| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| Other Sizes |
| Targets |
Not applicable. DBCO-PEG2-DBCO is a chemical linker for bioconjugation, not a drug. It has no biological target. The DBCO groups are designed for copper-free click chemistry, specifically for strain-promoted alkyne-azide cycloaddition (SPAAC) reactions. These DBCO groups react rapidly and selectively with azide-functionalized molecules (e.g., payloads, antibodies, or fluorescent probes) without the need for toxic copper catalysts. The PEG2 spacer (two ethylene glycol units) increases water solubility and reduces steric hindrance.
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|---|---|
| ln Vitro |
As a bioconjugation linker, DBCO-PEG2-DBCO has no direct biological activity. Its value is in enabling the efficient and specific conjugation of antibody-drug conjugates via copper-free click chemistry. The high strain energy of the DBCO groups promotes rapid reaction rates and high yields, while the PEG spacer improves water solubility, making it ideal for diverse research applications.
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| ln Vivo |
No specific in vivo data is reported. As a linker, it is not studied directly in vivo. However, ADCs synthesized using DBCO-PEG2-DBCO demonstrate improved stability and efficacy in tumor xenograft models. The copper-free click chemistry conjugation method avoids the potential toxicity of copper catalysts, making it suitable for in vivo applications.
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| Enzyme Assay |
Not applicable. DBCO-PEG2-DBCO is a chemical reagent. A typical conjugation protocol involves dissolving the linker (1-5 mM) in anhydrous DMSO or DMF. To conjugate an azide-functionalized payload, the linker and the azide are mixed in a 1:1 to 1:3 molar ratio in PBS (pH 7.2-7.4) containing 5-10% organic co-solvent. The reaction is incubated at room temperature for 2-6 hours, and conversion is monitored by LC-MS or TLC. The product is purified by preparative HPLC or size exclusion chromatography.
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| Cell Assay |
Not applicable. The compound is not used in cell-based assays. However, the fully synthesized ADC or labeled antibody can be tested in vitro. Target-positive cancer cells are seeded in 96-well plates and treated with the ADC or labeled antibody. For ADCs, cell viability is measured by CellTiter-Glo. For imaging applications, the DBCO-PEG2-DBCO linker can be used to conjugate azide-labeled antibodies to fluorescent dyes, and cell binding is assessed by flow cytometry or fluorescence microscopy.
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| Animal Protocol |
No specific in vivo animal study protocols are documented for DBCO-PEG2-DBCO itself. For an ADC synthesized with this linker, a typical protocol involves intravenous administration of the ADC (1-10 mg/kg) in immunodeficient mice bearing tumor xenografts of target-positive cancer cells. Efficacy is assessed by tumor volume measurement and survival analysis. PK studies measure ADC concentration in plasma and tissues by ELISA or LC-MS.
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| ADME/Pharmacokinetics |
Not applicable for the linker. The PEG2 spacer in DBCO-PEG2-DBCO imparts favorable properties to the final conjugate. The hydrophilic PEG chain reduces non-specific protein binding, improves solubility, and can increase the circulation half-life of the conjugated product. The small PEG2 size minimizes steric interference with the antibody's antigen binding.
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| Toxicity/Toxicokinetics |
No toxicity data is reported. DBCO-PEG2-DBCO is a chemical reagent. The DBCO groups are reactive and may form adducts with biological nucleophiles; therefore, it should be handled with care. Standard chemical safety precautions apply. The compound is for research use only, not for human therapeutic use.
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| References |
[1]. Jiang X, et al. Recent applications of click chemistry in drug discovery. Expert Opin Drug Discov. 2019 Aug;14(8):779-789.
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| Additional Infomation |
DBCO-PEG2-DBCO has the molecular formula C44H42N4O6 and a molecular weight of 722.83 g/mol. The DBCO (dibenzocyclooctyne) group enables strain-promoted alkyne-azide cycloaddition (SPAAC) copper-free click chemistry, which is a bioorthogonal reaction that does not interfere with biological systems. The linker is soluble in DMSO, DMF, and other organic solvents. It is stored as a powder at -20degC and is stable for up to 3 years.
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| Molecular Formula |
C44H42N4O6
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|---|---|
| Exact Mass |
722.31
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| CAS # |
2639395-48-3
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| PubChem CID |
155887591
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| Appearance |
White to yellow solid powder
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
15
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| Heavy Atom Count |
54
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| Complexity |
1320
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1C2=CC=CC=C2C#CC3=CC=CC=C3N1C(=O)CCC(=O)NCCOCCOCCNC(=O)CCC(=O)N4CC5=CC=CC=C5C#CC6=CC=CC=C64
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| InChi Key |
GPRBYNSGOSAHPU-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C44H42N4O6/c49-41(21-23-43(51)47-31-37-13-3-1-9-33(37)17-19-35-11-5-7-15-39(35)47)45-25-27-53-29-30-54-28-26-46-42(50)22-24-44(52)48-32-38-14-4-2-10-34(38)18-20-36-12-6-8-16-40(36)48/h1-16H,21-32H2,(H,45,49)(H,46,50)
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| Chemical Name |
4-(2-azatricyclo[10.4.0.04,9]hexadeca-1(16),4,6,8,12,14-hexaen-10-yn-2-yl)-N-[2-[2-[2-[[4-(2-azatricyclo[10.4.0.04,9]hexadeca-1(16),4,6,8,12,14-hexaen-10-yn-2-yl)-4-oxobutanoyl]amino]ethoxy]ethoxy]ethyl]-4-oxobutanamide
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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 (~138.4 mM; with ultrasonication and warming by heating to 60°C)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (3.46 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 (3.46 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), Suspended solution; with ultrasonication. 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. (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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