solo per uso di ricerca
BI 2536 inibitore di PLK1/BRD4
N. Cat.: S1109
Struttura chimica
Peso molecolare: 521.66
Vai a
Controllo Qualità (Quality Control)
Lotto:
Purezza:
99.88%
99.88
Coltura cellulare, trattamento e concentrazione di lavoro
(Cell Culture, Treatment & Working Concentration)
| Linee cellulari | Tipo di saggio | Concentrazione | Tempo di incubazione | Formulazione | Descrizione dell'attività | PMID |
|---|---|---|---|---|---|---|
| PSN1 | Growth Inhibition Assay | IC50=0.00776 μM | SANGER | |||
| ACN | Growth Inhibition Assay | IC50=0.00843 μM | SANGER | |||
| TE-8 | Growth Inhibition Assay | IC50=0.00941 μM | SANGER | |||
| LC-2-ad | Growth Inhibition Assay | IC50=0.01093 μM | SANGER | |||
| ALL-PO | Growth Inhibition Assay | IC50=0.013 μM | SANGER | |||
| EW-16 | Growth Inhibition Assay | IC50=0.01336 μM | SANGER | |||
| KM12 | Growth Inhibition Assay | IC50=0.01348 μM | SANGER | |||
| GI-1 | Growth Inhibition Assay | IC50=0.01383 μM | SANGER | |||
| LS-411N | Growth Inhibition Assay | IC50=0.01407 μM | SANGER | |||
| ES8 | Growth Inhibition Assay | IC50=0.01494 μM | SANGER | |||
| SNU-C2B | Growth Inhibition Assay | IC50=0.01526 μM | SANGER | |||
| CESS | Growth Inhibition Assay | IC50=0.01602 μM | SANGER | |||
| 697 | Growth Inhibition Assay | IC50=0.01668 μM | SANGER | |||
| NCI-H1963 | Growth Inhibition Assay | IC50=0.01673 μM | SANGER | |||
| IA-LM | Growth Inhibition Assay | IC50=0.01688 μM | SANGER | |||
| SW954 | Growth Inhibition Assay | IC50=0.01705 μM | SANGER | |||
| RL95-2 | Growth Inhibition Assay | IC50=0.01738 μM | SANGER | |||
| LXF-289 | Growth Inhibition Assay | IC50=0.0177 μM | SANGER | |||
| OCUB-M | Growth Inhibition Assay | IC50=0.01826 μM | SANGER | |||
| RKO | Growth Inhibition Assay | IC50=0.01987 μM | SANGER | |||
| LOUCY | Growth Inhibition Assay | IC50=0.0205 μM | SANGER | |||
| NOS-1 | Growth Inhibition Assay | IC50=0.02093 μM | SANGER | |||
| A4-Fuk | Growth Inhibition Assay | IC50=0.02218 μM | SANGER | |||
| A388 | Growth Inhibition Assay | IC50=0.02227 μM | SANGER | |||
| TE-9 | Growth Inhibition Assay | IC50=0.02261 μM | SANGER | |||
| KURAMOCHI | Growth Inhibition Assay | IC50=0.02285 μM | SANGER | |||
| KALS-1 | Growth Inhibition Assay | IC50=0.02338 μM | SANGER | |||
| HOP-62 | Growth Inhibition Assay | IC50=0.0242 μM | SANGER | |||
| RPMI-8402 | Growth Inhibition Assay | IC50=0.02508 μM | SANGER | |||
| TE-1 | Growth Inhibition Assay | IC50=0.02512 μM | SANGER | |||
| CCRF-CEM | Growth Inhibition Assay | IC50=0.02543 μM | SANGER | |||
| HUTU-80 | Growth Inhibition Assay | IC50=0.02624 μM | SANGER | |||
| NCI-H1648 | Growth Inhibition Assay | IC50=0.02647 μM | SANGER | |||
| HCE-4 | Growth Inhibition Assay | IC50=0.02682 μM | SANGER | |||
| ETK-1 | Growth Inhibition Assay | IC50=0.02736 μM | SANGER | |||
| TE-15 | Growth Inhibition Assay | IC50=0.02738 μM | SANGER | |||
| BE-13 | Growth Inhibition Assay | IC50=0.0274 μM | SANGER | |||
| KE-37 | Growth Inhibition Assay | IC50=0.02741 μM | SANGER | |||
| NCI-H1355 | Growth Inhibition Assay | IC50=0.02783 μM | SANGER | |||
| TE-11 | Growth Inhibition Assay | IC50=0.02809 μM | SANGER | |||
| BL-70 | Growth Inhibition Assay | IC50=0.02857 μM | SANGER | |||
| ES6 | Growth Inhibition Assay | IC50=0.02881 μM | SANGER | |||
| GT3TKB | Growth Inhibition Assay | IC50=0.02953 μM | SANGER | |||
| LB647-SCLC | Growth Inhibition Assay | IC50=0.03195 μM | SANGER | |||
| NB13 | Growth Inhibition Assay | IC50=0.03316 μM | SANGER | |||
| ST486 | Growth Inhibition Assay | IC50=0.03337 μM | SANGER | |||
