Inhibition of colony formation and cell viability of myeloid leukemia cell lines by MEK and PPMTase
| Cell line . | Leukemia . | Ras-to-MAPK . | U0126 . | PD098059 . | FTS . |
|---|---|---|---|---|---|
| HL-60 N-RAS/61 | AML M2 | ++ | 100 | 81.4 ± 8.1 | 64.4 ± 6.8 |
| Kasumi-1 K-RAS/12 | AML M2 | + | 100 | 100 | 100 |
| Mutz-2 | AML M2 | (+) | 100 | 62.1 ± 3.3 | 37.9 ± 11.4 |
| NB-4 t15;17 PML/RARA | AML M3 | +++ | 100 | 16.5 ± 6.8 | 46.5 ± 6.0 |
| THP-1 N-RAS/12 | AML M4 | ++ | 87.5 | 50 | 0 |
| PBL-985 | AML M4 | + | 100 | 54.6 ± 7.4 | 54.6 ± 6.5 |
| OCI-AML2 | AML M4 | — | 100 | 100 | 0 |
| OCI-AML5 | AML M4 | — | 99.1 ± 0.8 | 63.3 ± 5.2 | 20.5 ± 15.5 |
| Mutz-3 | AML M4 | — | 99.2 ± 0.3 | 56.3 ± 2.1 | 0 |
| ML-2 t6;11, MLL/AF6 | AML M4 | + | 100 | 100 | 0 |
| MV4-11 K-RAS/12&18 t4;11, MLL/AF4 | AML M5 | ++ | 100 | 100 | 13.4 ± 7.2 |
| Mono-Mac-1 | AML M5 | +++ | 90 | 0 | 20 |
| KG-1 | AML M6 | + | 90 | 50 | 50 |
| M-07e | AML M7 | + | 100 | 0 | 0 |
| EM-2 BCR-Abl | CML | — | 100 | 0 | 64.4 ± 12.5 |
| JK-1 BCR-Abl | CML | — | 100 | 70.5 ± 3.9 | 26.1 ± 12.0 |
| K562 BCR-Abl | CML | + | 100 | 30.4 ± 25.7 | 53.3 ± 22.1 |
| MEG-01 BCR-Abl | CML | — | 99.6 ± 0.6 | 79.4 ± 1.8 | 97.8 ± 1.6 |
| LAMA-84 BCR-Abl | CML | — | 100 | 87.6 ± 1.0 | 100 |
| Cell line . | Leukemia . | Ras-to-MAPK . | U0126 . | PD098059 . | FTS . |
|---|---|---|---|---|---|
| HL-60 N-RAS/61 | AML M2 | ++ | 100 | 81.4 ± 8.1 | 64.4 ± 6.8 |
| Kasumi-1 K-RAS/12 | AML M2 | + | 100 | 100 | 100 |
| Mutz-2 | AML M2 | (+) | 100 | 62.1 ± 3.3 | 37.9 ± 11.4 |
| NB-4 t15;17 PML/RARA | AML M3 | +++ | 100 | 16.5 ± 6.8 | 46.5 ± 6.0 |
| THP-1 N-RAS/12 | AML M4 | ++ | 87.5 | 50 | 0 |
| PBL-985 | AML M4 | + | 100 | 54.6 ± 7.4 | 54.6 ± 6.5 |
| OCI-AML2 | AML M4 | — | 100 | 100 | 0 |
| OCI-AML5 | AML M4 | — | 99.1 ± 0.8 | 63.3 ± 5.2 | 20.5 ± 15.5 |
| Mutz-3 | AML M4 | — | 99.2 ± 0.3 | 56.3 ± 2.1 | 0 |
| ML-2 t6;11, MLL/AF6 | AML M4 | + | 100 | 100 | 0 |
| MV4-11 K-RAS/12&18 t4;11, MLL/AF4 | AML M5 | ++ | 100 | 100 | 13.4 ± 7.2 |
| Mono-Mac-1 | AML M5 | +++ | 90 | 0 | 20 |
| KG-1 | AML M6 | + | 90 | 50 | 50 |
| M-07e | AML M7 | + | 100 | 0 | 0 |
| EM-2 BCR-Abl | CML | — | 100 | 0 | 64.4 ± 12.5 |
| JK-1 BCR-Abl | CML | — | 100 | 70.5 ± 3.9 | 26.1 ± 12.0 |
| K562 BCR-Abl | CML | + | 100 | 30.4 ± 25.7 | 53.3 ± 22.1 |
| MEG-01 BCR-Abl | CML | — | 99.6 ± 0.6 | 79.4 ± 1.8 | 97.8 ± 1.6 |
| LAMA-84 BCR-Abl | CML | — | 100 | 87.6 ± 1.0 | 100 |
Cells were seeded at 1.0 to 2.5 × 105/mL of cell suspension in a 96-well plate and treated with 50 μM inhibitor or solvent control for 4 days. Aliquots of the cell suspensions were then plated in 400 μL methylcellulose for 7 to 14 days and cell growth was evaluated as described in “Materials and methods.” Inhibition is given in percentage of solvent control.
For abbreviations, see Tables 1 and 2.