For research use only. Not for therapeutic Use.
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 has multilog differential in vitro cytotoxicity against a panel of human tumour cell lines with a mean GI50 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[1].
SG2057 (5-60 μg/kg; i.v) exhibits dose-dependent antitumor activity in human tumor xenograft models[1].
| Catalog Number | I008856 |
| CAS Number | 260417-62-7 |
| Synonyms | (6aS)-3-[5-[[(6aS)-2-methoxy-8-methylidene-11-oxo-7,9-dihydro-6aH-pyrrolo[2,1-c][1,4]benzodiazepin-3-yl]oxy]pentoxy]-2-methoxy-8-methylidene-7,9-dihydro-6aH-pyrrolo[2,1-c][1,4]benzodiazepin-11-one |
| Molecular Formula | C33H36N4O6 |
| Purity | ≥95% |
| InChI | InChI=1S/C33H36N4O6/c1-20-10-22-16-34-26-14-30(28(40-3)12-24(26)32(38)36(22)18-20)42-8-6-5-7-9-43-31-15-27-25(13-29(31)41-4)33(39)37-19-21(2)11-23(37)17-35-27/h12-17,22-23H,1-2,5-11,18-19H2,3-4H3/t22-,23-/m0/s1 |
| InChIKey | KYNCKSRRIFFPJS-GOTSBHOMSA-N |
| SMILES | COC1=C(C=C2C(=C1)C(=O)N3CC(=C)CC3C=N2)OCCCCCOC4=C(C=C5C(=C4)N=CC6CC(=C)CN6C5=O)OC |
| 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. |