| NCI-H82 | Growth Inhibition Assay | IC50=0.03343 μM | SANGER | |||
| NTERA-S-cl-D1 | Growth Inhibition Assay | IC50=0.03399 μM | SANGER | |||
| ES4 | Growth Inhibition Assay | IC50=0.03463 μM | SANGER | |||
| SK-NEP-1 | Growth Inhibition Assay | IC50=0.03499 μM | SANGER | |||
| Becker | Growth Inhibition Assay | IC50=0.03555 μM | SANGER | |||
| A101D | Growth Inhibition Assay | IC50=0.03748 μM | SANGER | |||
| SK-UT-1 | Growth Inhibition Assay | IC50=0.03774 μM | SANGER | |||
| SW982 | Growth Inhibition Assay | IC50=0.0379 μM | SANGER | |||
| TE-10 | Growth Inhibition Assay | IC50=0.04046 μM | SANGER | |||
| OVCAR-4 | Growth Inhibition Assay | IC50=0.04059 μM | SANGER | |||
| KP-N-YS | Growth Inhibition Assay | IC50=0.04085 μM | SANGER | |||
| BL-41 | Growth Inhibition Assay | IC50=0.04125 μM | SANGER | |||
| MZ1-PC | Growth Inhibition Assay | IC50=0.04127 μM | SANGER | |||
| PF-382 | Growth Inhibition Assay | IC50=0.04198 μM | SANGER | |||
| MOLT-13 | Growth Inhibition Assay | IC50=0.04238 μM | SANGER | |||
| HCC1599 | Growth Inhibition Assay | IC50=0.04258 μM | SANGER | |||
| IST-MEL1 | Growth Inhibition Assay | IC50=0.04442 μM | SANGER | |||
| LU-139 | Growth Inhibition Assay | IC50=0.04442 μM | SANGER | |||
| MS-1 | Growth Inhibition Assay | IC50=0.04701 μM | SANGER | |||
| MFH-ino | Growth Inhibition Assay | IC50=0.05003 μM | SANGER | |||
| IMR-5 | Growth Inhibition Assay | IC50=0.05021 μM | SANGER | |||
| TE-5 | Growth Inhibition Assay | IC50=0.05063 μM | SANGER | |||
| DJM-1 | Growth Inhibition Assay | IC50=0.05142 μM | SANGER | |||
| NB17 | Growth Inhibition Assay | IC50=0.05207 μM | SANGER | |||
| KARPAS-45 | Growth Inhibition Assay | IC50=0.05358 μM | SANGER | |||
| TGBC1TKB | Growth Inhibition Assay | IC50=0.05405 μM | SANGER | |||
| ML-2 | Growth Inhibition Assay | IC50=0.05414 μM | SANGER | |||
| no-10 | Growth Inhibition Assay | IC50=0.05474 μM | SANGER | |||
| CTV-1 | Growth Inhibition Assay | IC50=0.05502 μM | SANGER | |||
| SJSA-1 | Growth Inhibition Assay | IC50=0.0552 μM | SANGER | |||
| HC-1 | Growth Inhibition Assay | IC50=0.05597 μM | SANGER | |||
| TE-12 | Growth Inhibition Assay | IC50=0.05613 μM | SANGER | |||
| KY821 | Growth Inhibition Assay | IC50=0.05632 μM | SANGER | |||
| TALL-1 | Growth Inhibition Assay | IC50=0.05708 μM | SANGER | |||
| DEL | Growth Inhibition Assay | IC50=0.05709 μM | SANGER | |||
| TE-6 | Growth Inhibition Assay | IC50=0.05722 μM | SANGER | |||
| SK-LMS-1 | Growth Inhibition Assay | IC50=0.05805 μM | SANGER | |||
| EW-1 | Growth Inhibition Assay | IC50=0.05837 μM | SANGER | |||
| 8-MG-BA | Growth Inhibition Assay | IC50=0.05851 μM | SANGER | |||
| NALM-6 | Growth Inhibition Assay | IC50=0.05973 μM | SANGER | |||
| LB771-HNC | Growth Inhibition Assay | IC50=0.05979 μM | SANGER | |||
| HT-144 | Growth Inhibition Assay | IC50=0.0613 μM | SANGER | |||
| KM-H2 | Growth Inhibition Assay | IC50=0.06221 μM | SANGER | |||
| SF268 | Growth Inhibition Assay | IC50=0.06286 μM | SANGER | |||
| RS4-11 | Growth Inhibition Assay | IC50=0.06304 μM | SANGER | |||
| MHH-PREB-1 | Growth Inhibition Assay | IC50=0.06319 μM | SANGER | |||
| ATN-1 | Growth Inhibition Assay | IC50=0.06345 μM | SANGER | |||
| BB30-HNC | Growth Inhibition Assay | IC50=0.06436 μM | SANGER | |||
| CPC-N | Growth Inhibition Assay | IC50=0.06524 μM | SANGER | |||
| NB1 | Growth Inhibition Assay | IC50=0.06613 μM | SANGER | |||
| KS-1 | Growth Inhibition Assay | IC50=0.06748 μM | SANGER | |||
| RXF393 | Growth Inhibition Assay | IC50=0.06764 μM | SANGER | |||
| IST-SL2 | Growth Inhibition Assay | IC50=0.07004 μM | SANGER | |||
