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Contributor Information

  • Name Martin Swarbrick
  • Institute Cancer Research Technology AstraZeneca Metabolism Alliance Team

Tool Details

  • Tool name: PI4K alpha Inhibitor Small Molecule (Tool Compound)
  • Molecular formula: C23H25N5O4S2
  • Tool type: Small molecules
  • Tool sub-type: Inhibitor
  • Purpose: Inhibitor
  • Molecular weight of the target: 499.13
  • Description: Potent, small molecule inhibitor of PI4Ka, with no significant activity towards related kinases in the pathway. In a cellular environment, inhibition of PI4Ka led to a reduction in phosphatidylionositol-4-phosphate and phosphatidylionositol-4,5-biphosphate concentration, causing inhibition of inositol-1-phosphate formation and inhibition of proliferation in a panel of cancer cell lines.
  • Research area: Drug Discovery & Development;
  • Selectivity: 5.9 (PI4Kβ); 5.2 (PI3KÎą); <4.0 (PIP5KÉŁ); activity against only 3 kinases in the Millipore kinase panel (FGR 98%; ZIPK 72%; STK17A 68%; 259 kinases; tested at 1ÂľM)
  • IUPAC: >99%
  • IC50: 8.2 (PI4KÎą)
  • Additional notes: Compound 7 (PMID: 24366037). AstraZeneca Alliance. Purity >99%

  • For Research Use Only

Target Details

  • Target molecular weight: 499.13

Application Details

Handling

  • Purity: 499.13 g/mol
  • Solubility: 22 ľM
  • Shipping conditions: Dry Ice

Documentation

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  • Available on request

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References

  • •  Raubo et al. 2015. Bioorg Med Chem Lett. 25(16):3189-93. PMID: 26087940. Waring et al. 2014. Chem Commun (Camb). 50(40):5388-90. PMID: 24366037