IC50 for the tyrosine kinase inhibitors AG957, AG490, and STI571 in proliferation assays
Cell line . | IC50 (μM) inhibitor ± growth factor . | |||||
---|---|---|---|---|---|---|
AG957 . | AG490 . | STI571 . | ||||
+GF . | −GF . | +GF . | −GF . | +GF . | −GF . | |
FDC-P1 | 5.0 (5) | N/E | 12.5 (5) | N/E | > 10 (3) | N/E |
FDbcr210A | 2.0 (3) | 2.5 (3) | 10.0 (3) | 10.0 (3) | — | — |
FDbcr210E | 3.5 (2) | 3.5 (2) | 12.5 (3) | 11.0 (3) | 0.65* (5) | 0.08* (5) |
FDbcr210G | 3.2 (2) | 3.2 (2) | 12.5 (2) | 12.5 (2) | — | — |
FDrv210C | 2.7 (3) | 2.5 (3) | 10.0 (3) | 11.2 (3) | — | — |
FDrv210F | 2.0 (2) | 2.5 (2) | 11.3 (2) | 12.5 (2) | — | — |
FDrv210H | 3.5 (2) | 3.5 (2) | 15.0 (3) | 15.0 (3) | 2.0* (4) | 0.25* (6) |
32D | 1.0 (2) | N/E | 12.5 (3) | N/E | 25.0 (4) | N/E |
32Dp210 | — | — | 12.5 (3) | 10.0 (3) | 4.0* (3) | 0.08* (3) |
MO7e | 1.0 (3) | N/E | > 40 (2) | N/E | 12.5 (4) | N/E |
MO7p210 | 4.0 (2) | 3.2 (2) | 26.7 (2) | 26.7 (2) | 0.7* (4) | 0.2* (4) |
K562 | 8.0 (3) | 8.0 (3) | > 40 (1) | > 40 (1) | 0.8† (3) | 0.8† (3) |
Cell line . | IC50 (μM) inhibitor ± growth factor . | |||||
---|---|---|---|---|---|---|
AG957 . | AG490 . | STI571 . | ||||
+GF . | −GF . | +GF . | −GF . | +GF . | −GF . | |
FDC-P1 | 5.0 (5) | N/E | 12.5 (5) | N/E | > 10 (3) | N/E |
FDbcr210A | 2.0 (3) | 2.5 (3) | 10.0 (3) | 10.0 (3) | — | — |
FDbcr210E | 3.5 (2) | 3.5 (2) | 12.5 (3) | 11.0 (3) | 0.65* (5) | 0.08* (5) |
FDbcr210G | 3.2 (2) | 3.2 (2) | 12.5 (2) | 12.5 (2) | — | — |
FDrv210C | 2.7 (3) | 2.5 (3) | 10.0 (3) | 11.2 (3) | — | — |
FDrv210F | 2.0 (2) | 2.5 (2) | 11.3 (2) | 12.5 (2) | — | — |
FDrv210H | 3.5 (2) | 3.5 (2) | 15.0 (3) | 15.0 (3) | 2.0* (4) | 0.25* (6) |
32D | 1.0 (2) | N/E | 12.5 (3) | N/E | 25.0 (4) | N/E |
32Dp210 | — | — | 12.5 (3) | 10.0 (3) | 4.0* (3) | 0.08* (3) |
MO7e | 1.0 (3) | N/E | > 40 (2) | N/E | 12.5 (4) | N/E |
MO7p210 | 4.0 (2) | 3.2 (2) | 26.7 (2) | 26.7 (2) | 0.7* (4) | 0.2* (4) |
K562 | 8.0 (3) | 8.0 (3) | > 40 (1) | > 40 (1) | 0.8† (3) | 0.8† (3) |
Data are median values for (n) experiments.
For MO7e and MO7p210, the growth factor (GF) was granulocyte-macrophage colony-stimulating factor. In all other cases, the growth factor was interleukin 3 (IL-3) supplied by WEHI-3BD-conditioned medium.
IC50 indicates 50% inhibitory concentration; N/E, nonevaluable (the nontransfected cell lines were factor dependent).
Analysis by 2-sided sign test. There were 16 tests across these cell lines, each providing a test of the effect of adding IL-3. In all 16 tests, the +IL-3 result was greater than the −IL-3 result. The chance of this occurring at random is only 1 in 32,768.
Analysis by 2-sided sign test. There were 3 tests for the K562 cell line. In only 1 of 3 tests was the +IL-3 result noticeably greater than the −IL-3 result; there was no discernible difference in the other 2 tests.