| Bioactivity | 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]. |
| Invitro | 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]。 |
| In Vivo | 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: |
| Name | SG2057 |
| CAS | 260417-62-7 |
| Formula | C33H36N4O6 |
| Molar Mass | 584.66 |
| Appearance | Solid |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | -20°C, stored under nitrogen *In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen) |
| Reference | [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. |