Antia Laboratories Inc.

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Saracatinib (AZD0530)

CAS Number: 379231-04-6

Molecular Formula: C27H32ClN5O5

Molecular Weight: 542.03


1. AZD0530, a novel anilino quinazoline, is a potent dual-specific inhibitor of cSrc kinase (IC50: 2.7 nM) and the related Abl kinase (IC50: 30 nm). AZD0530 is highly selective for Src and Abl kinases against a large range of tyrosine and serine-threonine kinases (VEGFR2, FGFR, c-Kit, Aur-3 etc. >5 µM). AZD0530 exerts its activity through ATP competitive and reversible inhibition of the target enzyme. Structure-activity analyses that led to the discovery of AZD0530 are presented, focusing in particular on the critical role played by the aniline substitution pattern and the effect of the C5-C7 quinazoline substitution pattern. AZD0530 possesses excellent properties for a small molecule inhibitor of Src kinase that translate into excellent ADME properties in preclinical animal species. AZD0530 is orally available and is suitable for once-daily administration to humans. AZD0530 causes dramatic inhibition of human breast cancer cell (MDA-MB231) migration in vitro.AZD0530 completely prevents the growth of c-Src-NIH 3T3 xenografts grown in nude rats, and at 25 mg/kg/d significantly increases survival in an orthotopic model of human pancreatic cancer (BxPC-3). AZD0530 is a highly selective, orally available, dual-specific Src/Abl kinase inhibitor. It has the potential for activity in a wide range of tumors. AZD0530 is currently in early clinical development. 

2. "Effects of the Src Kinase Inhibitor Saracatinib (AZD0530)on Bone Turnover in Healthy Men: A Randomized,Double-Blind, Placebo-Controlled,Multiple-Ascending-Dose Phase I Trial" Rosemary A Hannon,Glen Clack,Martin Rimmer,Alan Swaisland,J Andrew Lockton,Richard D Finkelman,and Richard Eastell  Journal of Bone and Mineral Research, Vol. 25, No. 3, March 2010, pp 463–471 Full text

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