267243-68-5

Basic information

• Product Name: N4-(3-chloro-4-fluorophenyl)-7-(3-Morpholinopropoxy)quinazoline-4,6-diaMine
• Synonyms: N4-(3-chloro-4-fluorophenyl)-7-(3-Morpholinopropoxy)quinazoline-4,6-diaMine;4-N-(3-chloro-4-fluorophenyl)-7-(3-morpholin-4-ylpropoxy)quinazoline-4,6-diamine
• CAS NO: 267243-68-5
• Molecular Formula: C₂₁H₂₃ClFN₅O₂
• Molecular Weight: 431.8910232
• EINECS: 1312995-182-4
• Mol File: 267243-68-5.mol
• Article Data: 9

Chemical Properties

• Boiling Point: 613.5±55.0 °C(Predicted)
• Appearance: /
• Density: 1.366±0.06 g/cm3(Predicted)
• Storage Temp.: Keep in dark place,Inert atmosphere,Room temperature
• PKA: 7.03±0.10(Predicted)
• CAS DataBase Reference: N4-(3-chloro-4-fluorophenyl)-7-(3-Morpholinopropoxy)quinazoline-4,6-diaMine(CAS DataBase Reference)
• NIST Chemistry Reference: N4-(3-chloro-4-fluorophenyl)-7-(3-Morpholinopropoxy)quinazoline-4,6-diaMine(267243-68-5)
• EPA Substance Registry System: N4-(3-chloro-4-fluorophenyl)-7-(3-Morpholinopropoxy)quinazoline-4,6-diaMine(267243-68-5)

Safety Data

• Hazardous Substances Data: 267243-68-5(Hazardous Substances Data)

Usage

General Description

N4-(3-chloro-4-fluorophenyl)-7-(3-Morpholinopropoxy)quinazoline-4,6-diaMine is a chemical compound with potential pharmacological properties. It belongs to the quinazoline class of compounds and contains a morpholinopropoxy group as well as a chloro-fluorophenyl moiety. N4-(3-chloro-4-fluorophenyl)-7-(3-Morpholinopropoxy)quinazoline-4,6-diaMine has shown potential as an inhibitor of certain enzymes and receptors, and it may have applications in the development of drugs for various diseases and conditions. Its chemical structure makes it a promising candidate for further research and development in the field of medicinal chemistry.

Upstream product

• 125422-83-5 4 (3-bromopropyl)-morpholine 
• 446-32-2 4-fluoroanthranilic acid 
• 162012-69-3 7-fluoro-6-nitro-3H-quinazolin-4-one 
• 16499-57-3 7-fluoro-3H-quinazolin-4-one 
• 4441-30-9 3-morpholin-4-ylpropan-1-ol 
• 367-21-5 3-chloro-4-fluorophenylamine 
• 865-47-4 potassium tert-butylate 
• 162012-67-1 N-(3-chloro-4-fluorophenyl)-7-fluoro-6-nitroquinazolin-4-amine 
• 162012-70-6 4-chloro-7-fluoro-6-nitroquinazoline 
• 267243-64-1 (3-chloro-4-fluorophenyl)-[7-(3-morpholino-4-yl-propoxy)-6-nitroquinazolin-4-yl]-amine 

Downstream Products

• 267243-28-7 canertinib 

Relevant articles and documents

Quinazoline derivative, preparation method and pharmaceutical application thereof

The invention discloses a quinazoline derivative, a preparation method and pharmaceutical application thereof. The invention provides the quinazoline derivative which is a compound shown as formula Iin the specification, and also provides a pharmaceutical

6-Oxooxazolidine–quinazolines as noncovalent inhibitors with the potential to target mutant forms of EGFR

Despite the remarkable benefits of gefitinib, the clinical efficacy is eventually diminished due to the acquired point mutations in the EGFR (T790M). To address this unmet medical need, we demonstrated a strategy to prepare a hybrid analogue consisting of the oxooxazolidine ring and the quinazoline scaffold and provided alternative noncovalent inhibitors targeting mutant forms of EGFR. Most of the derivatives displayed moderate to good anti-proliferative activity against gefitinib-resistant NCI-H1975. Some of them exhibited potent EGFR kinase inhibitory activities, especially on EGFRT790Mand EGFRL858Rkinases. SAR studies led to the identification of a hit 9a that can target both of the most common EGFR mutants: L858R and T790M. Also, 9a displayed weaker inhibitory against cancer cell lines with low level of EGFR expression and good chemical stability under different pH conditions. The work presented herein showed the potential for developing noncovalent inhibitors targeting EGFR mutants.

Clinical stage EGFR inhibitors irreversibly alkylate Bmx kinase

Irreversible HER/erbB inhibitors selectively inhibit HER-family kinases by targeting a unique cysteine residue located within the ATP-binding pocket. Sequence alignment reveals that this rare cysteine is also present in ten other protein kinases including all five Tec-family members. We demonstrate that the Tec-family kinase Bmx is potently inhibited by irreversible modification at Cys496 by clinical stage EGFR inhibitors such as CI-1033. This cross-reactivity may have significant clinical implications.