Table 2.
High-Throughput Drug Screening of LPS PDCs.
| Drug | Target | IC50 (nmol/l) |
||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| 11GS_013 | 11GS_018 | 11GS_079 | 11GS_099 | 11GS_106 | 14GS_026 | 14GS_032 | 14GS_035 | 14GS_076 | 14GS_078 | LPS224 | LPS246 | FDA | ||
| Imatinib (Gleevec) | BCR/ABL | >20,000 | 7246 | 10,160 | 6693 | 7741 | 7247 | - | 9347 | 12,840 | 14,270 | 8141 | 11,310 | o |
| Dasatinib (BMS-354825) | BCR/ABL | 35 | - | - | - | - | - | - | 19 | 47 | 25 | 2798 | 5749 | o |
| Nilotinib (AMN-107) | BCR/ABL | 3089 | 2559 | 979 | 1977 | 2709 | 3018 | 2196 | 2506 | 1764 | 2250 | 2018 | 2300 | o |
| Sunitinib Malate (Sutent) | BCR/ABL | 2079 | 1277 | 1241 | 1017 | 1037 | 468 | 767 | 1564 | 2737 | 2356 | 1851 | 1230 | o |
| PD 0332991 (Palbociclib) | CDK4/6 | 6812 | 2866 | 598 | - | 2885 | 308 | 6939 | - | 8389 | - | 5146 | 4395 | o |
| LY2835219 | CDK4/6 | 1566 | 470 | 2720 | 2551 | 131 | 231 | 552 | 621 | 2148 | - | 444 | 171 | o |
| LEE011 | CDK4/6 | - | >20,000 | 119 | 170 | 11,250 | - | - | 438 | - | - | 25 | 1078 | x |
| BKM120 (NVP-BKM120) | PI3 | 1404 | 458 | 294 | 363 | 451 | 241 | 420 | 318 | 235 | 747 | 413 | 559 | x |
| AZD2014 | mTOR | 169 | 158 | 27 | 135 | 117 | 66 | 49 | 105 | 106 | 193 | 130 | 63 | x |
| Everolimus (RAD001) | mTOR | - | 7964 | 354 | 8513 | 1414 | 11,310 | 49 | - | 10,010 | - | - | 2258 | o |
| PF-05212384 (PKI-587) | PI3K & mTOR | 11 | 93 | 196 | 790 | 0 | - | - | 2 | - | 10 | 27 | 24 | x |
| BEZ235 | PI3K & mTOR | - | 5 | 12 | 46 | - | 11 | - | 21 | 1 | 14 | 48 | 32 | x |
| Bortezomib (Velcade) | Proteasome | - | - | - | 2 | 11 | - | 11 | - | - | 9 | - | 7 | o |
| Panobinostat (LBH589) | HDAC | 36 | 18 | 17 | 10 | 22 | 31 | 19 | 15 | 27 | 23 | 14 | 2 | o |
| Cabozantinib (XL184) | VEGFR2 | 2141 | 1429 | 2450 | 1131 | 5838 | 4310 | 2424 | 8892 | 1861 | 7233 | 1426 | 2190 | o |
| Crizotinib (PF-02341066) | c-Met,ALK | 3223 | 2538 | 761 | 766 | 1576 | 1539 | 641 | 3122 | 4897 | 2307 | 918 | 1042 | o |
| vandetanib | VEGFR | 7030 | 3966 | 3616 | 2233 | 2385 | 1756 | 2315 | 3207 | 6449 | 5667 | 2205 | 2430 | o |
| Axitinib | VEGFR1,FLT1 | 1178 | 935 | 462 | 433 | 888 | 1296 | - | 1372 | 1235 | 871 | 809 | 483 | o |
| Foretinib (XL880) | c-MET,KDR | 249 | 256 | 341 | 198 | 368 | 556 | 258 | 775 | 1220 | 357 | 137 | 162 | x |
| regorafenib | VEGFR,c-KIT | 3114 | 7626 | 3185 | - | 9472 | - | - | 6828 | 8788 | 5952 | 5790 | 4536 | o |
| Trametinib | MEK1 | 19 | 155 | 3 | 98 | 5 | 18 | 98 | - | 16,370 | 49 | 99 | 64 | o |
| Pazopanib HCl | VEGFR, PDGFR, FGFR, c-Kit | 4769 | 1061 | 2194 | 4126 | 2762 | 6415 | 1947 | 6142 | 3982 | 1976 | 2234 | 1438 | o |
| Dovitinib (TKI-258) | c-Kit,VEGFR, FGFR | 214 | 232 | 1103 | 431 | 298 | 668 | 282 | 822 | 1356 | 177 | 303 | 196 | x |
| Erlotinib HCl | EGFR | >20,000 | 2721 | 955 | 2908 | 2341 | 4795 | - | 6296 | - | - | 9910 | 16,080 | o |
| Afatinib (BIBW2992) | EGFR,HER2 | - | 717 | 784 | 891 | 1170 | 1120 | 580 | 1212 | 2006 | 1765 | 1501 | 1283 | o |
| Gefitinib (Iressa) | EGFR | 42,640 | - | 6271 | 6827 | 8518 | 6963 | - | - | 12,730 | - | 8899 | 11,050 | o |
| Neratinib (HKI-272) | HER2 & EGFR | 1848 | 441 | 100 | 448 | 776 | 200 | 181 | 780 | 1573 | 193 | 548 | 524 | x |
| vemurafenib | BRAF | >20,000 | 10,160 | 5945 | 19,130 | 12,250 | 11,130 | 9782 | 17,880 | 13,430 | 12,550 | >20,000 | 16,310 | o |