145325-57-1

PBD dimer-2 (compound 2c) is a C8-linked pyrrolobenzodiazepine dimer. PBD dimer-2 can span an extra base pair and cross-link the 5′-Pu-GA(T/A)TC-Py sequence. PBD dimer-2 can be used as a payload for antibody–agent conjugates (ADCs), and it can be used for the research of cancer[1][2].

[1] Smellie M, et al. Sequence-selective recognition of duplex DNA through covalent interstrand cross-linking: kinetic and molecular modeling studies with pyrrolobenzodiazepine dimers. Biochemistry. 2003 Jul 15;42(27):8232-9. DOI:10.1021/bi034313t
[2] Staben LR, et al. Systematic Variation of Pyrrolobenzodiazepine (PBD)-Dimer Payload Physicochemical Properties Impacts Efficacy and Tolerability of the Corresponding Antibody-Drug Conjugates. J Med Chem. 2020 Sep 10;63(17):9603-9622. DOI:10.1021/acs.jmedchem.0c00691
[3] Howard PW, et al. Pyrrolobenzodiazepines as key intermediates in the synthesis of dimeric cytotoxic pyrrolobenzodiazepines. WO2005085259