Table 2

Growth inhibitory profile of KW-2449

Cell linesKW-2449Imatinib
32D transfectant   
    Mock (with IL-3) > 10 — 
    FLT3/ITD 0.024 — 
    FLT3/D835Y 0.046 — 
    Wt-FLT3/FL 0.014 — 
Human leukemia   
    MOLM-13 0.024 > 10 
    MV4;11 0.011 — 
    RS4;11 0.23 20 
    HL-60 0.65 > 10 
BCR/ABL+ leukemia   
    K562 0.27 0.24 
    TCC-Y 0.49 0.18 
    TCC-Y/sr 0.42 24 
Cell linesKW-2449Imatinib
32D transfectant   
    Mock (with IL-3) > 10 — 
    FLT3/ITD 0.024 — 
    FLT3/D835Y 0.046 — 
    Wt-FLT3/FL 0.014 — 
Human leukemia   
    MOLM-13 0.024 > 10 
    MV4;11 0.011 — 
    RS4;11 0.23 20 
    HL-60 0.65 > 10 
BCR/ABL+ leukemia   
    K562 0.27 0.24 
    TCC-Y 0.49 0.18 
    TCC-Y/sr 0.42 24 

Growth inhibition GI50 (μmol/L). GI50 values of KW-2449 and imatinib were determined by in vitro XTT assays. MOLM-13 and MV4;11 cells had FLT3/ITD. K562 and TCC-Y cells had wt-BCR/ABL, and TCC-Y/sr had the T315I mutation in the BCR/ABL gene.

— indicates not applicable.

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