Potent Raf kinase inhibitor (IC50
values are 2.1, 2.5 and 4.2 nM for B-RafV600E
, C-Raf and wild-type B-Raf respectively). Also inhibits Abl-1, DDR2, EPHA2 and RET tyrosine kinase activity. Inhibits pERK formation and attenuates tumor growth in melanoma cell xenografts expressing the B-RafV600E
mutation in vivo
. Orally bioavailable.
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Design and optimization of potent and orally bioavailable tetrahydronaphthalene Raf inhibitors.
Gould et al.