MAL-dPEG®4-Lys(TFA)-NH-m-dPEG®24, product number QBD-11576, 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.
Sidewinder™ products are designed to facilitate the creation of stable, high-DAR ADCs. Published research has shown that putting a hydrophobic payload (e.g., a cytotoxin) 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 be used to 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. This differs from traditional, non-uniform polymer PEG linkers and spacers, which have a dispersed range of PEG chain lengths, each with a unique molecular weight. In contrast to dispersed polymer PEGs, dPEG® products are high-purity compounds with reproducible purity profiles.
The maleimide reactive group of MAL-dPEG®4-Lys(TFA)-NH-m-dPEG®24, product number QBD-11576 reacts with free thiols on the biomolecule through the thiol-maleimide reaction (a Michael addition reaction). The sidearm’s amine exists as the TFA salt and can be reacted with carboxylic acids and their active esters to form stable amide bonds. Any amine-reactive payload can be loaded onto the sidearm once the amine is deprotected.
Sidewinder™ molecules are also fully designable. MAL-dPEG®4-Lys(TFA)-NH-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 different reactivities, change the maleimide attachment group to a different reactive group, and many more customizations. Please inquire about your specific needs.
| Unit Size | 50 mg, 250 mg |
|---|---|
| Molecular Weight | 1728.94; single compound |
| Chemical formula | C₇₅H₁₄₀F₃N₅O₃₅ |
| CAS | N/A |
| Purity | > 95% |
| Spacers | dPEG® Spacer is 98 atoms and 108.9 Å |
| Shipping | Ambient |
| Typical solubility properties (for additional information contact Customer Support) | Methylene Chloride, Acetonitrile, Methanol, DMSO or DMF. |
| Storage and handling | -20°C; Always let come to room temperature before opening; be careful to limit exposure to moisture and restore under an inert atmosphere; stock solutions can be prepared with dry solvent and kept for several days (freeze when not in use). dPEG® pegylation compounds are generally hygroscopic and should be treated as such. This will be less noticeable with liquids, but the solids will become tacky and difficult to manipulate, if care is not taken to minimize air exposure. |
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.
Applicable patents and legal notices are available at legal notices.
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