Synthesis and in vitro evaluation of SG3227, a pyrrolobenzodiazepine dimer antibody-drug conjugate payload based on Sibiromycin (cas 12684-33-2)

Add time:08/24/2019    Source:sciencedirect.com

A novel pyrrolobenzodiazepine dimer payload, SG3227, was rationally designed based on the naturally occurring antitumour compound sibiromycin. SG3227 was synthesized from a dimeric core in an efficient fashion. An unexpected room temperature Diels-Alder reaction occurred during the final step of the synthesis and was circumvented by use of an iodoacetamide conjugation moiety in place of a maleimide. The payload was successfully conjugated to trastuzumab and the resulting ADC exhibited potent activity against a HER2-expressing human cancer cell line in vitro.

We also recommend Trading Suppliers and Manufacturers of Sibiromycin (cas 12684-33-2). Pls Click Website Link as below: cas 12684-33-2 suppliers

Prev:Determination of Sibiromycin (cas 12684-33-2) and its natural derivatives using new analytical and structural approaches
Next:Identification of the dioxygenase-generated intermediate formed during biosynthesis of the dihydropyrrole moiety common to anthramycin and Sibiromycin (cas 12684-33-2))