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DBCO-PEG4-GGFG-Dxd

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Catalog No. T84734Cas No. 2694856-51-2

DBCO-PEG4-GGFG-Dxd is an ADC linker-payload intermediate used for synthesizing antibody-drug conjugates. This product consists of the DNA topoisomerase I inhibitor Dxd (Deruxtecan) conjugated to a cleavable GGFG tetrapeptide-based linker. The terminal DBCO group functions as a click chemistry handle, enabling strain-promoted alkyne-azide cycloaddition (SPAAC) with azide-containing molecules for the efficient construction of tumor-targeted ADCs.

DBCO-PEG4-GGFG-Dxd

DBCO-PEG4-GGFG-Dxd

😃Good
Purity: 96.58%
Catalog No. T84734Cas No. 2694856-51-2
DBCO-PEG4-GGFG-Dxd is an ADC linker-payload intermediate used for synthesizing antibody-drug conjugates. This product consists of the DNA topoisomerase I inhibitor Dxd (Deruxtecan) conjugated to a cleavable GGFG tetrapeptide-based linker. The terminal DBCO group functions as a click chemistry handle, enabling strain-promoted alkyne-azide cycloaddition (SPAAC) with azide-containing molecules for the efficient construction of tumor-targeted ADCs.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
1 mg$289-In Stock
5 mg$689-In Stock
10 mg$1,180-In Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.
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Purity:96.58%
ee:100%
Appearance:Solid
Color:White
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Product Introduction

Bioactivity
Description
DBCO-PEG4-GGFG-Dxd is an ADC linker-payload intermediate used for synthesizing antibody-drug conjugates. This product consists of the DNA topoisomerase I inhibitor Dxd (Deruxtecan) conjugated to a cleavable GGFG tetrapeptide-based linker. The terminal DBCO group functions as a click chemistry handle, enabling strain-promoted alkyne-azide cycloaddition (SPAAC) with azide-containing molecules for the efficient construction of tumor-targeted ADCs.
In vitro
In biochemical and cell-based conjugation assays, DBCO-PEG4-GGFG-Dxd exhibits rapid and specific reactivity with azide-functionalized antibodies, forming stable ADCs that release the active Dxd payload upon lysosomal cathepsin-mediated cleavage of the GGFG peptide linker, resulting in potent cytotoxicity against topoisomerase I-expressing cancer cells [1].
In vivo
In pharmacological studies using tumor-bearing mouse models, the administration of ADCs synthesized using DBCO-PEG4-GGFG-Dxd leads to a significant, dose-dependent inhibition of tumor growth and prolonged survival; the GGFG linker ensures systemic stability while allowing efficient intratumoral release of Dxd, demonstrating the potential for targeted delivery and reduced off-target toxicity in preclinical cancer therapy research [1].
Chemical Properties
Molecular Weight1375.45
FormulaC72H79FN10O17
Cas No.2694856-51-2
SmilesN(C(COCNC(CNC([C@H](CC1=CC=CC=C1)NC(CNC(CNC(CCOCCOCCOCCOCCNC(CCC(=O)N2C=3C(C#CC=4C(C2)=CC=CC4)=CC=CC3)=O)=O)=O)=O)=O)=O)=O)[C@@H]5C6=C7C(C=8N(C7)C(=O)C9=C(C8)[C@](CC)(O)C(=O)OC9)=NC=%10C6=C(CC5)C(C)=C(F)C%10
Storage & Solubility Information
Storagestore at low temperature,The compound is unstable in solution. Please use soon | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
DMSO: 40 mg/mL (29.08 mM), Sonication is recommended.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM0.7270 mL3.6352 mL7.2703 mL36.3517 mL
5 mM0.1454 mL0.7270 mL1.4541 mL7.2703 mL
10 mM0.0727 mL0.3635 mL0.7270 mL3.6352 mL
20 mM0.0364 mL0.1818 mL0.3635 mL1.8176 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
TargetMol | Animal experiments For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.
Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSOTargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH2OTargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.
1 Enter information below:
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2 Enter the in vivo formulation:
% DMSO
%
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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc

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