260417-62-7

260417-62-7 structure

Name: SG2057
Chemical 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)
CAS Number: 260417-62-7
Molecular Formula: C₃₃H₃₆N₄O₆
Molecular Weight: 584.662
Catalog: Signaling Pathways Antibody-drug Conjugate ADC Cytotoxin
Create Date: 2018-06-30 19:07:49
Modify Date: 2024-01-11 21:29:57
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].

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)
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)-

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.