455922-81-3

Upstream product

• 616-79-5 2-amino-5-nitro-benzoic acid 
• 2729-36-4 4,5-dichloro-2-fluoro-phenylamine 
• 67-63-0 isopropyl alcohol 
• 455922-78-8 4-[(3,4-dichloro-6-fluorophenyl)amino]-6-nitroquinazoline 
• 2339-78-8 1,2-dichloro-4-fluoro-5-nitrobenzene 
• 6943-17-5 6-nitroquinazolone 
• 19815-16-8 4-chloro-6-nitro-quinazoline 

Downstream Products

• 733009-43-3 N-[4-(4,5-dichloro-2-fluoro-phenylamino)-quinazolin-6-yl]-2-methoxy-acetamide 
• 733009-42-2 TKS 050 
• 1400741-90-3 N-[4-[(4,5-dichloro-2-fluorophenyl)amino]quinazolin-6-yl]-2-hydrazinylacetamide 
• 1400741-91-4 N-[4-[(4,5-dichloro-2-fluorophenyl)amino]quinazolin-6-yl]-2-(5-sulfanyl-2-sulfanylidene-2,3-dihydro-1,3,4-thiadiazol-3-yl)acetamide 
• 1400741-92-5 N-[4-[(4,5-dichloro-2-fluorophenyl)amino]quinazolin-6-yl]-2-[5-[(2,5-dioxooxolan-3-yl)sulfanyl]-2-sulfanylidene-2,3-dihydro-1,3,4-thiadiazol-3-yl]acetamide 
• 1400741-85-6 2-([4-[([4-[(4,5-dichloro-2-fluorophenyl)amino]quinazolin-6-yl]carbamoyl)methyl]-5-sulfanylidene-4,5-dihydro-1,3,4-thiadiazol-2-yl]sulfanyl)butanedioic acid 

Relevant academic research and scientific papers

METHODS AND USE OF BIFUNCTIONAL ENZYME-BUILDING CLAMP-SHAPED MOLECULES

This invention is in the fields of cancer therapy. More particularly it concerns compounds which are useful agents for inhibiting cell proliferative disorders, especially those disorders characterized by over activity and/or inappropriate activity of a EG

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.

Radiolabeled irreversible inhibitors of epidermal growth factor receptor tyrosine kinase and their use in radioimaging and radiotherapy

Radiolabeled epidermal growth factor receptor tyrosine kinase (EGFR-TK) irreversible inhibitors and their use as biomarkers for medicinal radioimaging such as Positron Emission Tomography (PET) and Single Photon Emission Computed Tomography (SPECT) and as