Table 1.
Summary of cell area and roundness in 70 cancer drugs (including two controls). * These drugs are migration inhibition drugs without cytotoxicity.
| Targeted Anticancer Drug | Target | Chip Number #1 | Chip Number #2 | Chip Number #3 | Average | ||||||
|---|---|---|---|---|---|---|---|---|---|---|---|
| Cell Area [%] |
Round-ness [%] | Cell Area [%] |
Round-ness [%] | Cell Area [%] |
Round-ness [%] | Cell Area [%] |
Round-ness [%] | p-Value | |||
| 1 | DMSO | - | 94.79 | 103.36 | 100.88 | 94.29 | 108.20 | 99.99 | 101.29 | 99.21 | - |
| 2 | DMSO | - | 105.21 | 96.64 | 99.12 | 105.71 | 91.80 | 100.01 | 98.71 | 100.79 | - |
| 3 * | AEE788 (NVP-AEE788) | EGFR | 69.06 | 55.50 | 62.50 | 55.89 | 65.38 | 61.66 | 65.65 | 57.68 | 0.0001 |
| 4 | Afatinib (BIBW2992) | EGFR | 54.61 | 57.69 | 52.01 | 61.95 | 67.68 | 67.80 | 58.10 | 62.48 | 0.0006 |
| 5 | BMS-599626 (AC480) | EGFR | 81.63 | 73.69 | 76.44 | 78.58 | 88.11 | 99.62 | 82.06 | 83.96 | 0.75 |
| 6 | Erlotinib HCl | HER1/EGFR | 72.96 | 72.69 | 80.02 | 90.46 | 67.76 | 87.89 | 73.58 | 83.68 | 0.7216 |
| 7 * | Dacomitinib (PF299804, PF-00299804) | EGFR | 57.76 | 55.84 | 56.03 | 55.60 | 69.99 | 64.49 | 61.26 | 58.64 | 0.0001 |
| 8 * | Gefitinib (Iressa) | EGFR | 60.62 | 57.17 | 60.45 | 58.81 | 67.12 | 75.38 | 62.73 | 63.79 | 0.0011 |
| 9 | Lapatinib | EGFR | 67.08 | 57.42 | 72.09 | 85.04 | 75.61 | 78.18 | 71.59 | 73.55 | 0.0603 |
| 10 | Neratinib (HKI-272) | EGFR | 76.44 | 94.96 | 79.24 | 93.30 | 90.27 | 94.22 | 81.98 | 94.16 | 0.9992 |
| 11 | CI-1033 (Canertinib) | EGFR, HER2 | 38.26 | 54.89 | 47.97 | 55.21 | 52.14 | 68.18 | 46.13 | 59.43 | 0.0001 |
| 12 | CO-1686 | EGFR | 40.62 | 58.73 | 53.64 | 62.96 | 48.69 | 64.64 | 47.65 | 62.11 | 0.0005 |
| 13 | BKM120 (NVP-BKM120) | PI3K | 54.91 | 58.80 | 55.38 | 58.03 | 60.85 | 70.24 | 57.05 | 62.36 | 0.0006 |
| 14 | BYL719 | PI3K | 39.10 | 66.13 | 58.45 | 75.64 | 64.15 | 74.42 | 53.90 | 72.06 | 0.036 |
| 15 | XL147 | PI3K | 48.48 | 55.73 | 54.08 | 59.90 | 60.23 | 71.83 | 54.26 | 62.49 | 0.0006 |
| 16 | Everolimus (RAD001) | mTOR | 60.65 | 95.53 | 89.76 | 137.26 | 69.68 | 82.25 | 73.36 | 105.01 | 0.999 |
| 17 | AZD2014 | mTOR | 48.24 | 96.33 | 63.74 | 100.02 | 64.85 | 92.44 | 58.94 | 96.27 | 0.9996 |
| 18 | PF-05212384 (PKI-587) | PI3K/mTOR | 41.57 | 67.66 | 60.59 | 90.06 | 54.02 | 79.78 | 52.06 | 79.17 | 0.3033 |
| 19 | XL765 (SAR245409) | PI3K/mTOR | 80.57 | 105.60 | 82.54 | 106.67 | 71.79 | 105.11 | 78.30 | 105.79 | 0.9988 |
| 20 | BEZ235 | PI3K/mTOR | 79.75 | 104.83 | 88.85 | 132.12 | 63.90 | 125.80 | 77.50 | 120.92 | 0.1993 |
| 21 | AZD5363 | Akt1/2/3 | 125.69 | 188.76 | 127.99 | 184.57 | 72.51 | 149.46 | 108.73 | 174.26 | <0.0001 |
| 22 | ABT-199 (GDC-0199) | Bcl-2 | 56.94 | 81.25 | 67.70 | 79.67 | 50.74 | 84.60 | 58.46 | 81.84 | 0.5344 |
| 23 | ABT-888 (Veliparib) | PARP | 82.36 | 99.89 | 93.57 | 120.18 | 70.65 | 104.00 | 82.20 | 108.02 | 0.9983 |
