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Biological Activity:
A highly potent and selective smallmolecule ALK inhibitor, which blocked the growth of ALCL-derived and ALK-dependent cell lines with IC50 values between 2 and 10 nM.NVP-TAE684 treatment resulted in a rapid and sustained inhibition of phosphorylation of NPM-ALK and its downstream effectors and subsequent induction of apoptosis and cell cycle arrest.In vivo, NVP-TAE684 suppressed lymphomagenesis in two independent models of ALK-positive ALCL and induced regression of established Karpas-299 lymphomas.
References:
1. Hellwig S et al.Small-molecule inhibitors of the c-Fes protein-tyrosine kinase.Chem Biol19:529-40 (2012).
2. Galkin AV et al.Identification of NVP-TAE684, a potent, selective, and efficacious inhibitor of NPM-ALK.Proc Natl Acad Sci U S A104:270-5 (2007).