| GI-ME-N | Growth Inhibition Assay | IC50=0.07286 μM | SANGER | |||
| VA-ES-BJ | Growth Inhibition Assay | IC50=0.07475 μM | SANGER | |||
| NCI-H1581 | Growth Inhibition Assay | IC50=0.07478 μM | SANGER | |||
| U-266 | Growth Inhibition Assay | IC50=0.07497 μM | SANGER | |||
| DMS-114 | Growth Inhibition Assay | IC50=0.07528 μM | SANGER | |||
| NCI-H187 | Growth Inhibition Assay | IC50=0.07726 μM | SANGER | |||
| SW962 | Growth Inhibition Assay | IC50=0.07839 μM | SANGER | |||
| MONO-MAC-6 | Growth Inhibition Assay | IC50=0.07986 μM | SANGER | |||
| MOLT-16 | Growth Inhibition Assay | IC50=0.08121 μM | SANGER | |||
| KNS-42 | Growth Inhibition Assay | IC50=0.08161 μM | SANGER | |||
| CMK | Growth Inhibition Assay | IC50=0.08225 μM | SANGER | |||
| Ramos-2G6-4C10 | Growth Inhibition Assay | IC50=0.08225 μM | SANGER | |||
| Daudi | Growth Inhibition Assay | IC50=0.08256 μM | SANGER | |||
| NCI-H510A | Growth Inhibition Assay | IC50=0.08336 μM | SANGER | |||
| LB831-BLC | Growth Inhibition Assay | IC50=0.08561 μM | SANGER | |||
| HEL | Growth Inhibition Assay | IC50=0.08668 μM | SANGER | |||
| LU-134-A | Growth Inhibition Assay | IC50=0.08708 μM | SANGER | |||
| NCI-H1694 | Growth Inhibition Assay | IC50=0.08744 μM | SANGER | |||
| KGN | Growth Inhibition Assay | IC50=0.08759 μM | SANGER | |||
| A253 | Growth Inhibition Assay | IC50=0.08822 μM | SANGER | |||
| DG-75 | Growth Inhibition Assay | IC50=0.08922 μM | SANGER | |||
| MOLT-4 | Growth Inhibition Assay | IC50=0.08983 μM | SANGER | |||
| NCI-SNU-5 | Growth Inhibition Assay | IC50=0.09258 μM | SANGER | |||
| ONS-76 | Growth Inhibition Assay | IC50=0.09276 μM | SANGER | |||
| NCI-H446 | Growth Inhibition Assay | IC50=0.09462 μM | SANGER | |||
| COR-L279 | Growth Inhibition Assay | IC50=0.09556 μM | SANGER | |||
| Calu-6 | Growth Inhibition Assay | IC50=0.09598 μM | SANGER | |||
| BC-3 | Growth Inhibition Assay | IC50=0.09662 μM | SANGER | |||
| NCI-H2126 | Growth Inhibition Assay | IC50=0.09791 μM | SANGER | |||
| NCI-H1882 | Growth Inhibition Assay | IC50=0.09809 μM | SANGER | |||
| BB65-RCC | Growth Inhibition Assay | IC50=0.10294 μM | SANGER | |||
| DU-4475 | Growth Inhibition Assay | IC50=0.10407 μM | SANGER | |||
| NCI-H526 | Growth Inhibition Assay | IC50=0.1044 μM | SANGER | |||
| NEC8 | Growth Inhibition Assay | IC50=0.10525 μM | SANGER | |||
| NCI-H1304 | Growth Inhibition Assay | IC50=0.10594 μM | SANGER | |||
| L-540 | Growth Inhibition Assay | IC50=0.10708 μM | SANGER | |||
| NCI-SNU-16 | Growth Inhibition Assay | IC50=0.10742 μM | SANGER | |||
| HD-MY-Z | Growth Inhibition Assay | IC50=0.10856 μM | SANGER | |||
| K-562 | Growth Inhibition Assay | IC50=0.10858 μM | SANGER | |||
| JAR | Growth Inhibition Assay | IC50=0.10925 μM | SANGER | |||
| MZ2-MEL | Growth Inhibition Assay | IC50=0.1105 μM | SANGER | |||
| L-363 | Growth Inhibition Assay | IC50=0.11079 μM | SANGER | |||
| BV-173 | Growth Inhibition Assay | IC50=0.11243 μM | SANGER | |||
| NCI-H524 | Growth Inhibition Assay | IC50=0.11274 μM | SANGER | |||
| EoL-1-cell | Growth Inhibition Assay | IC50=0.11672 μM | SANGER | |||
| K052 | Growth Inhibition Assay | IC50=0.11712 μM | SANGER | |||
| TK10 | Growth Inhibition Assay | IC50=0.11728 μM | SANGER | |||
| KU812 | Growth Inhibition Assay | IC50=0.12044 μM | SANGER | |||
| RPMI-8226 | Growth Inhibition Assay | IC50=0.12052 μM | SANGER | |||
| MZ7-mel | Growth Inhibition Assay | IC50=0.12237 μM | SANGER | |||
| SK-PN-DW | Growth Inhibition Assay | IC50=0.12287 μM | SANGER | |||
