Bcr-abl Inhibitor

A cell-permeable and reverisble pyrimidine compound that binds to the c-abl myristoyl binding pocket and acts as an allosteric, non-ATP-competitive inhibitor of cellular Bcr-abl activity and Bcr-abl-dependent cellular functions. Exhibits little inhibitory effect against a panel of 63 kinases even at concentration as high as 10 µM. Exhibits potent and selective antiproliferative activity toward Bcr-abl-expressing cells (IC₅₀ = 138 nM, 194 nM, 268 nM and 273 nM in Ba/F3.p210, Ba/F3.p^185Y253H, SUP-B15 and Ba/F3.p^210E255V, and K562, respectively). Brij-35 is reported to mask the inhibitory effect of GNF-2 in cell-free c-abl and Bcr-abl kinase assays.

Cell permeable: yes

Primary Target
Bcr-abl-expressing cells in Ba/F3.p210

Product does not compete with ATP.

Reversible: yes

Target IC₅₀: 138 nM, 194 nM, 268 nM and 273 nM in Ba/F3.p210, Ba/F3.p185Y253H, SUP-B15 and Ba/F3.p210E255V, and K562, respectively

Packaged under inert gas

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Zhang, J., et al. 2010. Nature463, 501.
Choi, Y., et al. 2009. J. Biol. Chem.284, 29005.
Adrian, F.J., et al. 2006. Nat. Chem. Biol.2, 95.

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Toxicity: Irritant (B)