897441-42-8

Basic information

• Product Name: N-(3-chloro-4-(pyridin-2-ylmethoxy)phenyl)-7-fluoro-6-nitroquinazolin-4-amine
• Synonyms: N-(3-chloro-4-(pyridin-2-ylmethoxy)phenyl)-7-fluoro-6-nitroquinazolin-4-amine
• CAS NO: 897441-42-8
• Molecular Weight: 425.806
• Mol File: 897441-42-8.mol
• Article Data: 7

Chemical Properties

• CAS DataBase Reference: N-(3-chloro-4-(pyridin-2-ylmethoxy)phenyl)-7-fluoro-6-nitroquinazolin-4-amine(CAS DataBase Reference)
• NIST Chemistry Reference: N-(3-chloro-4-(pyridin-2-ylmethoxy)phenyl)-7-fluoro-6-nitroquinazolin-4-amine(897441-42-8)
• EPA Substance Registry System: N-(3-chloro-4-(pyridin-2-ylmethoxy)phenyl)-7-fluoro-6-nitroquinazolin-4-amine(897441-42-8)

Safety Data

• Hazardous Substances Data: 897441-42-8(Hazardous Substances Data)

Upstream product

• 1194097-41-0 2-amino-4-fluoro-5-nitrobenzoic acid 
• 162012-69-3 7-fluoro-6-nitro-3H-quinazolin-4-one 
• 162012-70-6 4-chloro-7-fluoro-6-nitroquinazoline 
• 524955-09-7 3-chloro-4-(2-pyridylmethoxy)aniline 

Downstream Products

• 897384-03-1 N-(3-chloro-4-(pyridin-2-ylmethoxy)phenyl)-7-methoxy-6-nitroquinazoline-4-amine 
• 1402086-41-2 (E)-N-(4-(3-chloro-4-(pyridin-2-ylmethoxy)phenylamino)-7-(2-methoxyethoxy)quinazolin-6-yl)-4-(dimethylamino)but-2-enamide 
• 897025-71-7 C₂₃H₂₂ClN₅O₃ 
• 897025-29-5 (2S)-pyrrolidine-2-carboxylic acid {4-[3-chloro-4-(pyridin-2-ylmethoxy)-phenylamino]-7-fluoro-quinazolin-6-yl}-amide 

Relevant articles and documents

POLYMORPHIC FORMS AND RELATED USES

The present disclosure relates to polymorphic forms of the receptor tyrosine kinases inhibitor compound of formula (I), pharmaceutical compositions comprising the polymorphic forms, methods of making the polymorphic forms, and methods of using the polymor

Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors

A series of novel quinazoline derivatives bearing various C-6 benzamide substituents were synthesized and evaluated as EGFR inhibitors, and most showed significant inhibitory potency against EGFR kinase. In particular, compound 6g possessed potent inhibitory activity against EGFR wild-type (IC50 = 5 nM), and strong antiproliferative activity against HCC827 and Ba/F3 (L858R) cell lines. Kinase profiling against a panel of 365 kinases showed that 6g was highly selective for EGFR. Furthermore, 6g showed desirable properties in assays of liver microsome metabolic stability and cytochromes P450 inhibition and preliminary pharmacokinetic study. The overall attractive profile of 6g made it an interesting compound for further development.

Structure-activity study of quinazoline derivatives leading to the discovery of potent EGFR-T790M inhibitors

We have developed a series of 6, 7-disubstituted-4-(arylamino) quinazoline derivatives that functioned as irreversible EGFR inhibitors, and these compounds exhibited excellent enzyme inhibition potency. As compared with afatinib, some of them showed significantly enhanced activities towards H1975 cells (EGFR-T790M). Furthermore, the optimized compounds 7q and 8f also demonstrated good pharmacokinetic profiles, oral bioavailability as well as excellent in vivo efficacy in H1975 and HCC827 xenografts at a non-toxic dose. Based on the improved safety and efficacy against EGFR-T790M resistance, 7q and 8f are promising candidates for further studies.