Table 1.

Tyrosine kinase sensitivity to CR4 inhibition


Kinase

IC50, μM
Btk   > 5  
Bcr-Abl   0.5-0.7  
Jak2   0.1-0.6  
Lck   > 5  
Lyn   > 50  
Src   > 25  
Syk   > 5  
Zap-70
 
> 5
 

Kinase

IC50, μM
Btk   > 5  
Bcr-Abl   0.5-0.7  
Jak2   0.1-0.6  
Lck   > 5  
Lyn   > 50  
Src   > 25  
Syk   > 5  
Zap-70
 
> 5
 

Results represent multiple independent experiments with each protein tyrosine kinase. In particular, Jak-2 and Bcr-Abl kinase assays were performed repeatedly (>6 each) on enzymes extracted from various cell lines including Ph+ and Ph ALL and AML. To reflect most accurately the large number of experiments, the range of IC50 for Jak-2 and Bcr-Abl is given.

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