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Saracatinib (AZD0530)
Cat No.
CEI-0268
Description
Saracatinib (AZD0530) can inhibit src and abl with IC50 of 2.7 nM and 30 nM.
CAS No.
379231-04-6
Molecular Weight
542.03
Purity
>99%
Storage
2 years at -20centigrade Powder
Targets
Src, Abl
Molecular Formula
C27H32ClN5O5
Chemical Name
N-(5-chlorobenzo[d][1,3]dioxol-4-yl)-7-(2-(4-methylpiperazin-1-yl)ethoxy)-5-(tetrahydro-2H-pyran-4-yloxy)quinazolin-4-amine
Solubility
DMSO 108 mg/mL Water
In vitro
AZD0530 is a novel Src family kinase/Abl dual-kinase inhibitor and AZD 0530 can inhibit Src and Abl with IC50 of 2.7 nM and 30 nM. Src activation is inhibited by AZD0530 in a rapid and dose-dependent manner. AZD0530 inhibit Src resulting in decreased binding of beta-catenin to the promoters of G1 phase cell cycle regulators cyclin D1 and c-Myc. AZD0530 specifically inhibited the growth of, and induced apoptosis in CML and Ph+ ALL cells in a dose dependent manner, but showed only marginal effects on Ph- ALL cells. Resistance to Imatinib due to the mutation Y253F in p185Bcr-Abl was overcome by AZD0530. Combination of AZD0530 and Imatinib showed an additive inhibitory effect on the proliferation of CML BV173 cells but not on Ph+ ALL SupB15 cells. AZD0530 was most effective in inhibiting osteoclast-like cell formation. AZD0530 on human osteoclast differentiation and activity in a dose-depend manner. AZD0530 significantly reduced level of active phosphorylated c-Src in human osteoclast-like cells.
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