| Cell line: |  | PMC42-ET | PMC42-LA | MDA-MB-468 | |||||
---|---|---|---|---|---|---|---|---|---|---|
 | Stimulus: |  | EGF | HPX | ||||||
 | Measured IC 50 for: | Biochemical assay (published data from compound vendors) | % vimentin-positive cells (μM) | Cell count ( μM) | % vimentin-positive cells ( μM) | Cell count ( μM) | % vimentin-positive cells ( μM) | Cell count ( μM) | % vimentin-positive cells ( μM) | Cell count ( μM) |
Targets: | Compound name | Â | Â | Â | Â | Â | Â | Â | Â | Â |
 | Erlotinib (Tarceva) | EGFR (2 nM) | >25 | 15.04 | 0.18 | 16.42 | 0.14 | 16.42 | 5.71 | >25 |
 | Lapatinib (GW572016) | EGFR (10.2 nM), HER2 (9.8 nM) | >25 | 2.46 | 0.57 | 1.65 | 4.32 | 2.99 | 1.96 | 1.44 |
a) HERs/EGFR | Vandetanib (Zactima) | VEGFR2 (40 nM), VEGFR3 (110 nM), EGFR (500 nM) | >25 | 1.84 | 0.57 | 1.57 | 0.50 | 3.77 | - | - |
 | Gefitinib (Iressa) | EGFR (33 nM) | >25 | 5.78 | 0.26 | 1.48 | 0.25 | 2.31 | 6.62 | 6.27 |
 | TOVOK (Afatinib) | Irreversible binder. EGFR (0.5 nM), HER2 (14 nM) | >25 | 1.24 | 0.02 | 0.96 | 0.03 | 0.26 | 2.38 | 1.01 |
 | AV-412 | EGFR (43 nM), HER2 (282 nM) | >25 | 0.33 | 0.05 | 0.32 | 0.05 | 0.54 | >25 | 0.06 |
 | U0126 | MEK1 (70 nM), MEK2 (60 nM) | >25 | >25 | 1.38 | >25 | 0.38 | 8.74 | 4.99 | >25 |
 | SL 327 | MEK1 (180 nM), MEK2 (220 nM) | >25 | 16.43 | 1.43 | >25 | >25 | 12.56 | >25 | 0.03 |
b) MEK-1/2 | PD 198306 | MEK (8 nM) | >25 | 1.36 | 0.34 | 2.50 | 0.46 | 0.97 | 1.7 | 2.94 |
 | AZD6244 (Selumetinib) | MEK1 (14 nM) | >25 | >25 | 0.06 | >25 | 1.38 | 13.71 | >25 | >25 |
 | CI-1040 (PD-184352) | MEK (1–1.3 nM) | >25 | 3.27 | 0.16 | 1.40 | 0.19 | 2.00 | 4.7 | 6.33 |
 | PD0325901 | MEK (0.33 nM) | >25 | >25 | <0.02 | >25 | <0.02 | 2.77 | 4.17 | 0.06 |
 | PD173955-Analogue 1 | c-Src (9 nM) | >25 | 5.94 | >25 | 6.28 | 1.70 | 3.40 | 6.55 | >25 |
 | Saracatinib (AZD0530) | Src (2.7 nM) | >25 | 0.75 | 0.94 | 0.50 | >25 | 6.35 | >25 | 0.72 |
c) Src family | Bosutinib (SKI-606) | Src (1.2 nM), Abl (1 nM) | >25 | 1.40 | 0.23 | 1.17 | 0.25 | 1.05 | 1.19 | 0.54 |
 | Dasatinib (BMS-354825) | Src (0.8 nM), Abl (0.6 nM) | >25 | 0.04 | 0.76 | <0.02 | 0.64 | 5.59 | >25 | 0.04 |
