Azide-Hexanoyl-Val-Cit-PAB(m-PEG8)-Exatecan

SOLU-KNEX® cleavable linker features a Val-Cit dipeptide. m-PEG8 is attached to the commonly used self-immolative para-aminobenzyl (PAB) moiety to increase aqueous solubility. The payload is Exatecan, a highly potent topoisomerase I inhibitor derived from camptothecin, which induces DNA damage by stabilizing the topoisomerase I–DNA complex, resulting in cell-cycle arrest and apoptosis.

Derived from established ADC linker architectures, SOLU-KNEX® ADC linkers integrate solubilizing moieties—such as PEG, amine-containing groups, or polysarcosine (PSAR), to enhance aqueous solubility. Solubility and physicochemical properties can be finely tuned through selection and combination of these groups, making the linkers highly adaptable for diverse ADC and related applications. SOLU-KNEX® is a registered trademark of Tenova Pharmaceuticals, Inc. For research use only.

References

(1) Yamazoe, S., Poudel, Y., Sega, E., Mukhopadhyay, A., Ramakrishnan, R., Ukairo, O., Liu, S., Akter, R., Sadanala, K., Que, K., Cheng, Q., Kotapati, S., Deshpande, M., Cox, M., Chourey, S., Gupta, A., Kempson, J., Pabbisetty, K., Kaspady, M., … Chekler, E. P. (2025). Discovery and Characterization of a First-in-Class LIV1-TLR7/8 Immunomodulatory Conjugate with Robust Myeloid Activation and Antitumor Activity. Journal of Medicinal Chemistry. https://doi.org/10.1021/acs.jmedchem.5c00356

Documents 

Datasheet          MSDS

Citations

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