Overview

  • Product name

    PP242, mTOR inhibitor
  • Description

    Potent, selective and ATP-competitive mTOR inhibitor
  • Biological description

    Potent, selective and ATP-competitive mTOR inhibitor (IC50 = 8 nM). Inhibits both mTORC1 and mTORC2. Activates ERK via TORC1/eIF-4E/RAF pathway in cancer cells. Selective for mTOR over PI3K family kinases (IC50 values are 0.1 (p110γ), 0.41 (DNA-PK), 1.27 (p110δ), 1.96 (p110α) and 2.2 (p110β) μM). Anticancer agent. Active in vivo and in vitro.
  • Purity

    > 98%
  • CAS Number

    1092351-67-1
  • Chemical structure

    Chemical Structure

Properties

References

This product has been referenced in:

  • Ono A  et al. Comparative effects of PP242 and rapamycin on mTOR signalling and NOTCH signalling in leukemia cells. Anticancer Res 33:809-13 (2013). Read more (PubMed: 23482748) »
  • Hoang B  et al. The PP242 mammalian target of rapamycin (mTOR) inhibitor activates extracellular signal-regulated kinase (ERK) in multiple myeloma cells via a target of rapamycin complex 1 (TORC1)/eukaryotic translation initiation factor 4E (eIF-4E)/RAF pathway and activation is a mechanism of resistance. J Biol Chem 287:21796-805 (2012). Read more (PubMed: 22556409) »
  • Apsel B  et al. Targeted polypharmacology: discovery of dual inhibitors of tyrosine and phosphoinositide kinases. Nat Chem Biol 4:691-9 (2008). Read more (PubMed: 18849971) »

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