Table 1. US FDA approved anticancer agents - Activity in the NCI60 panel.
Mean drug sensitivity across all cell lines.
Mean GI50, TGI and LC50 values across all cell lines in the NCI60 were calculated as described in the text. Data are presented as the concentration in μM producing 50% growth inhibition (GI50), total growth inhibition (TGI) and 50% lethality (LC50). These values were determined using the optimal concentration range(s) for each endpoint.
| Potency in mM | ||||
|---|---|---|---|---|
| Name | NSC # | Mean GI50 | Mean TGI | Mean LC50 |
| Signaling agents | ||||
| Bortezomib | 681239 | 0.00051 | 0.0063 | 3.6 |
| Dasatinib | 732517 | 0.33 | 8.9 | 51 |
| Erlotinib | 718781 | 5.5 | 59 | >90 |
| Everolimus | 733504 | 0.095 | 14 | 56 |
| Gefitinib | 715055 | 3.2 | 19 | 49 |
| Imatinib | 743414 | 15 | 43 | 81 |
| Lapatinib | 745750 | 2.9 | 20 | 61 |
| Nilotinib | 747599 | 2.9 | 13 | 49 |
| Sorafenib | 747971 | 1.9 | 6 | 30 |
| Sunitinib | 750690 | 2.2 | 9.6 | 31 |
| Temsirolimus | 683864 | 0.038 | 51 | >100 |
| DNA damaging agents | ||||
| Actinomycin D | 3053 | 0.0014 | 0.058 | 0.52 |
| BCNU (Carmustine) | 409962 | 65 | 170 | 330 |
| Bendamustine | 138783 | 60 | >100 | >100 |
| Bleomycin | 125066 | 1.3 | 12 | 23 |
| Busulfan | 750 | 210 | 970 | >1000 |
| Carboplatin | 241240 | 100 | >220 | >240 |
| CCNU (Lomustine) | 79037 | 36 | 120 | 310 |
| Chlorambucil | 3088 | 52 | 260 | 580 |
| Cisplatin | 119875 | 1.4 | 32 | >420 |
| Cyclophosphamide | 26271 | 210 | >250 | >250 |
| Dacarbazine | 45388 | 55 | >800 | >1000 |
| Hexamethylmelamine | 13875 | 140 | >150 | >150 |
| Ifosfamide | 109724 | 320 | >440 | >475 |
| Melphalan | 8806 | 27 | 110 | 210 |
| Methoxsalen | 45923 | 96 | >100 | >100 |
| Mitomycin C | 26980 | 0.71 | 6.6 | 18 |
| Mithramycin | 24559 | 0.013 | 0.65 | 200 |
| Nitrogen mustard | 762 | 2.8 | 19 | 100 |
| Oxaliplatin | 266046 | 2.8 | 52 | >90 |
| Pipobroman | 25154 | 64 | 210 | 370 |
| Procarbazine | 77213 | 440 | >470 | >500 |
| Quinacrine | 14229 | 1.7 | 5.2 | 19 |
| Streptozotocin | 85998 | 570 | >650 | >700 |
| Temozolomide | 362856 | 97 | >100 | >100 |
| ThioTEPA | 6396 | 70 | 400 | 770 |
| Triethylenemelamine | 9706 | 8.7 | 33 | 75 |
| Uracil mustard | 34462 | 24 | 160 | >410 |
| Tubulin-directed agents | ||||
| Docetaxel | 628503 | 0.014 | 12 | >85 |
| Ixabepilone | 747973 | <0.00001 | <0.00001 | <0.00001 |
| Paclitaxel | 125973 | 0.025 | 3.9 | 75 |
| Vinblastine | 49842 | 0.00001 | 0.28 | 32 |
| Vincristine | 67574 | 0.0045 | 13 | 250 |
| Vinorelbine | 608210 | 0.018 | 4.2 | 52 |
| Anthracyclines/Topoisomerase poisons | ||||
| Daunorubicin | 82151 | 0.068 | 1.1 | 10 |
| Doxorubicin | 123127 | 0.097 | 2.1 | 13 |
