GNF-6 is a potent inhibitor of the BCR-ABL-T315I mutation, acting primarily as an ATP-competitive inhibitor. It demonstrates inhibitory activity with IC50 values of 0.25 μM for c-ABL-T334I, 0.09 μM for BCR-ABL, and 0.590 μM for the BCR-ABL-T315I variant. By disrupting the assembly of the hydrophobic spine, GNF-6 stabilizes the kinase in an inactive 'DFG-out' conformation, making it a valuable tool for research on resistance mechanisms in chronic myeloid leukemia (CML) and targeted therapeutic strategies.
GNF-6 is a potent inhibitor of the BCR-ABL-T315I mutation, acting primarily as an ATP-competitive inhibitor. It demonstrates inhibitory activity with IC50 values of 0.25 μM for c-ABL-T334I, 0.09 μM for BCR-ABL, and 0.590 μM for the BCR-ABL-T315I variant. By disrupting the assembly of the hydrophobic spine, GNF-6 stabilizes the kinase in an inactive 'DFG-out' conformation, making it a valuable tool for research on resistance mechanisms in chronic myeloid leukemia (CML) and targeted therapeutic strategies.
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