Table 2: Relative activity of BCR/ABL inhibitors against different tyrosine kinases (adapted from Uitdehaag[19]).
Activity of BCR/ABL TKIs. The number represents the percentage of inhibition of tyrosine kinase activity at a concentration of 1μmol/l of each inhibitor.
Percentage inhibition of >95-100% noted in Red, 75-95% noted in Orange, 50-75% noted in Yellow, 25-50% noted in Blue, and <25% noted in Green.
BCR/ABL: breakpoint cluster region/Abelson murine leukemia gene; SRC: stored response chain, Sarcoma; TEC: Tec protein kinase; CAMK2G: Calcium/calmodulin dependent protein kinase; C-KIT: Mast/stem cell growth factor receptor; PDGFR: Platelet-derived growth factor receptor; EPHA: Ephrin tyrosine kinase; RET: rearranged during transfection proto-oncogene tyrosine kinase; TIE2: Angiopoietin 1 receptor; FGFR: fibroblast growth factor receptor; VEGFR: vascular endothelial growth factor receptor; TKI: tyrosine kinase inhibitor.
Activity of BCR/ABL TKIs. The number represents the percentage of inhibition of tyrosine kinase activity at a concentration of 1μmol/l of each inhibitor.
Percentage inhibition of >95-100% noted in Red, 75-95% noted in Orange, 50-75% noted in Yellow, 25-50% noted in Blue, and <25% noted in Green.
BCR/ABL: breakpoint cluster region/Abelson murine leukemia gene; SRC: stored response chain, Sarcoma; TEC: Tec protein kinase; CAMK2G: Calcium/calmodulin dependent protein kinase; C-KIT: Mast/stem cell growth factor receptor; PDGFR: Platelet-derived growth factor receptor; EPHA: Ephrin tyrosine kinase; RET: rearranged during transfection proto-oncogene tyrosine kinase; TIE2: Angiopoietin 1 receptor; FGFR: fibroblast growth factor receptor; VEGFR: vascular endothelial growth factor receptor; TKI: tyrosine kinase inhibitor.