 | PD173952 | Src (8 nM), Lck (5 nM), FGFR1 (100 nM) | >25 | 0.35 | 1.61 | 0.23 | 0.10 | 0.25 | - | - |
 | PIK-90 | PI3K (α 11 nM, β 350 nM, γ 18 nM, δ 58 nM) | >25 | 16.35 | >25 | 16.36 | 3.26 | >25 | >25 | <0.02 |
 | ZSTK474 | PI3K (α 17 nM, β 53 nM, γ 6 nM) | >25 | 0.83 | >25 | 2.11 | 0.21 | 0.72 | 2.35 | >25 |
 | GDC-0941 | PI3K (α 3 nM, β 33 nM, γ 75 nM, δ 3 nM) | >25 | 0.46 | 8.67 | 1.18 | 1.27 | 1.79 | 4.69 | 4.88 |
 | BEZ-235 (NVP-BEZ235) | p110 (α 4 nM, β 75 nM, γ 5 nM, δ 7 nM) | >25 | 0.06 | >25 | >25 | 0.02 | 0.05 | 0.05 | 3.43 |
d) PI3K/mTOR | PI103 | DNA-PK (2 nM), mTORC1 (20 nM), PI3K-C2b (26 nM), p110 (α 8 nM, β 88 nM, γ 150 nM, δ 48 nM) | 15.18 | 0.32 | >25 | 1.82 | 0.38 | 0.88 | 1.22 | 1.04 |
 | GNE-493 | PI3K (α 3.4 nM, β 12 nM, γ 16 nM, δ 16 nM) | >25 | 1.11 | >25 | 12.09 | 0.29 | 1.45 | 0.99 | 6.41 |
 | GSK2126458 (HYR-582) | Ki: P110 (α 0.019 nM, β 0.13 nM, γ 0.06 nM, δ 0.024 nM), mTORC1 (0.18 nM), mTORC2 (0.3 nM) | >25 | 0.02 | 6.69 | 0.62 | <0.02 | 0.08 | 0.29 | 0.74 |
 | GNE-490 | PI3K (α 3.5 nM, β 25 nM, γ 5.2 nM, δ 15 nM) | >25 | 2.16 | >25 | 2.23 | 0.93 | 1.25 | 12.68 | >25 |
 | LY294002 | PI3K (α 0.5 uM, β 0.97 uM, γ 0.57 uM) | >25 | 14.86 | >25 | 12.12 | 4.18 | 13.22 | >25 | >25 |
 | GSK690693 | Akt1 (2 nM), Akt2 (13 nM), Akt3 (9 nM) | >25 | >25 | >25 | 8.32 | >25 | 3.31 | >25 | >25 |
 | A-674563 | Ki: Akt1 (11 nM), PKA (16 nM), CDK2 (46 nM), ERK2 (260 nM) | >25 | 0.48 | 0.17 | 0.76 | 0.65 | 0.25 | 2.83 | 0.60 |
 | Akt-i-1 | Akt1 (4.6 μM) | >25 | >25 | >25 | >25 | >25 | 6.46 | >25 | 12.30 |
e) Akt | Akt-i-1/2 | Akt1 (58 nM), Akt2 (210 nM) | >25 | >25 | >25 | >25 | >25 | 2.82 | >25 | 4.79 |
 | AT7867 | Akt1 (32 nM), Akt2 (17 nM), Akt3 (47 nM), PKA (20 nM) | >25 | 2.63 | >25 | 0.24 | >25 | 2.95 | >25 | 4.57 |
 | AZD5363 | Akt1 (3 nM), Akt2 (8 nM), Akt3 (8 nM), ROCK2 (56 nM) | >25 | >25 | >25 | >25 | 0.63 | >25 | >25 | >25 |
 | Merck-22-6 | Akt1 (138 nM), Akt2 (212 nM) | >25 | 4.27 | >25 | 1.48 | >25 | 0.46 | >25 | 0.55 |
 | MK-2206 | Akt1 (8 nM), Akt2 (12 nM), Akt3 (65 nM) | >25 | 5.62 | >25 | 3.16 | >25 | 1.86 | >25 | 9.77 |