| 24 * | AUY922 (NVP-AUY922) | HSP (e.g., HSP90) | 65.79 | 57.14 | 67.87 | 62.98 | 57.08 | 74.03 | 63.58 | 64.72 | 0.0017 |
| 25 | Axitinib | VEGFR1/2/3, PDGFRβ and c-Kit | 87.19 | 85.53 | 77.38 | 107.06 | 61.00 | 92.71 | 75.19 | 95.10 | 0.9994 |
| 26 | AZD4547 | FGFR1/2/3 | 51.78 | 64.85 | 62.87 | 72.44 | 68.26 | 83.80 | 60.97 | 73.70 | 0.0633 |
| 27 | AZD6244 (Selumetinib) | MEK1 | 65.14 | 72.99 | 62.75 | 69.57 | 72.98 | 80.13 | 66.96 | 74.23 | 0.0755 |
| 28 | LGK-974 | PORCN | 46.90 | 74.60 | 65.73 | 74.46 | 65.42 | 83.49 | 59.35 | 77.52 | 0.1995 |
| 29 | BGJ398 (NVP-BGJ398) | FGFR1/2/3 | 64.52 | 78.02 | 76.15 | 82.44 | 62.56 | 81.34 | 67.74 | 80.60 | 0.418 |
| 30 | Bortezomib (Velcade) | proteasome | 50.72 | 72.65 | 64.43 | 86.97 | 61.71 | 86.31 | 58.95 | 81.98 | 0.5476 |
| 31 * | Cediranib (AZD2171) | VEGFR, Flt | 68.77 | 68.14 | 63.70 | 62.38 | 60.78 | 73.95 | 64.42 | 68.16 | 0.0078 |
| 32 | Crizotinib (PF-02341066) | Met, ALK | 27.10 | 55.61 | 34.59 | 61.27 | 43.96 | 76.35 | 35.22 | 64.41 | 0.0015 |
| 33 | Dasatinib (BMS-354825) | Bcr-Abl | 45.84 | 60.08 | 52.31 | 67.96 | 60.87 | 80.35 | 53.01 | 69.46 | 0.0134 |
| 34 | Dovitinib (TKI-258) | Flt3, c-Kit, FGFR1/3, VEGFR1/2/3, PDGFRα/β | 39.31 | 64.12 | 44.12 | 61.21 | 50.03 | 72.33 | 44.49 | 65.89 | 0.0029 |
| 35 * | Imatinib (Gleevec) | v-Abl, c-Kit, and PDGFR | 60.99 | 56.33 | 58.13 | 64.82 | 63.48 | 73.51 | 60.87 | 64.89 | 0.0019 |
| 36 | INCB28060 | Met | 75.04 | 85.68 | 54.00 | 62.89 | 83.63 | 89.35 | 70.89 | 79.31 | 0.3133 |
| 37 * | LY2835219 | CDK4/6 | 65.04 | 63.88 | 61.82 | 61.12 | 74.88 | 72.56 | 67.25 | 65.85 | 0.0029 |
| 38 * | Cabozantinib (XL184) | VEGFR2,c-Met, Ret, Kit, Flt-1/3/4, Tie2, and AXL | 72.29 | 53.61 | 61.67 | 53.81 | 66.80 | 61.60 | 66.92 | 56.34 | 0.0001 |
| 39 * | Foretinib (XL880) | HGFR and VEGFR, mostly for Met and KDR | 68.42 | 62.34 | 54.61 | 51.91 | 60.14 | 65.09 | 61.06 | 59.78 | 0.0002 |
| 40 | Ibrutinib | Btk, modestly potent to Bmx, CSK, FGR, BRK, HCK | 64.18 | 57.45 | 56.69 | 61.32 | 52.83 | 61.29 | 57.90 | 60.02 | 0.0002 |
| 41 | Vemurafenib | B-Raf V600E | 89.30 | 87.57 | 73.61 | 85.28 | 81.12 | 95.50 | 81.34 | 89.45 | 0.998 |
| 42 * | Trametinib | MEK1/2 | 72.87 | 63.45 | 65.34 | 58.27 | 76.21 | 74.03 | 71.48 | 65.25 | 0.0022 |
| 43 | LDE225 (NVP-LDE225,Erismodegib) | smoothened | 71.75 | 67.78 | 66.42 | 67.76 | 74.75 | 79.47 | 70.97 | 71.67 | 0.0312 |
| 44 | LDK378 | ALK | 40.91 | 71.54 | 40.08 | 52.30 | 45.02 | 76.56 | 42.00 | 66.80 | 0.0044 |
| 45 | LEE011 | CDK4/6 | 64.46 | 68.06 | 58.82 | 76.17 | 61.15 | 87.17 | 61.48 | 77.13 | 0.18 |
| 46 | Nilotinib (AMN-107) | Bcr-Abl | 56.55 | 57.67 | 55.32 | 56.94 | 49.39 | 62.52 | 53.75 | 59.04 | 0.0001 |
| 47 | Olaparib (AZD2281) | PARP1/2 | 52.88 | 65.03 | 59.36 | 79.15 | 57.27 | 77.26 | 56.50 | 73.81 | 0.0658 |
| 48 | Panobinostat (LBH589) | HDAC | 65.80 | 72.57 | 68.79 | 85.28 | 61.72 | 75.96 | 65.44 | 77.94 | 0.223 |