| SR | Growth Inhibition Assay | IC50=0.12441 μM | SANGER | |||
| RPMI-6666 | Growth Inhibition Assay | IC50=0.12743 μM | SANGER | |||
| no-11 | Growth Inhibition Assay | IC50=0.12869 μM | SANGER | |||
| EW-3 | Growth Inhibition Assay | IC50=0.12893 μM | SANGER | |||
| LAMA-84 | Growth Inhibition Assay | IC50=0.13187 μM | SANGER | |||
| HT | Growth Inhibition Assay | IC50=0.13574 μM | SANGER | |||
| KP-N-RT-BM-1 | Growth Inhibition Assay | IC50=0.13612 μM | SANGER | |||
| NCI-H747 | Growth Inhibition Assay | IC50=0.137 μM | SANGER | |||
| NCCIT | Growth Inhibition Assay | IC50=0.13939 μM | SANGER | |||
| MLMA | Growth Inhibition Assay | IC50=0.14167 μM | SANGER | |||
| LP-1 | Growth Inhibition Assay | IC50=0.1424 μM | SANGER | |||
| CAL-148 | Growth Inhibition Assay | IC50=0.14483 μM | SANGER | |||
| GB-1 | Growth Inhibition Assay | IC50=0.14526 μM | SANGER | |||
| COR-L88 | Growth Inhibition Assay | IC50=0.14802 μM | SANGER | |||
| NKM-1 | Growth Inhibition Assay | IC50=0.14906 μM | SANGER | |||
| NB5 | Growth Inhibition Assay | IC50=0.15462 μM | SANGER | |||
| SH-4 | Growth Inhibition Assay | IC50=0.15466 μM | SANGER | |||
| EM-2 | Growth Inhibition Assay | IC50=0.15467 μM | SANGER | |||
| TGBC24TKB | Growth Inhibition Assay | IC50=0.15659 μM | SANGER | |||
| SCLC-21H | Growth Inhibition Assay | IC50=0.15702 μM | SANGER | |||
| COLO-684 | Growth Inhibition Assay | IC50=0.15721 μM | SANGER | |||
| KINGS-1 | Growth Inhibition Assay | IC50=0.1591 μM | SANGER | |||
| LS-123 | Growth Inhibition Assay | IC50=0.15917 μM | SANGER | |||
| MC116 | Growth Inhibition Assay | IC50=0.16158 μM | SANGER | |||
| SU-DHL-1 | Growth Inhibition Assay | IC50=0.16206 μM | SANGER | |||
| NCI-H64 | Growth Inhibition Assay | IC50=0.16347 μM | SANGER | |||
| HCE-T | Growth Inhibition Assay | IC50=0.16504 μM | SANGER | |||
| LOXIMVI | Growth Inhibition Assay | IC50=0.16949 μM | SANGER | |||
| ARH-77 | Growth Inhibition Assay | IC50=0.17379 μM | SANGER | |||
| DOHH-2 | Growth Inhibition Assay | IC50=0.17672 μM | SANGER | |||
| COLO-320-HSR | Growth Inhibition Assay | IC50=0.18154 μM | SANGER | |||
| NB6 | Growth Inhibition Assay | IC50=0.18566 μM | SANGER | |||
| L-428 | Growth Inhibition Assay | IC50=0.18813 μM | SANGER | |||
| SNB75 | Growth Inhibition Assay | IC50=0.18824 μM | SANGER | |||
| NCI-H2141 | Growth Inhibition Assay | IC50=0.19011 μM | SANGER | |||
| KARPAS-299 | Growth Inhibition Assay | IC50=0.19241 μM | SANGER | |||
| LC4-1 | Growth Inhibition Assay | IC50=0.19502 μM | SANGER | |||
| UACC-257 | Growth Inhibition Assay | IC50=0.19947 μM | SANGER | |||
| EVSA-T | Growth Inhibition Assay | IC50=0.20312 μM | SANGER | |||
| JiyoyeP-2003 | Growth Inhibition Assay | IC50=0.20477 μM | SANGER | |||
| NCI-H720 | Growth Inhibition Assay | IC50=0.20525 μM | SANGER | |||
| GAK | Growth Inhibition Assay | IC50=0.21189 μM | SANGER | |||
| HH | Growth Inhibition Assay | IC50=0.21405 μM | SANGER | |||
| NCI-H1436 | Growth Inhibition Assay | IC50=0.21464 μM | SANGER | |||
| GR-ST | Growth Inhibition Assay | IC50=0.21488 μM | SANGER | |||
| BC-1 | Growth Inhibition Assay | IC50=0.22616 μM | SANGER | |||
| SIG-M5 | Growth Inhibition Assay | IC50=0.22727 μM | SANGER | |||
| NCI-H345 | Growth Inhibition Assay | IC50=0.23805 μM | SANGER | |||
| OPM-2 | Growth Inhibition Assay | IC50=0.23882 μM | SANGER | |||
| LB1047-RCC | Growth Inhibition Assay | IC50=0.2441 μM | SANGER | |||
| CTB-1 | Growth Inhibition Assay | IC50=0.24493 μM | SANGER | |||
| A3-KAW | Growth Inhibition Assay | IC50=0.25341 μM | SANGER | |||
| SF126 | Growth Inhibition Assay | IC50=0.25383 μM | SANGER | |||
