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[1].
SG2057 对一组人类肿瘤细胞系具有多重差异体外细胞毒性，平均 GI50 为 212 pM。SG2057 可高效地在细胞中产生 DNA 链间交联，这种交联快速形成并持续 48 小时[1]。
SG2057（5-60 μg/kg；静脉注射）在人肿瘤异种移植模型中表现出剂量依赖性抗肿瘤活性[1]。
| Animal Model: | Female NCr-nude mice injected with SKOV-3 cells[1] |
| 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. |
[1]. John A Hartley, et al. DNA interstrand cross-linking and in vivo antitumor activity of the extended pyrrolo[2,1-c][1,4]benzodiazepine dimer SG2057. Invest New Drugs. 2012 Jun;30(3):950-8.