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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.p185Y253H, SUP-B15 and Ba/F3.p210E255V, 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.
产品信息
Form White solid
Primary Target Bcr-abl-expressing cells in Ba/F3.p210
Primary Target IC50 138 nM
Secondary target Bcr-abl-expressing cells (IC50 = 194 nM, 268 nM and 273 nM in Ba/F3.p185Y253H, SUP-B15 and Ba/F3.p210E255V, and K562, respectively)
Molar mass 374.3
Protect from Light 是的
Packaged under inert gas 是的
Cell permeable 是的
Purity ≥97% by HPLC
Solubility DMSO or EtOH
Chemical formula C18H13F3N4O2
CAS number 778270-11-4
商店和运输信息
Storage +2°C to +8°C
Ship Ambient Temperature Only
Irritant |