| KARPAS-422 | Growth Inhibition Assay | IC50=0.25435 μM | SANGER | |||
| MEG-01 | Growth Inhibition Assay | IC50=0.25673 μM | SANGER | |||
| NCI-H209 | Growth Inhibition Assay | IC50=0.26374 μM | SANGER | |||
| SBC-1 | Growth Inhibition Assay | IC50=0.265 μM | SANGER | |||
| K5 | Growth Inhibition Assay | IC50=0.26984 μM | SANGER | |||
| QIMR-WIL | Growth Inhibition Assay | IC50=0.27155 μM | SANGER | |||
| NMC-G1 | Growth Inhibition Assay | IC50=0.28217 μM | SANGER | |||
| IST-MES1 | Growth Inhibition Assay | IC50=0.29238 μM | SANGER | |||
| SW684 | Growth Inhibition Assay | IC50=0.30047 μM | SANGER | |||
| MV-4-11 | Growth Inhibition Assay | IC50=0.30788 μM | SANGER | |||
| LAN-6 | Growth Inhibition Assay | IC50=0.31572 μM | SANGER | |||
| RH-1 | Growth Inhibition Assay | IC50=0.31871 μM | SANGER | |||
| CP66-MEL | Growth Inhibition Assay | IC50=0.31878 μM | SANGER | |||
| EC-GI-10 | Growth Inhibition Assay | IC50=0.32987 μM | SANGER | |||
| GDM-1 | Growth Inhibition Assay | IC50=0.33059 μM | SANGER | |||
| IST-SL1 | Growth Inhibition Assay | IC50=0.34914 μM | SANGER | |||
| KMOE-2 | Growth Inhibition Assay | IC50=0.35175 μM | SANGER | |||
| OS-RC-2 | Growth Inhibition Assay | IC50=0.35544 μM | SANGER | |||
| HDLM-2 | Growth Inhibition Assay | IC50=0.37814 μM | SANGER | |||
| DSH1 | Growth Inhibition Assay | IC50=0.38631 μM | SANGER | |||
| LS-1034 | Growth Inhibition Assay | IC50=0.38954 μM | SANGER | |||
| LB373-MEL-D | Growth Inhibition Assay | IC50=0.39197 μM | SANGER | |||
| GOTO | Growth Inhibition Assay | IC50=0.42118 μM | SANGER | |||
| MRK-nu-1 | Growth Inhibition Assay | IC50=0.42205 μM | SANGER | |||
| SK-MM-2 | Growth Inhibition Assay | IC50=0.43442 μM | SANGER | |||
| BOKU | Growth Inhibition Assay | IC50=0.43792 μM | SANGER | |||
| NOMO-1 | Growth Inhibition Assay | IC50=0.4386 μM | SANGER | |||
| J-RT3-T3-5 | Growth Inhibition Assay | IC50=0.44878 μM | SANGER | |||
| COLO-668 | Growth Inhibition Assay | IC50=0.45668 μM | SANGER | |||
| SF539 | Growth Inhibition Assay | IC50=0.48684 μM | SANGER | |||
| LB2518-MEL | Growth Inhibition Assay | IC50=0.49703 μM | SANGER | |||
| TE-441-T | Growth Inhibition Assay | IC50=0.5012 μM | SANGER | |||
| MDA-MB-134-VI | Growth Inhibition Assay | IC50=0.50921 μM | SANGER | |||
| SCC-3 | Growth Inhibition Assay | IC50=0.51873 μM | SANGER | |||
| KLE | Growth Inhibition Assay | IC50=0.52171 μM | SANGER | |||
| LB2241-RCC | Growth Inhibition Assay | IC50=0.52525 μM | SANGER | |||
| NCI-H1417 | Growth Inhibition Assay | IC50=0.53435 μM | SANGER | |||
| NCI-H2081 | Growth Inhibition Assay | IC50=0.58611 μM | SANGER | |||
| NCI-H1522 | Growth Inhibition Assay | IC50=0.59383 μM | SANGER | |||
| NCI-H889 | Growth Inhibition Assay | IC50=0.59844 μM | SANGER | |||
| CGTH-W-1 | Growth Inhibition Assay | IC50=0.60755 μM | SANGER | |||
| EB-3 | Growth Inhibition Assay | IC50=0.61153 μM | SANGER | |||
| D-336MG | Growth Inhibition Assay | IC50=0.61791 μM | SANGER | |||
| LC-1F | Growth Inhibition Assay | IC50=0.62592 μM | SANGER | |||
| MHH-NB-11 | Growth Inhibition Assay | IC50=0.63801 μM | SANGER | |||
| SK-N-FI | Growth Inhibition Assay | IC50=0.6391 μM | SANGER | |||
| NCI-H69 | Growth Inhibition Assay | IC50=0.64879 μM | SANGER | |||
| SCH | Growth Inhibition Assay | IC50=0.66023 μM | SANGER | |||
| LS-513 | Growth Inhibition Assay | IC50=0.67259 μM | SANGER | |||
| CP67-MEL | Growth Inhibition Assay | IC50=0.67596 μM | SANGER | |||
| GCIY | Growth Inhibition Assay | IC50=0.70363 μM | SANGER | |||
