Potent and selective Src tyrosine kinase family inhibitor (IC50= 4-10 nM). Inhibits Src, c-Yes, Fyn, Lyn, Blk, Fgr, and Lck. Exhibits selectivity over other tyrosine kinases (IC50values are 30, 66 and 200 nM for v-Abl, EGFR and c-Kit, respectively). Supp
Storage Temp
Store at -20°C
Shipped In
Ice chest + Ice pads
Grade
Moligand™
Action Type
INHIBITOR
Mechanism of action
Tyrosine-protein kinase SRC inhibitor
Product Description
Saracatinib (AZD0530) is a potent Src inhibitor with IC50 of 2.7 nM, and potent to c-Yes, Fyn, Lyn, Blk, Fgr and Lck; less active for Abl and EGFR (L858R and L861Q). Phase 2/3. A diverse Src inhibitor.
Product Properties
ALogP
4.1
Associated Targets
CYBBTchem Cytochrome b-245 heavy chain 0 Activities
1.Hennequin LF, Allen J, Breed J, Curwen J, Fennell M, Green TP, Lambert-van der Brempt C, Morgentin R, Norman RA, Olivier A et al.. (2006) 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.. J Med Chem, 49 (22):(6465-88). [PMID:17064066]
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G2228128