| 49 | Pazopanib HCl | VEGFR1/2/3, PDGFR, FGFR, c-Kit | 49.69 | 60.19 | 58.62 | 81.79 | 45.25 | 79.23 | 51.18 | 73.74 | 0.0642 |
| 50 | PD 0332991 (Palbociclib HCl) | CDK4/6 | 41.81 | 62.29 | 52.55 | 66.70 | 42.79 | 72.85 | 45.72 | 67.28 | 0.0054 |
| 51 | PF-04449913 | HSP90 | 56.63 | 71.01 | 67.66 | 109.08 | 52.38 | 83.74 | 58.89 | 87.94 | 0.9818 |
| 52 | Sotrastaurin (AEB071) | PKC | 72.33 | 110.89 | 96.21 | 118.09 | 75.36 | 117.47 | 81.30 | 115.48 | 0.6462 |
| 53 | Sunitinib Malate (Sutent) | VEGFR2 and PDGFRβ | 30.35 | 59.15 | 48.48 | 61.27 | 43.38 | 68.56 | 40.74 | 62.99 | 0.0008 |
| 54 | Tandutinib (MLN518) | FLT3, PDGFR, and KIT | 38.86 | 66.33 | 52.07 | 65.61 | 49.69 | 73.96 | 46.88 | 68.63 | 0.0096 |
| 55 | Tivozanib (AV-951) | VEGFR, c-Kit, PDGFR | 56.42 | 80.38 | 53.08 | 56.41 | 59.65 | 75.81 | 56.38 | 70.87 | 0.0232 |
| 56 | Vismodegib (GDC-0449) |
Smoothened homologue (SMO) | 62.85 | 86.17 | 89.86 | 89.25 | 70.88 | 92.06 | 74.53 | 89.16 | 0.992 |
| 57 | PHA-665752 | c-Met inhibitor | N/A | N/A | N/A | N/A | N/A | N/A | N/A | N/A | N/A |
| 58 | Dabrafenib | BRAFV600 | 72.19 | 79.85 | 88.35 | 87.54 | 62.29 | 94.79 | 74.27 | 87.39 | 0.9783 |
| 59 | Regorafenib | VEGFR1/2/3, PDGFRβ, Kit, RET and Raf-1 | 35.18 | 68.49 | 66.17 | 79.01 | 59.54 | 85.13 | 53.63 | 77.54 | 0.201 |
| 60 | Bosutinib | dual Src/Abl | 52.73 | 84.80 | 62.73 | 86.68 | 60.19 | 93.09 | 58.55 | 88.19 | 0.9828 |
| 61 | Carfilzomib | proteasome | 77.84 | 76.12 | 69.89 | 84.25 | 71.24 | 79.79 | 72.99 | 80.05 | 0.3711 |
| 62 | Ruxolitinib | JAK1/2 | 55.32 | 119.28 | 78.83 | 123.65 | 75.30 | 108.41 | 69.82 | 117.11 | 0.4832 |
| 63 | Vandetanib | VEGFR2 | 44.57 | 84.42 | 66.13 | 78.01 | 64.67 | 72.19 | 58.45 | 78.21 | 0.2388 |
| 64 | TMZ | alkylating agent | 48.11 | 113.45 | 92.32 | 118.08 | 73.51 | 103.04 | 71.31 | 111.52 | 0.9624 |
| 65 | Amorolfine | morpholine antifungal drug | 45.15 | 111.07 | 78.28 | 95.52 | 64.67 | 97.78 | 62.70 | 101.46 | 0.9997 |
| 66 | Mevastatin | HMG-CoA reductase inhibitor | 59.74 | 68.48 | 60.21 | 78.15 | 60.06 | 86.09 | 60.00 | 77.57 | 0.2027 |
| 67 | Amiodarone | antiarrhythmic medication | 67.57 | 98.77 | 73.39 | 69.44 | 64.55 | 85.92 | 68.51 | 84.71 | 0.8207 |
| 68 | Fluvastatin Na | anticholesterol agent; HMGCoA inhibitor | 36.69 | 63.96 | 66.91 | 69.80 | 56.38 | 79.94 | 53.33 | 71.23 | 0.0265 |
| 69 | Mycophenolic acid | inosine-5′-monophosphate dehydrogenase inhibitor | 50.11 | 65.49 | 57.27 | 63.37 | 58.64 | 77.28 | 55.34 | 68.71 | 0.0099 |
| 70 | Raloxifene HCl | estrogen receptor inhibitor | 65.00 | 72.15 | 62.60 | 81.25 | 72.44 | 90.00 | 66.68 | 81.13 | 0.4663 |
| 71 | Astemizole | histamine receptor ligand | 56.49 | 69.10 | 59.70 | 67.00 | 77.90 | 81.21 | 64.69 | 72.44 | 0.0412 |
| 72 | Fenretinide | retinoic acid receptor ligand | 70.80 | 74.34 | 49.86 | 62.30 | 87.74 | 89.79 | 69.47 | 75.48 | 0.1116 |