| SHP-77 | Growth Inhibition Assay | IC50=0.70734 μM | SANGER | |||
| EHEB | Growth Inhibition Assay | IC50=0.71854 μM | SANGER | |||
| D-247MG | Growth Inhibition Assay | IC50=0.73232 μM | SANGER | |||
| Raji | Growth Inhibition Assay | IC50=0.74989 μM | SANGER | |||
| MPP-89 | Growth Inhibition Assay | IC50=0.75978 μM | SANGER | |||
| EKVX | Growth Inhibition Assay | IC50=0.79073 μM | SANGER | |||
| HCC2218 | Growth Inhibition Assay | IC50=0.79131 μM | SANGER | |||
| KNS-81-FD | Growth Inhibition Assay | IC50=0.81011 μM | SANGER | |||
| HCC2157 | Growth Inhibition Assay | IC50=0.84951 μM | SANGER | |||
| BT-474 | Growth Inhibition Assay | IC50=0.88854 μM | SANGER | |||
| NCI-H748 | Growth Inhibition Assay | IC50=0.912 μM | SANGER | |||
| EW-24 | Growth Inhibition Assay | IC50=0.92002 μM | SANGER | |||
| D-263MG | Growth Inhibition Assay | IC50=0.94512 μM | SANGER | |||
| OMC-1 | Growth Inhibition Assay | IC50=0.96373 μM | SANGER | |||
| NCI-H2196 | Growth Inhibition Assay | IC50=0.97777 μM | SANGER | |||
| HAL-01 | Growth Inhibition Assay | IC50=0.99872 μM | SANGER | |||
| NCI-H2107 | Growth Inhibition Assay | IC50=1.01854 μM | SANGER | |||
| LB996-RCC | Growth Inhibition Assay | IC50=1.08051 μM | SANGER | |||
| NCI-H1395 | Growth Inhibition Assay | IC50=1.1067 μM | SANGER | |||
| CHP-126 | Growth Inhibition Assay | IC50=1.16199 μM | SANGER | |||
| NB69 | Growth Inhibition Assay | IC50=1.26148 μM | SANGER | |||
| CAS-1 | Growth Inhibition Assay | IC50=1.34231 μM | SANGER | |||
| JVM-3 | Growth Inhibition Assay | IC50=1.47855 μM | SANGER | |||
| DMS-153 | Growth Inhibition Assay | IC50=1.57674 μM | SANGER | |||
| SK-MEL-2 | Growth Inhibition Assay | IC50=1.71789 μM | SANGER | |||
| NCI-H1155 | Growth Inhibition Assay | IC50=1.73676 μM | SANGER | |||
| NCI-H1092 | Growth Inhibition Assay | IC50=1.76182 μM | SANGER | |||
| LU-165 | Growth Inhibition Assay | IC50=1.86476 μM | SANGER | |||
| HL-60 | Growth Inhibition Assay | IC50=1.99908 μM | SANGER | |||
| REH | Growth Inhibition Assay | IC50=2.00582 μM | SANGER | |||
| JVM-2 | Growth Inhibition Assay | IC50=2.06135 μM | SANGER | |||
| MN-60 | Growth Inhibition Assay | IC50=2.17308 μM | SANGER | |||
| SCC-15 | Growth Inhibition Assay | IC50=2.2027 μM | SANGER | |||
| SNU-C1 | Growth Inhibition Assay | IC50=2.21343 μM | SANGER | |||
| SK-MEL-1 | Growth Inhibition Assay | IC50=2.32047 μM | SANGER | |||
| TGW | Growth Inhibition Assay | IC50=2.35027 μM | SANGER | |||
| CA46 | Growth Inhibition Assay | IC50=2.75967 μM | SANGER | |||
| NCI-H23 | Growth Inhibition Assay | IC50=2.80791 μM | SANGER | |||
| MMAC-SF | Growth Inhibition Assay | IC50=2.86628 μM | SANGER | |||
| NCI-H2171 | Growth Inhibition Assay | IC50=3.03448 μM | SANGER | |||
| A704 | Growth Inhibition Assay | IC50=3.14194 μM | SANGER | |||
| DB | Growth Inhibition Assay | IC50=3.25576 μM | SANGER | |||
| NCI-H719 | Growth Inhibition Assay | IC50=3.30384 μM | SANGER | |||
| MC-CAR | Growth Inhibition Assay | IC50=3.54817 μM | SANGER | |||
| SIMA | Growth Inhibition Assay | IC50=3.58416 μM | SANGER | |||
| SW872 | Growth Inhibition Assay | IC50=3.78101 μM | SANGER | |||
| HCC1187 | Growth Inhibition Assay | IC50=3.78315 μM | SANGER | |||
| EW-13 | Growth Inhibition Assay | IC50=3.83417 μM | SANGER | |||
| NCI-SNU-1 | Growth Inhibition Assay | IC50=4.21999 μM | SANGER | |||
| NCI-H226 | Growth Inhibition Assay | IC50=4.33606 μM | SANGER | |||
| RPMI-8866 | Growth Inhibition Assay | IC50=4.36029 μM | SANGER | |||
| OCI-AML2 | Growth Inhibition Assay | IC50=4.5523 μM | SANGER | |||
| LU-65 | Growth Inhibition Assay | IC50=4.93033 μM | SANGER | |||
