Table S1. b. The COMBO plate Handout

(presently listed as Plate number 3948)

NCI COMBO plate Compounds approved by FDA (for any indication) are highlighted in pink. Information from http://www.accessdata.fda.gov/scripts/cder/drugsatfda/ Compounds tested in clinical trials (for any indication) are highlighted in orange. Date is the most recent publication found searching pubmed or Google for clinical trials with this agent. Compounds are supplied as 20 microL at the given concentration (approx. 500x the conc. of the GI50 of the least sensitive line in the NCI60) Some compounds were not soluble at the desired conc., these are highlighted in yellow, with the actual conc. plated shown Mechanisms given are from published reports. Some compounds may have additional activities. NCI-DTP has not verified mechanism for any of the compounds.

WELL A1 A2 A3 A4 A5 A6 A7 A8 A9 A10 A11 A12 NSC BLANK 332598 89671 681228 56410 289487 166454 312887 169091 65690 129943 BLANK NAME Rhizoxin Brefeldin A Velcade analog Porfiromycin Asterriquinone Dequalinium Fludarabine phosphateMethdilazine Agaric Acid ICRF 159 (Razoxane) milliM 0.005 mM 0.05 mM 0.5 mM 5mM 5mM 3 mM 50 mM 50 mM 50 mM 200 mM MECHANISM Tubulin Arf-GEF Proteasome Alkyl Intercalater Ion channel Nucleoside analog Antihistamine GAPDH; adenine nucleotideTopo II translocase catalytic CLINICAL STATUS Clinical trials (2000) analog of approved agentClinical trials (1997) Clinical trials (2002) FDA approved FDA approved Clinical trials (2000) WELL B1 B2 B3 B4 B5 B6 B7 B8 B9 B10 B11 B12 NSC BLANK 153858 757 521777 63878 102816 77037 3088 324368 657799 85998 BLANK NAME Maytansine Colchicine Curcurbitacin I ara-C (CYTARABINE) 5-azacytidine Tetrandrine Chlorambucil Alkyl lysophospholipid Verapamil Streptozocin milliM 0.005 mM 0.05 mM 0.5 mM 5mM 12.5 mM 25 mM 40 mM 3 mM 50 mM 250 mM MECHANISM Tubulin Tubulin Actin Antimetabolite DNA methylation MDR-reversing agent Alkyl Cell membrane Ion channel Methylating agent CLINICAL STATUS Clinical trials (1985) FDA approved FDA approved FDA approved Clinical trials (1999) FDA approved FDA approved FDA approved WELL C1 C2 C3 C4 C5 C6 C7 C8 C9 C10 C11 C12 NSC BLANK 58514 82151 330500 246131 180973 221019 141538 365793 638080 1026 BLANK NAME Chromomycin A3 Daunorubicin Macbecin II Valrubicin Tamoxifen Wortmannin Ovalicin Perezone Herbimycin analog Cycloleucine milliM 0.005 mM 0.05 mM 2.5 mM 5mM 12.5 mM 50 mM 50 mM 50 mM 50 mM 1 mM MECHANISM DNA binding Topo II Hsp90 Topo II Anti-estrogen PI3K Methionine aminopeptidase-2Mitochondrial Ca++ potential Hsp90 NMDA receptor CLINICAL STATUS Clinical trials (1975) FDA approved FDA approved FDA approved Clinical trials (1983) WELL D1 D2 D3 D4 D5 D6 D7 D8 D9 D10 D11 D12 NSC BLANK 526417 67574 119875 141540 308847 106193 170984 4060 95090 109724 BLANK NAME Echinomycin Vincristine sulfate Cisplatin Etoposide Amonafide Fusarubin Pimozide Ursolic acid Ergotamine Iphosphamide milliM 0.005 mM 0.05 mM 2.5 mM 5mM 12.5 mM 50 mM 50 mM 21 mM 50 mM Alkyl MECHANISM DNA binding Tubulin Alkyl Topo II Topo II Redox Dopamine receptor Pol beta; TGF beta Vasoconstriction; possible phosphodiesterase CLINICAL STATUS Clinical trials (1998) FDA approved FDA approved FDA approved Clinical trials (2002) FDA approved FDA approved FDA approved WELL E1 E2 E3 E4 E5 E6 E7 E8 E9 E10 E11 E12 NSC BLANK 122023 89201 122819 639366 126771 85236 3590 408120 719627 32065 BLANK NAME Valinomycin Estramustine Teniposide Dichlorallyl lawsone Helenalin Calcium leucovorin Emodin Celecoxib Hydroxyurea milliM 0.005 mM 0.05 mM 2.5 mM 5mM 12.5 mM 50 mM 3 mM 50 mM 50 mM 250 mM MECHANISM Ionophore Tubulin Topo II Angiogenesis Dihydroorotate dehydrogenaseNF-kappaB inhibitor Antifol antidote Tyr kinase COX2 RNR CLINICAL STATUS FDA approved FDA approved FDA approved FDA approved FDA approved WELL F1 F2 F3 F4 F5 F6 F7 F8 F9 F10 F11 F12 NSC BLANK 325319 740 368390 705701 92859 314622 58368 4644 362856 BLANK BLANK NAME Didemnin B Methotrexate Brequinar Alsterpaullone Arsenic Trioxide Topo1A Fumagillin dicyclohexylamineBetulin salt Temozolomide milliM 0.005 mM 0.5 mM 2.5 mM 5mM 1 mM 0.5 mM 5 mM 20 mM 50 mM MECHANISM elongation factor eEF1A,Antifolate protein palmitoyl thioesteraseDihydroorotate 1 dehydrogenaseCDK Reactive oxygen? Topo I Angiogenesis possible kinase Alkyl CLINICAL STATUS Clinical trials (2000) FDA approved Clinical trials (1998) FDA approved Clinical trials (2002) FDA approved WELL G1 G2 G3 G4 G5 G6 G7 G8 G9 G10 G11 G12 NSC BLANK 3053 123127 752 680410 125066 32982 11905 106997 8661 BLANK BLANK NAME Actinomycin D ( DACTINOMYCIN,Doxorubicin (Adriamycin) COSMEGEN)Thioguanine Adaphostin Bleomycin Curcumin Lapachol Lipoxamycin Brasilin milliM 0.005 mM 0.5 mM 2.5 mM 5mM 9 mM 50 mM 50 mM 30 mM 50 mM MECHANISM Transcription inhib Topo II Antimetabolite BCR-Abl kinase DNA breaks Antioxidant; NF-kappaBDihydroorotate dehydrogenaseSerine palmitoyl-transferaseKinase CLINICAL STATUS FDA approved FDA approved FDA approved FDA approved Clinical trials (2002) Clinical trials (1974) WELL H1 H2 H3 H4 H5 H6 H7 H8 H9 H10 H11 H12 NSC BLANK 125973 301739 226080 227279 19893 169434 5355 118343 409962 BLANK BLANK NAME Paclitaxel (Taxol) Mitoxantrone Rapamycin ( SIROLIMUS)Juglone analog 5-fluorouracil Miconazole Berberine sulfate Radicinin BCNU milliM 0.05 mM 0.5 mM 5mM 5mM 25 mM 50 mM 10 mM 50 mM 250 mM MECHANISM Tubulin Topo II mTOR possible PIN1 prolyl isomeraseNucleoside analog Aromatase Telomerase Protease Alkyl CLINICAL STATUS FDA approved FDA approved FDA approved FDA approved FDA approved Clinical trials (2003) FDA approved