Selective, non-ATP competitive allosteric inhibitor of Bcr-Abl (IC50
= 220 nM for wild-type Abl). Binds the myristate-binding site of Abl. Acts in combination with nilotinib to inhibit T315I Bcr-Abl in vitro
and in vivo
. Analog of GNF 2
(Cat. No. 4399).
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.
Allosteric interactions between the myristate- and ATP-site of the Abl kinase.
Iacob et al.
PLoS One, 2011;6:e15929
Expanding the diversity of allosteric Bcr-Abl inhibitors.
Deng et al.
Targeting Bcr-Abl by combining allosteric with ATP-binding-site inhibitors.
Zhang et al.