2 Biological Activity
TAE684 (NVP-TAE684) is 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. [1]
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. [1]
In vivo, NVP-TAE684 suppressed lymphomagenesis in two independent models of ALK-positive ALCL and induced regression of established Karpas-299 lymphomas. [1]
3 References:
Identification of NVP-TAE684, a potent, selective,and efficacious inhibitor of NPM-ALK Anna V. Galkin,Jonathan S. Melnick,et al. PNAS January 2, 2007;104:270–275
The pharmacological and toxicological properties of this product have not been fully investigated. Exercise caution in use and handling. This product must not be used in humans.