733009-42-2

Usage

Uses

Used in Pharmaceutical Industry:
Acetamide, 2-chloro-N-[4-[(4,5-dichloro-2-fluorophenyl)amino]-6-quinazolinyl]is used as an EGFR inhibitor for inhibiting EGFR-kinase activity and blocking phosphorylation. This makes it a potential candidate for the development of drugs targeting cancer cells with high EGFR expression levels.
Used in Cancer Research:
In cancer research, Acetamide, 2-chloro-N-[4-[(4,5-dichloro-2-fluorophenyl)amino]-6-quinazolinyl]is used to study the effects of EGFR inhibition on tumor growth and progression. Its ability to induce apoptosis and cell cycle arrest makes it a valuable tool for understanding the mechanisms of cancer cell death and the development of targeted therapies.
Used in Drug Combination Therapy:
Acetamide, 2-chloro-N-[4-[(4,5-dichloro-2-fluorophenyl)amino]-6-quinazolinyl]is used in combination with other drugs, such as Genistein, to enhance the suppression of leiomyoma cell proliferation. This combination therapy approach can potentially improve the efficacy of treatments and overcome drug resistance in cancer cells.

Biochem/physiol Actions

Target IC50: 0.7 μM and 1.1 μM suppressesing leiomyoma and myometrical cell proliferation, respectively

Upstream product

• 79-04-9 chloroacetyl chloride 
• 455922-81-3 6-amino-4-(4,5-dichloro-2-fluorophenylamino)quinazoline 
• 6943-17-5 6-nitroquinazolone 
• 2729-36-4 4,5-dichloro-2-fluoro-phenylamine 
• 2339-78-8 1,2-dichloro-4-fluoro-5-nitrobenzene 
• 455922-78-8 4-[(3,4-dichloro-6-fluorophenyl)amino]-6-nitroquinazoline 
• 616-79-5 2-amino-5-nitro-benzoic acid 
• 19815-16-8 4-chloro-6-nitro-quinazoline 

Downstream Products

• 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 
• 1400741-85-6 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.