848006-02-0

Basic information

• Product Name: 4-Quinazolinamine, N-(4,5-dichloro-2-fluorophenyl)-7-fluoro-6-nitro-
• CAS NO: 848006-02-0
• Molecular Formula: C14H6Cl2F2N4O2
• Molecular Weight: 371.13
• Mol File: 848006-02-0.mol

Chemical Properties

• CAS DataBase Reference: 4-Quinazolinamine, N-(4,5-dichloro-2-fluorophenyl)-7-fluoro-6-nitro-(CAS DataBase Reference)
• NIST Chemistry Reference: 4-Quinazolinamine, N-(4,5-dichloro-2-fluorophenyl)-7-fluoro-6-nitro-(848006-02-0)
• EPA Substance Registry System: 4-Quinazolinamine, N-(4,5-dichloro-2-fluorophenyl)-7-fluoro-6-nitro-(848006-02-0)

Safety Data

• Hazardous Substances Data: 848006-02-0(Hazardous Substances Data)

Upstream product

• 162012-69-3 7-fluoro-6-nitro-3H-quinazolin-4-one 
• 2729-36-4 4,5-dichloro-2-fluoro-phenylamine 
• 162012-70-6 4-chloro-7-fluoro-6-nitroquinazoline 

Downstream Products

• 863488-63-5 4-[(3,4-dichloro-6-fluorophenyl)amino]-7-methylpiperazine-6-nitroquinazoline 
• 929037-11-6 2-{2-[4-(4,5-dichloro-2-fluoro-phenylamino)-6-nitro-quinazoline-7-yloxy]-ethoxy}-ethanol 
• 863488-65-7 4-(3,4-dichloro-6-fluorophenylamino)-7-methylpiperazine-6-aminoquinazoline 

Relevant articles and documents

High-affinity epidermal growth factor receptor (EGFR) irreversible inhibitors with diminished chemical reactivities as positron emission tomography (PET)-imaging agent candidates of EGFR overexpressing tumors

Previous studies with the anilinoquinazoline epidermal growth factor receptor (EGFR) irreversible inhibitor [11C]-ML03 demonstrated a rapid metabolism of the tracer, which led to its low in vivo accumulation in EGFR overexpressing tumors. To enhance tumor uptake, the chemical structure of the compound was modified, and four new groups of EGFR inhibitors with a wide range of chemical reactivities were synthesized. Chemical reactivity assay of the compounds, performed with reduced glutathione (GSH), revealed that the group C (4-(dimethylamino)-but-2-enoic amide) derivative was the least chemically reactive against the nucleophilic attack of GSH. Nonetheless, it demonstrated a high inhibitory potency and bound irreversibly to the EGFR. Consequently, the blood stability of the group C compound (5a, ML04) labeled with 11C was studied. In a time frame of 60 min, no radioactive metabolites were detected in blood. The stability of [11C]-5a, as indicated both from in vitro blood-stability assays and injection into nude rats, was significantly higher as compared to [11C]-ML03. Since group C presented a greater promise for tumor accumulation, it represents, to date, the most suitable candidate for radiolabeling with long-lived positron emission tomography (PET) radioisotopes.

POLYALKYLENE GLYCOL DERIVATIVES OF IRREVERSIBLE INHIBITORS OF EPIDERMAL GROWTH FACTOR RECEPTOR TYROSINE KINASE

Novel epidermal growth factor receptor tyrosine kinase (EGFR-TK) irreversible inhibitors, pharmaceutical compositions including same and their use in the treatment of EGFR-TK related diseases or disorders are disclosed. Novel radiolabeled EGFR-TK irrevers