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- Inventor Info
|Synonyms||Src/Abl1 Kinase Inhibitor AZD0424|
Potent and selective inhibitor of Src/Abl1 kinases showing additional activity against other Src family kinase members including Yes, Fgr, Lck, Hck, Fyn and Blk.
Suggested application in Alzheimer's disease, schizophrenia and treatment of alcoholism; Saracatinib, a related Src inhibitor has been used in clinical trials for Alzheimer’s disease and alcoholism.
|On Target IC50||4 nM|
Src family kinase members including Fyn, Yes, Fgr, Lck, Hck, and Blk screened at 100nM at which of the SrcA family it had >99% inhibition of Src.
In comparison Yes was 97%, Fgr 93% and Fyn 86% inhibited.
ADZ0424 shows potent inhibition of proliferation of engineered Src kinase over-expressing mouse fibroblasts and growth factor stimulated HUVEC cultures.
Also a potent inhibitor of in vitro migration of human tumour cells.
The tool further shows evidence of inhibition of phosphorylation of the Src kinase substrate paxillin, indicating inhibition of Src-mediated adhesion and motility signalling pathways.
Profound dose-dependent inhibition of tumour growth in mouse xenograft models over-expressing an activated form of Src.
Moderate anti-tumour growth effects were also seen in rats bearing human Calu-6 lung tumour xenografts.
|Research Area||Cancer, Drug Discovery & Development, Neurobiology, Other|
|Storage||Cold storage required (2-8°C)|
Blocking the activity of the Src family kinase Fyn slows the progression of Alzheimer’s disease.
Fyn has been implicated in involvement in signalling pathways that may lead to other severe brain pathologies such as Parkinson’s disease. Fyn also plays a role in the regulation of amyloid-β (Αβ) plaque production and mediates Αβ-induced synaptic deficits and neurotoxicity and is also known to induce tyrosine phosphorylation of tau.
Src has also been shown to play a role in alcoholism.
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