MAL-dPEG®₄-Glu(TFP ester)-NH-dPEG®₄-Glu(TFP ester)-NH-m-dPEG®₂₄ (QBD-11626)

Description

MAL-dPEG®4-Glu(TFP)-NH-dPEG®4-Glu(TFP)-m-dPEG®24, product number QBD-11626, is one of Vector Laboratories’ unique, patented class of modular, designable payload delivery reagents called Sidewinder™. Sidewinder™ products are built on a discrete PEG (dPEG®) backbone for use in antibody-drug conjugates (ADCs) and related constructs. The payload (cytotoxin, dye, small molecule) loads onto the chain’s sidearm. The distal end’s methoxy-terminated dPEG®24 spacer protects payloads and modifies performance.

The maleimide group of MAL-dPEG®4-Glu(TFP)-NH-dPEG®4-Glu(TFP)-m-dPEG®24, product number QBD-11626, reacts with free thiols to form stable thioether bonds. It is the attachment point for the Sidewinder™ to the biomolecule (e.g., mAb, Fab, Fab’, targeting peptide, and so forth). The backbone contains two carboxylic acid sidearms functionalized as 2,3,5,6-tetrafluorophenyl (TFP) esters. The TFP esters react with free amines in an optimal pH range of 7.5 – 8.0 and are more reactive toward amines than NHS esters within the optimal pH range.

Sidewinder™ products are designed to facilitate the creation of stable, high-DAR ADCs. Published research has shown that putting a hydrophobic payload close to the antibody surface and protecting it with a SuperHydrophilic™ dPEG® construct is better by many measures of efficacy than putting the payload at the distal end of the linker. This molecule can also modify and optimize BD, cell trafficking and internalization, serum half-life, and immunogenicity.

The dPEG® linkers and spacers in the Sidewinder™ construct are uniform, single molecular-weight PEGs with discrete chain lengths. In contrast, traditional, non-uniform polymer PEG linkers and spacers have a dispersed range of PEG chain lengths, each with a unique molecular weight. Unlike dispersed polymer PEGs, dPEG® products are high-purity compounds with reproducible purity profiles.

Sidewinder™ molecules are also fully designable. MAL-dPEG®4-Glu(TFP)-NH-dPEG®4-Glu(TFP)-m-dPEG®24 can be modified to change the spacer lengths, add more sidearm attachment points, add different sidearm attachment points to carry payloads with other reactivities, change the maleimide attachment group to another reactive group, and many more customizations. Please inquire about your specific needs.

Specifications

Documents

References

Greg T. Hermanson, Bioconjugate Techniques 3rd Edition, Elsevier, Waltham, MA 02451, 2013, ISBN 978-0-12-382239-0; See Chapter 18, Discrete PEG Reagents, pp. 787-821, for a full overview of the dPEG® products.