Table 2.

Summary of BCR-ABL kinase domain mutations




IC50 cell growth, μM imatinib

IC50 BCR/ABL phosphorylation

Location
Wild-type   0.08   0.11   NA  
M2371   0.17   0.25   Adjacent to P-loop  
L248V   4.62   1.87   P-loop  
D276G   2.97   0.60   C-helix  
G321E   2.61   0.39   Imatinib binding site  
Y353H   0.02   0.2   Adjacent to activation loop  
E373G
 
2.78
 
0.71
 
Activation loop
 



IC50 cell growth, μM imatinib

IC50 BCR/ABL phosphorylation

Location
Wild-type   0.08   0.11   NA  
M2371   0.17   0.25   Adjacent to P-loop  
L248V   4.62   1.87   P-loop  
D276G   2.97   0.60   C-helix  
G321E   2.61   0.39   Imatinib binding site  
Y353H   0.02   0.2   Adjacent to activation loop  
E373G
 
2.78
 
0.71
 
Activation loop
 

NA indicates not applicable.

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