| Identification | Back Directory | [Name]
SG2057 | [CAS]
260417-62-7 | [Synonyms]
SG2057
5H-Pyrrolo[2,1-c][1,4]benzodiazepin-5-one, 8,8'-[1,5-pentanediylbis(oxy)]bis[1,2,3,11a-tetrahydro-7-methoxy-2-methylene-, (11aS,11'aS)- | [Molecular Formula]
C33H36N4O6 | [MOL File]
260417-62-7.mol | [Molecular Weight]
584.66 |
| Hazard Information | Back Directory | [Uses]
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]. | [in vivo]
SG2057 (5-60 μg/kg; i.v) exhibits dose-dependent antitumor activity in human tumor xenograft models[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.
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| [IC 50]
Pyrrolobenzodiazepines | [References]
[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. DOI:10.1007/s10637-011-9647-z |
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