SG2057 (DRG16) is a PBD dimer containing a pentyldioxy linkage which binds sequence selectively in the minor groove of DNA forming DNA interstrand and intrastrand cross-linked adducts. SG2057 is a highly active antitumor agent
In Vitro
SG2057 has multilog differential in vitro cytotoxicity against a panel of human tumour cell lines with a mean GI 50 of 212 pM. SG2057 is highly efficient at producing DNA interstrand cross-links in cells which form rapidly and persist over a 48 h period. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
SG2057 (5-60 μg/kg; i.v) exhibits dose-dependent antitumor activity in human tumor xenograft models . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Female NCr-nude mice injected with SKOV-3 cells Dosage: 5 μg/kg, 10 μg/kg, 20 μg/kg, 30 μg/kg, 40 μg/kg, 50 μg/kg, 60 μg/kg Administration: i.v.; daily, once a week, or once every four days Result: Showed significant antitumor activity.
