GNF-2 CAS NO.778270-11-4

gnf-2 is a highly selective non-atp competitive inhibitor of oncogenic bcr-abl activity (ic50 = 0.14 μm).
ic50 value: 0.14 um [1]
target: bcr-abl
in vitro: ba/f3 cells harboring native or t315i mutated bcr-abl constructs were treated with gnf-2 and akis. we monitored the effect of gnf-2 with akis on the proliferation and clonigenicity of the different ba/f3 cells. in addition, we monitored the auto-phosphorylation activity of bcr-abl and jak2 in cells treated with gnf-2 and akis [2]. gnf-2 increased the effects of akis on unmutated bcr/abl. interestingly, the combination of dasatinib and gnf-2 overcame resistance of bcr/abl-t315i in all models used in a synergistic manner [3].gnf-2 dose-dependently inhibited the proliferation of osteoclast precursors through the suppression of the m-csfr c-fms. in addition, gnf-2 accelerated osteoclast apoptosis by inducing caspase-3 and bim expression. furthermore, gnf-2 interfered with actin cytoskeletal organization and subsequently blocked the bone-resorbing activity of mature osteoclasts [4].
in vivo: combining pdmp and gnf-2 eliminated transplanted-cml-t315i-mutants in vivo and dose dependently sensitized primary cells from cml t315i patients to gnf-2-induced proliferation inhibition and apoptosis[5].