SG2057

SG2057 is a synthetic **pyrrolo[2,1-c][1,4]benzodiazepine (PBD) dimer** that selectively binds to sequences in the DNA minor groove and forms **DNA interstrand crosslinks** by bis-alkylating guanine residues. It is used as a highly potent cytotoxic payload in antibody-drug conjugates (ADCs), enabling targeted delivery of DNA cross-linking agents to cancer cells. The imine groups of SG2057 are the active pharmacophores for DNA crosslinking. Chemical modifications such as monoamine or monoamide derivatives of SG2057 can convert it to mono-alkylating agents that retain DNA alkylation capability but reduce crosslinking and potency. SG2057's cytotoxicity is utilized in preclinical studies for anti-tumor efficacy in models such as HER2-positive and HER2-low cancers, and non-Hodgkin lymphoma, delivered via various ADC linkers.

Other names

SG2057SG-2057SG 2057DRG16DRG-16DRG 16