379228-40-7

Basic information

• Product Name: 5-Quinazolinol, 4-[(2-chloro-5-methoxyphenyl)amino]-
• CAS NO: 379228-40-7
• Molecular Formula: C15H12ClN3O2
• Molecular Weight: 301.732
• Mol File: 379228-40-7.mol
• Article Data: 1

Chemical Properties

• CAS DataBase Reference: 5-Quinazolinol, 4-[(2-chloro-5-methoxyphenyl)amino]-(CAS DataBase Reference)
• NIST Chemistry Reference: 5-Quinazolinol, 4-[(2-chloro-5-methoxyphenyl)amino]-(379228-40-7)
• EPA Substance Registry System: 5-Quinazolinol, 4-[(2-chloro-5-methoxyphenyl)amino]-(379228-40-7)

Safety Data

• Hazardous Substances Data: 379228-40-7(Hazardous Substances Data)

Upstream product

• 436-72-6 5-fluoroquinazolin-4(3H)-one 
• 135106-52-4 5-methoxy-4-(3H)-quinazolinone 
• 179246-14-1 4-chloro-5-methoxyquinazoline 

Relevant articles and documents

N-(5-chloro-1,3-benzodioxol-4-yl)-7-[2-(4-methylpiperazin-1-yl)ethoxy] -5-(tetrahydro-2H-pyran-4-yloxy)quinazolin-4-amine, a novel, highly selective, orally available, dual-specific c-Src/Abl kinase inhibitor

Src family kinases (SFKs) are nonreceptor tyrosine kinases that are reported to be critical for cancer progression. We report here a novel subseries of C-5-substituted anilinoquinazolines that display high affinity and specificity for the tyrosine kinase domain of the c-Src and Abl enzymes. These compounds exhibit high selectivity for SFKs over a panel of recombinant protein kinases, excellent pharmacokinetics, and in vivo activity following oral dosing. N-(5-Chloro-1,3-benzodioxol-4-yl)-7-[2-(4-methylpiperazin-1-yl)ethoxy]-5- (tetrahydro-2H-pyran-4-yloxy)quinazolin-4-amine (AZD0530) inhibits c-Src and Abl enzymes at low nanomolar concentrations and is highly selective over a range of kinases. AZD0530 displays excellent pharmacokinetic parameters in animal preclinically and in man (t1/2 = 40 h). AZD0530 is a potent inhibitor of tumor growth in a c-Src-transfected 3T3-fibroblast xenograft model in vivo and led to a significant increase in survival in a highly aggressive, orthotopic model of human pancreatic cancer when dosed orally once daily. AZD0530 is currently undergoing clinical evaluation in man.