Overview

  • Product name
    PD 0325901
  • Description
    Potent MEK 1 and 2 inhibitor
  • Biological description
    Potent MEK 1 and 2 allosteric inhibitor (IC50 = 0.59 nM in vivo). Preferential binding (7-10-fold) to unphosphorylated MEK1 than pMEK1 in vitro. Induces apoptosis in malignant cells through p53, TRAIL, caspase, mitochondrial depolarisation and Bid activation. Systemically active following oral and intravenous administration.
  • Purity
    > 99%

Properties

References

This product has been referenced in:
  • Sheth PR  et al. Fully activated MEK1 exhibits compromised affinity for binding of allosteric inhibitors U0126 and PD0325901. Biochemistry 50:7964-76 (2011). Read more (PubMed: 21793567) »
  • Lunghi P  et al. Targeting MEK/MAPK signal transduction module potentiates ATO-induced apoptosis in multiple myeloma cells through multiple signaling pathways. Blood 112:2450-62 (2008). Read more (PubMed: 18583568) »
  • Brown AP  et al. Pharmacodynamic and toxicokinetic evaluation of the novel MEK inhibitor, PD0325901, in the rat following oral and intravenous administration. Cancer Chemother Pharmacol 59:671-9 (2007). Read more (PubMed: 16944149) »
  • Thompson N & Lyons J Recent progress in targeting the Raf/MEK/ERK pathway with inhibitors in cancer drug discovery. Curr Opin Pharmacol 5:350-6 (2005). Read more (PubMed: 15955734) »

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Please note: All products are "FOR RESEARCH USE ONLY AND ARE NOT INTENDED FOR DIAGNOSTIC OR THERAPEUTIC USE, NOT FOR USE IN HUMANS"

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