SU5614-resistant cell lines are sensitive to PKC412
. | SU5614 . | . | PKC412 . | . | ||
|---|---|---|---|---|---|---|
. | IC50, μM . | Fold . | IC50, nM . | Fold . | ||
| ITD native | 0.2 | 1.0 | 7.5 | 1.0 | ||
| ITD-R1 | 4.5 | 23 | ND | ND | ||
| ITD-R2 | 5.2 | 26 | 8.7 | 1.2 | ||
| ITD-R3 | 2.1 | 11 | ND | ND | ||
| ITD-R4 | 1.3 | 6.5 | 17 | 2.3 | ||
. | SU5614 . | . | PKC412 . | . | ||
|---|---|---|---|---|---|---|
. | IC50, μM . | Fold . | IC50, nM . | Fold . | ||
| ITD native | 0.2 | 1.0 | 7.5 | 1.0 | ||
| ITD-R1 | 4.5 | 23 | ND | ND | ||
| ITD-R2 | 5.2 | 26 | 8.7 | 1.2 | ||
| ITD-R3 | 2.1 | 11 | ND | ND | ||
| ITD-R4 | 1.3 | 6.5 | 17 | 2.3 | ||
The IC50 of SU5614 in Ba/F3 FLT3-ITD-R2 and -R4 cells was determined as described in Figure 4. The IC50 of PKC412 was determined by MTT assays as described previously.15 Fold indicates the ratio of the IC50 of parental Ba/F3 FLT3-ITD cells to IC50 of R2 and R4 cell lines, respectively. All values represent means of 3 independent experiments.