| Size | Price | Stock | Qty |
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| 50mg |
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| 100mg |
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| Other Sizes |
| Targets |
Disulfide Cleavable Linker Cleavable Linker
As a chemical linker for ADC construction, PEG4-SPDP does not have a defined biological target. Its role is to serve as a cleavable connector between an antibody and a cytotoxic payload in antibody-drug conjugates. The pyridyl disulfide group provides a cleavable disulfide linkage that enables intracellular drug release in the reducing environment of target cells. The PEG4 spacer enhances solubility and biocompatibility. |
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| ln Vitro |
In cell-free biochemical systems, this linker is used to covalently attach small molecule drugs to antibodies, enabling the formation of cleavable antibody-drug conjugates. The NHS ester reacts with primary amines on the antibody, while the pyridyl disulfide reacts with thiol groups on the drug payload. The PEG4 spacer improves the solubility and stability of the resulting conjugate. The cleavable disulfide bond enables controlled drug release in the intracellular environment.
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| ln Vivo |
This compound does not exhibit direct cellular activity as it is a chemical linker rather than a bioactive molecule. Antibody-drug conjugates constructed using this linker can be delivered to target cells where the antibody binds to cell surface antigens, followed by internalization and intracellular release of the cytotoxic payload via cleavage of the disulfide bond. The cleavable nature of the linker enables selective drug release within target cells.
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| Enzyme Assay |
The cell-free assay for this linker involves conjugation reactions between the NHS ester and primary amines on proteins or antibodies, followed by reaction of the pyridyl disulfide with thiol-containing payloads. The reaction is typically performed in aqueous buffer at pH 7.0-8.5. The efficiency of conjugation is assessed by mass spectrometry, SDS-PAGE, or HPLC analysis. The cleavability of the disulfide bond can be confirmed by treatment with reducing agents such as DTT or TCEP.
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| Cell Assay |
No cell-based experimental protocols are directly applicable to this linker as it is a chemical synthesis reagent. Antibody-drug conjugates synthesized using this linker can be evaluated in cell culture experiments. Typical protocols include treating cancer cell lines with the ADC at concentrations ranging from 0.001 to 10 μg/mL. Cells are incubated for 24-96 hours, and cell viability is assessed using MTT or CCK-8 assays. The specificity of target cell killing is evaluated by comparing antigen-positive and antigen-negative cell lines.
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| Animal Protocol |
This linker is not administered to animals as it is a chemical intermediate for ADC synthesis. Antibody-drug conjugates incorporating this linker may be evaluated in animal models for pharmacokinetics and efficacy. Typical studies involve administration of the ADC to tumor-bearing mice via intravenous routes at doses ranging from 0.1-10 mg/kg. Tumor volumes are measured, and tissues are collected for analysis of ADC distribution, payload release, and therapeutic efficacy.
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| ADME/Pharmacokinetics |
As a chemical reagent, this compound does not have established pharmacokinetic properties. The pharmacokinetics of ADCs incorporating this linker depend on the antibody, payload, and overall conjugate properties. The cleavable disulfide bond influences payload release kinetics. The PEG4 spacer may affect the circulation time and biodistribution of the ADC. The compound itself is not intended for therapeutic use and is not administered systemically.
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| Toxicity/Toxicokinetics |
The compound is not intended for therapeutic use and lacks established toxicity profiles. Standard laboratory safety precautions should be observed when handling this chemical reagent. The compound is typically stored as powder at -20°C for 3 years or at 4°C for 2 years. It is soluble in DMSO. The compound is for research use only and is not for human therapeutic applications.
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| References |
[1]. Zhao RY, et al. Synthesis and evaluation of hydrophilic linkers for antibody-maytansinoid conjugates. J Med Chem. 2011 May 26;54(10):3606-23.
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| Additional Infomation |
PEG4-SPDP is a research-grade chemical supplied for ADC linker synthesis applications. It is not an approved pharmaceutical and has no clinical trial history. The compound is a cleavable ADC linker that may be utilized to prepare antibody-conjugated active molecules. References include a study on hydrophilic linkers for antibody-maytansinoid conjugates. This product is intended for research use only and is not for human therapeutic applications.
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| Molecular Formula |
C20H28N2O8S2
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|---|---|
| Exact Mass |
488.128
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| CAS # |
1305053-43-3
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| PubChem CID |
53248045
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| Appearance |
Colorless to light yellow viscous liquid
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| LogP |
0.1
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
11
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| Rotatable Bond Count |
19
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| Heavy Atom Count |
32
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| Complexity |
554
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1CC(=O)N(C1=O)OC(=O)CCOCCOCCOCCOCCSSC2=CC=CC=N2
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| InChi Key |
AZXJOPLHLVNPKQ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C20H28N2O8S2/c23-18-4-5-19(24)22(18)30-20(25)6-8-26-9-10-27-11-12-28-13-14-29-15-16-31-32-17-3-1-2-7-21-17/h1-3,7H,4-6,8-16H2
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| Chemical Name |
(2,5-dioxopyrrolidin-1-yl) 3-[2-[2-[2-[2-(pyridin-2-yldisulfanyl)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) |
DMSO: ~100 mg/mL (~204.7 mM; with ultrasonication)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.12 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), Clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (25.0 mg/mL) to 400 μL of PEG300 and mix well; then add 50 μL of Tween-80 and mix well; finally add 450 μL of physiological saline and adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.12 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), Clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (25.0 mg/mL) to 900 μL of 20% SBE-β-CD saline and mix well. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 3: ≥ 2.5 mg/mL (5.12 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), Clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (25.0 mg/mL) to 900 μL of corn oil and mix well. (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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