8068 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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