260546-06-3

Basic information

• Product Name: (11aS)-8-benzyloxy-7-methoxy-2-methylidene-1,2,3,11a-tetrahydro-5H-pyrrolo[2,1-c][1,4]benzodiazepin-5-one
• Synonyms: (11aS)-8-benzyloxy-7-methoxy-2-methylidene-1,2,3,11a-tetrahydro-5H-pyrrolo[2,1-c][1,4]benzodiazepin-5-one
• CAS NO: 260546-06-3
• Molecular Weight: 348.401
• Mol File: 260546-06-3.mol
• Article Data: 9

Chemical Properties

• CAS DataBase Reference: (11aS)-8-benzyloxy-7-methoxy-2-methylidene-1,2,3,11a-tetrahydro-5H-pyrrolo[2,1-c][1,4]benzodiazepin-5-one(CAS DataBase Reference)
• NIST Chemistry Reference: (11aS)-8-benzyloxy-7-methoxy-2-methylidene-1,2,3,11a-tetrahydro-5H-pyrrolo[2,1-c][1,4]benzodiazepin-5-one(260546-06-3)
• EPA Substance Registry System: (11aS)-8-benzyloxy-7-methoxy-2-methylidene-1,2,3,11a-tetrahydro-5H-pyrrolo[2,1-c][1,4]benzodiazepin-5-one(260546-06-3)

Safety Data

• Hazardous Substances Data: 260546-06-3(Hazardous Substances Data)

Upstream product

• 91203-74-6 4-benzyloxy-3-methoxybenzoic acid benzyl ester 
• 926279-19-8 (S)-(4-methylenepyrrolidin-2-yl)methanol hydrochloride salt 
• 260418-16-4 (2S)-N-(4-benzyloxy-5-methoxy-2-nitrobenzoyl)-2-(hydroxymethyl)-4-methylidenepyrrolidine 
• 232931-59-8 (2S)-2-(tert-butyldimethylsilyloxymethyl)-4-methylidenepyrrolidine 
• 945490-08-4 (S)-1-(4-(benzyloxy)-5-methoxy-2-nitrobenzoyl)-4-methylenepyrrolidine-2-carbaldehyde 
• 64154-78-5 4-benzyloxy-5-methoxy-2-nitrobenzoyl chloride 
• 945490-07-3 1-(4-benzyloxy-5-methoxy-2-nitrobenzoyl)-(2S)-4-methylenepyrrolidine-2-carboxylic acid methyl ester 
• 84348-41-4 (S)-methyl 4-methylenepyrrolidine-2-carboxylate hydrochloride 
• 84348-39-0 (S)-1-tert-butyl 2-methyl 4-methylenepyrrolidine-1,2-dicarboxylate 
• 60547-92-4 4-(benzyloxy)-5-methoxy-2-nitrobenzoic acid 
• 100-39-0 benzyl bromide 
• 1486-53-9 4-(benzyloxy)-3-methoxybenzoic acid 
• 121-34-6 3-methoxy-4-hydroxybenzoic acid 
• 301838-53-9 {5-benzyloxy-2-[2-(tert-butyl-dimethyl-silanyloxymethyl)-4-methylene-pyrrolidine-1-carbonyl]-4-methoxy-phenyl}-carbamic acid allyl ester 

Relevant articles and documents

VISUAL DETECTION OF PBD INDUCED DNA CROSSLINKS

The present invention relates to the field of oncology, laboratory tools and methods, and especially anti-tumor DNA crosslinking agents. Most patients with advanced solid tumors develop resistance to chemotherapy due to the ability of cancer cells to repair or tolerate sustained DNA damages. The inventors showed that the compounds according to the present invention allow the detection and visualization of alkylated DNA damages induced by PBDs without altering their DNA crosslinking ability. This enables the study of the effect and properties of PBDs. In particular, the present invention relates new derivates of PBD molecules and their synthesis. The present invention also relates to a method for visualizing DNA crosslinking; to a method for assessing the resistance of a tumor to a crosslinking agent and to a method for identifying a molecule or treatment for improving the efficiency of a crosslinking agent.

SPECIFIC CONJUGATION LINKERS, SPECIFIC IMMUNOCONJUGATES THEREOF, METHODS OF MAKING AND USES SUCH CONJUGATES THEREOF

The present invention relates to novel linkers containing a 2,3-disubstituted succinic group, or 2-monosubstituted, or 2,3-disubstituted fumaric or maleic (trans (E)- or cis (Z)- butenedioic), or acetylenedicarboxyl group for conjugation of a cytotoxic agent, and/or one or more different functional molecules per linker to a cell-binding molecule, through bridge linking pairs of thiols on the cell-binding molecule specifically. The invention also relates to methods of making such linkers, and of using such linkers in making homogeneous conjugates, as well as of application of the conjugates in treatment of cancers, infections and autoimmune disorders.

NOVEL CYTOTOXIC AGENTS FOR CONJUGATION OF DRUGS TO CELL BINDING MOLECULE

Provided are cytotoxic agents, pyrrolo[2,1-c][1,4]benzodiazepine (PBD) derivatives, their conjugates with a cell-binding agent, the preparation and the therapeutic uses in the targeted treatment of cancers, autoimmune disorders, and infectious diseases.