<Suppliers Price>

SG2057

Names

[ CAS No. ]:
260417-62-7

[ Name ]:
SG2057

[Synonym ]:
(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)-

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]:

Research Areas >> Cancer
Signaling Pathways >> Antibody-drug Conjugate >> ADC Cytotoxin
Signaling Pathways >> Cell Cycle/DNA Damage >> DNA Alkylator/Crosslinker

[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

Related Compounds