| SK-N-DZ | Growth Inhibition Assay | IC50=5.63465 μM | SANGER | |||
| NB14 | Growth Inhibition Assay | IC50=5.97135 μM | SANGER | |||
| COLO-829 | Growth Inhibition Assay | IC50=6.33359 μM | SANGER | |||
| MHH-CALL-2 | Growth Inhibition Assay | IC50=6.51508 μM | SANGER | |||
| NCI-H1770 | Growth Inhibition Assay | IC50=6.66904 μM | SANGER | |||
| ECC4 | Growth Inhibition Assay | IC50=6.82179 μM | SANGER | |||
| A498 | Growth Inhibition Assay | IC50=6.87192 μM | SANGER | |||
| DMS-79 | Growth Inhibition Assay | IC50=7.04512 μM | SANGER | |||
| P30-OHK | Growth Inhibition Assay | IC50=7.21906 μM | SANGER | |||
| D-502MG | Growth Inhibition Assay | IC50=7.9836 μM | SANGER | |||
| RCC10RGB | Growth Inhibition Assay | IC50=8.0628 μM | SANGER | |||
| U-698-M | Growth Inhibition Assay | IC50=8.29226 μM | SANGER | |||
| BB49-HNC | Growth Inhibition Assay | IC50=9.42265 μM | SANGER | |||
| ES1 | Growth Inhibition Assay | IC50=9.68956 μM | SANGER | |||
| MFM-223 | Growth Inhibition Assay | IC50=10.9927 μM | SANGER | |||
| C2BBe1 | Growth Inhibition Assay | IC50=11.3523 μM | SANGER | |||
| EB2 | Growth Inhibition Assay | IC50=12.6881 μM | SANGER | |||
| C8166 | Growth Inhibition Assay | IC50=13.8303 μM | SANGER | |||
| ES3 | Growth Inhibition Assay | IC50=13.9977 μM | SANGER | |||
| NCI-H1650 | Growth Inhibition Assay | IC50=16.3765 μM | SANGER | |||
| Mo-T | Growth Inhibition Assay | IC50=17.4029 μM | SANGER | |||
| NB7 | Growth Inhibition Assay | IC50=17.7467 μM | SANGER | |||
| ES7 | Growth Inhibition Assay | IC50=19.5507 μM | SANGER | |||
| ES5 | Growth Inhibition Assay | IC50=21.7671 μM | SANGER | |||
| MSTO-211H | Growth Inhibition Assay | IC50=21.8858 μM | SANGER | |||
| U-87-MG | Growth Inhibition Assay | IC50=25.1966 μM | SANGER | |||
| THP-1 | Growth Inhibition Assay | IC50=29.7201 μM | SANGER | |||
| NB10 | Growth Inhibition Assay | IC50=30.2694 μM | SANGER | |||
| NH-12 | Growth Inhibition Assay | IC50=33.2017 μM | SANGER | |||
| COLO-824 | Growth Inhibition Assay | IC50=34.1006 μM | SANGER | |||
| SKM-1 | Growth Inhibition Assay | IC50=37.8422 μM | SANGER | |||
| NCI-H1838 | Growth Inhibition Assay | IC50=38.3797 μM | SANGER | |||
| RL | Growth Inhibition Assay | IC50=39.2477 μM | SANGER | |||
| COLO-800 | Growth Inhibition Assay | IC50=40.0773 μM | SANGER | |||
| KG-1 | Growth Inhibition Assay | IC50=40.8955 μM | SANGER | |||
| TUR | Growth Inhibition Assay | IC50=41.6399 μM | SANGER | |||
| LNCaP-Clone-FGC | Growth Inhibition Assay | IC50=41.9017 μM | SANGER | |||
| NCI-H322M | Growth Inhibition Assay | IC50=42.5984 μM | SANGER | |||
| LNCaP | Growth Inhibition Assay | IC50=91.3 nM | 25505174 | |||
| C4-2 | Growth Inhibition Assay | IC50=8 nM | 25505174 | |||
| JURKAT | Growth Inhibition Assay | 24 h | IC50=416.66 nM | 24519995 | ||
| MOLT-4 | Growth Inhibition Assay | 24 h | IC50=2853.5 nM | 24519995 | ||
| REH | Growth Inhibition Assay | 24 h | IC50=287.68 nM | 24519995 | ||
| NALM-6 | Growth Inhibition Assay | 24 h | IC50=34330 nM | 24519995 | ||
| RS 4;11 | Growth Inhibition Assay | 24 h | IC50=519.05 nM | 24519995 | ||
| 697 | Growth Inhibition Assay | 24 h | IC50=2107.1 nM | 24519995 | ||
| SIL-ALL | Growth Inhibition Assay | 24 h | IC50=199.77 nM | 24519995 | ||
| CEM | Growth Inhibition Assay | 24 h | IC50=52.18 nM | 24519995 | ||
| P12 | Growth Inhibition Assay | 24 h | IC50=39.27 nM | 24519995 | ||
| NALM-16 | Growth Inhibition Assay | 24 h | IC50=96.28 nM | 24519995 | ||
| JURKAT | Growth Inhibition Assay | 48 h | IC50=14.84 nM | 24519995 | ||
