#153985

[Src/Abl1] Inhibitor AZD0424 Small Molecule Tool Compound

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Cat. #153985

[Src/Abl1] Inhibitor AZD0424 Small Molecule Tool Compound

Cat. #: 153985

Sub-type: Inhibitor

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Contributor

Institute: AstraZeneca

Tool Details
Handling
Target Details
References

Tool Details

*FOR RESEARCH USE ONLY

  • Tool name: [Src/Abl1] Inhibitor AZD0424 Small Molecule Tool Compound
  • Alternate name: Src/Abl1 Kinase Inhibitor AZD424
  • Research fields: Cancer;Cell signaling and signal transduction;Other
  • Tool sub type: Inhibitor
  • Description: 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.
  • Purpose: Inhibitor
  • Selectivity: 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.
  • Additional notes: 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.

Handling

  • Storage conditions: Cold storage required (2-8° C)
  • Shipping conditions: Dry Ice

Target Details

  • Ic50: 4 nM

References

  • Woodcock et al. 2018. Br J Cancer. 118(6):770-776. PMID: 29438361.
  • A first-in-human phase I study to determine the maximum tolerated dose of the oral Src/ABL inhibitor AZD0424.