Table 2. IC50 for growth of Ba/F3 stable lines grown in the presence of BMS-354825 and imatinib.
Ba/F3 Clone | BMS-354825 IC50, nM (fold WT IC50) | Imatinib IC50, nM (fold WT IC50) |
---|---|---|
p210 WT | 1.34 (1) | 323 (1) |
L248R | 16 (12) | >10,000 (>30) |
Y253H | 10 (7.5) | >10,000 (>30) |
E255K | 13 (9.7) | 8,400 (26) |
V299L | 18 (13.4) | 540 (1.7) |
T315I | >1,000 (>750) | >10,000 (>30) |
T315A | 125 (93) | 760 (2.4) |
F317L | 18 (13.4) | 810 (2.5) |
F317V | 53 (40) | 350 (1.1) |
Viable cell counts normalized to the no-drug control were preformed after 3 days of growth in triplicate. Stable Ba/F3 cells were exposed to no drug, BMS-354825 (5, 10 25, 50, 100, 200, and 500 nM), and imatinib (500, 1,000, 5,000, and 10,000 nM). Biological IC50 was determined from semilogarithmic graphing of the dose–response curve for each mutant. The adjacent column represents the fold change in IC50 as compared with WT BCR-ABL.