SG2057

Modify Date: 2024-01-11 21:29:57

SG2057 Structure
SG2057 structure
Common Name SG2057
CAS Number 260417-62-7 Molecular Weight 584.662
Density 1.3±0.1 g/cm3 Boiling Point 820.0±65.0 °C at 760 mmHg
Molecular Formula C33H36N4O6 Melting Point N/A
MSDS N/A Flash Point 449.7±34.3 °C

 Use of SG2057


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].

 Names

Name (11aS,11a'S)-8,8'-[1,5-Pentanediylbis(oxy)]bis(7-methoxy-2-methylene-1,2,3,11a-tetrahydro-5H-pyrrolo[2,1-c][1,4]benzodiazepin-5-one)
Synonym More Synonyms

 SG2057 Biological Activity

Description 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].
Related Catalog
Target

Pyrrolobenzodiazepines

In Vitro 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: 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.
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.  

 Chemical & Physical Properties

Density 1.3±0.1 g/cm3
Boiling Point 820.0±65.0 °C at 760 mmHg
Molecular Formula C33H36N4O6
Molecular Weight 584.662
Flash Point 449.7±34.3 °C
Exact Mass 584.263489
LogP 2.75
Vapour Pressure 0.0±3.0 mmHg at 25°C
Index of Refraction 1.647

 Synonyms

(11aS,11a'S)-8,8'-[1,5-Pentanediylbis(oxy)]bis(7-methoxy-2-methylene-1,2,3,11a-tetrahydro-5H-pyrrolo[2,1-c][1,4]benzodiazepin-5-one)
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)-