| Epirubicin | 256942 | 0.2 | 2.7 | 27 |
| Etoposide | 141540 | 6.6 | 50 | 420 |
| Idarubicin | 256439 | 0.038 | 0.25 | 3.8 |
| Irinotecan | 616348 | 14 | 58 | >100 |
| Mitoxantrone | 301739 | 0.059 | 0.88 | 7.8 |
| Teniposide | 122819 | 0.41 | 4.6 | 20 |
| Topotecan | 609699 | 0.031 | 2.5 | 43 |
| Valrubicin | 246131 | 0.49 | 6 | 41 |
| Antimetabolites/Nucleosides | ||||
| 5-azacytidine | 102816 | 0.95 | 8.7 | 350 |
| 5-fluorouracil | 19893 | 18 | 1600 | >2400 |
| 6-Mercaptopurine | 755 | 7.4 | 540 | >740 |
| Allopurinol | 1390 | 430 | 4200 | >5000 |
| Calcium leucovorin | 3590 | 93 | >100 | >100 |
| Capcitebine | 712807 | 80 | >10000 | >10000 |
| Cladribine | 105014 | 5.1 | 55 | >100 |
| Clofarabine | 606869 | 0.42 | 25 | 86 |
| Cytarabine | 63878 | 8.2 | 340 | >500 |
| Decitabine | 127716 | 37 | 260 | 350 |
| Floxuridine | 27640 | 0.39 | 755 | >2400 |
| Fludarabine | 312887 | 43 | 410 | >1100 |
| Gemcitabine | 613327 | 0.24 | 18 | 78 |
| Hydroxyurea | 32065 | 560 | >2000 | >2400 |
| Methotrexate | 740 | 0.3 | 210 | >250 |
| Nelarabine | 686673 | 2700 | >5000 | >5000 |
| Pemetrexed | 698037 | 11 | >100 | >100 |
| Pentostatin | 218321 | 440 | >480 | >500 |
| Thioguanine | 752 | 1.3 | 47 | 210 |
| Hormonal agents | ||||
| Anastrozole | 719344 | 2500 | >9000 | >10000 |
| Delta-1-testololactone | 23759 | 420 | >500 | >500 |
| Dimethyltestosterone | 88536 | 27 | >80 | >100 |
| Dromostanolone propionate | 12198 | 29 | 86 | >100 |
| Estramustine | 702294 | 42 | 85 | >100 |
| Ethinyl estradiol | 10973 | 25 | 78 | >100 |
| Exemestane | 713563 | 25 | 68 | >100 |
| Fulvestrant | 719276 | 62 | >100 | >100 |
| Letrozole | 719345 | 3400 | >5000 | >5000 |
| Megestrol acetate | 71423 | 64 | >100 | >100 |
| Mitotane | 38721 | 14 | 37 | 73 |
| Naldrolone | 23162 | 18 | 45 | 83 |
| Raloxifene | 747974 | 8.1 | 28 | 71 |
| Tamoxifen | 180973 | 4.6 | 18 | 23 |
| Toremifene | 613680 | 13 | 29 | 59 |
| Other | ||||
| Amifostine | 296961 | 540 | >700 | >750 |
| Aminolevulinic acid | 18509 | >100 | >100 | >100 |
| Arsenic trioxide | 706363 | 4.5 | >10 | >13 |
| Celecoxib | 719627 | 17 | 34 | 63 |
| Dexrazoxane | 169780 | 160 | 970 | >2000 |
| Imiquimod | 369100 | 43 | >100 | >100 |
| Lenalidomide | 747972 | >100 | >100 | >100 |
| Levamisole | 177023 | >100 | >100 | >100 |
| Mesna | 113891 | 98 | >100 | >100 |
| Nefinavir | 747167 | 5.2 | 20 | 68 |
| Nelfinavir mesylate | 722664 | 3.9 | 16 | 63 |
| Romidepsin | 630176 | 0.00025 | 0.0081 | 0.038 |
| Thalidomide | 66847 | >100 | >100 | >100 |
| Tretinoin (ATRA) | 122758 | 51 | 78 | >100 |
| Vorinostat | 701852 | 0.94 | 17 | 70 |
| Zoledronic acid | 721517 | 64 | >100 | >100 |