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Description: GNF-2 (GNF 2; GNF2) is a highly potent, selective and allosteric/non-ATP competitive inhibitor of Bcr-Abl with potential anticancer activity. It shows no activity against Flt3-ITD, Tel-PDGFR, TPR-MET and Tel-JAK1 transformed tumor cells. GNF-2 acts by allosterically binding the myristate-binding site of ABL and inhibits the proliferation of BCR-ABL positive cell and induces cell apoptosis. GNF-2 eliminatedtransplanted-CML-T315I-mutants in vivo and dose dependently sensitizedprimary cells from CML T315I patients to GNF-2-induced proliferationinhibition and apoptosis
References: Nat Chem Biol. 2006; 2(2):95-102; J Biol Chem. 2009; 284(42):29005-14; Nature. 2010; 463:501-6.
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