| MOLT-4 | Growth Inhibition Assay | 48 h | IC50=26.6 nM | 24519995 | ||
| REH | Growth Inhibition Assay | 48 h | IC50=44.71 nM | 24519995 | ||
| NALM-6 | Growth Inhibition Assay | 48 h | IC50=23.26 nM | 24519995 | ||
| RS 4;11 | Growth Inhibition Assay | 48 h | IC50=164.28 nM | 24519995 | ||
| 697 | Growth Inhibition Assay | 48 h | IC50=305.3 nM | 24519995 | ||
| SIL-ALL | Growth Inhibition Assay | 48 h | IC50=74.62 nM | 24519995 | ||
| CEM | Growth Inhibition Assay | 48 h | IC50=24.55 nM | 24519995 | ||
| P12 | Growth Inhibition Assay | 48 h | IC50=18.46 nM | 24519995 | ||
| NALM-16 | Growth Inhibition Assay | 48 h | IC50=63.24 nM | 24519995 | ||
| JURKAT | Growth Inhibition Assay | 72 h | IC50=3.65 nM | 24519995 | ||
| MOLT-4 | Growth Inhibition Assay | 72 h | IC50=7.39 nM | 24519995 | ||
| REH | Growth Inhibition Assay | 72 h | IC50=16.01 nM | 24519995 | ||
| NALM-6 | Growth Inhibition Assay | 72 h | IC50=1.78 nM | 24519995 | ||
| RS 4;11 | Growth Inhibition Assay | 72 h | IC50=4.38 nM | 24519995 | ||
| 697 | Growth Inhibition Assay | 72 h | IC50=74.28 nM | 24519995 | ||
| SIL-ALL | Growth Inhibition Assay | 72 h | IC50=7.2 nM | 24519995 | ||
| CEM | Growth Inhibition Assay | 72 h | IC50=5.42 nM | 24519995 | ||
| P12 | Growth Inhibition Assay | 72 h | IC50=6.37 nM | 24519995 | ||
| NALM-16 | Growth Inhibition Assay | 72 h | IC50=77.73 nM | 24519995 | ||
| Y79 | Apoptosis Assay | 1-50 nM | 12/24 h | DMSO | induced apoptosis which can be enhanced by HT | 24366665 |
| WER-Rb-1 | Apoptosis Assay | 1-50 nM | 12/24 h | DMSO | induced apoptosis which can be enhanced by HT | 24366665 |
| G7 | Growth Inhibition Assay | IC50=3.3 nM | 24204733 | |||
| G166 | Growth Inhibition Assay | IC50=7.0 nM | 24204733 | |||
| CB660 | Growth Inhibition Assay | IC50=6.4 nM | 24204733 | |||
| CB1117 | Growth Inhibition Assay | IC50=15.6 nM | 24204733 | |||
| KB-3-1 | Growth Inhibition Assay | IC50=1.48 ± 0.53 nM | 23962445 | |||
| KB-8-5-11 | Growth Inhibition Assay | IC50=5.01 ± 2.01 nM | 23962445 | |||
| KB-C-1 | Growth Inhibition Assay | IC50=16.76 ± 4.51 nM | 23962445 | |||
| KB-V-1 | Growth Inhibition Assay | IC50=281.24 ± 31.57 nM | 23962445 | |||
| OVCAR-8 | Growth Inhibition Assay | IC50=7.19 ± 3.60 nM | 23962445 | |||
| NCI-ADR-RES | Growth Inhibition Assay | IC50=1273.30 ± 191.20 nM | 23962445 | |||
| MCF7 | Growth Inhibition Assay | IC50=5.11 ± 1.47 nM | 23962445 | |||
| MCF7-FLV1000 | Growth Inhibition Assay | IC50=393.18 ± 74.83 nM | 23962445 | |||
| S1 | Growth Inhibition Assay | IC50=24.30 ± 4.75 nM | 23962445 | |||
| S1-M1-80 | Growth Inhibition Assay | IC50=261.06 ± 48.25 nM | 23962445 | |||
| CORL-23/P | Growth Inhibition Assay | IC50=4.38 ± 1.25 nM | 23962445 | |||
| CORL-23/R | Growth Inhibition Assay | IC50=5.16 ± 1.83 nM | 23962445 | |||
| NIH3T3 | Growth Inhibition Assay | IC50=40.60 ± 4.97 nM | 23962445 | |||
| NIH3T3-G185 | Growth Inhibition Assay | IC50=2413.40 ± 423.66 nM | 23962445 | |||
| pcDNA-HEK293 | Growth Inhibition Assay | IC50=2.75 ± 0.67 nM | 23962445 | |||
| MDR19-HEK293 | Growth Inhibition Assay | IC50=85.50 ± 13.67 nM | 23962445 | |||
| R482-HEK293 | Growth Inhibition Assay | IC50=25.97 ± 4.95 nM | 23962445 | |||
| MRP1-HEK293 | Growth Inhibition Assay | IC50=2.99 ± 1.49 nM | 23962445 | |||
| SF188 | Growth Inhibition Assay | 10-100 nM | 24-96 h | DMSO | inhibits cell growth in both time- and concentration- depedent manner | 23887645 |
| T98G | Growth Inhibition Assay | 10-100 nM | 24-96 h | DMSO | inhibits cell growth in concentration- depedent manner | 23887645 |
| DU145 | Growth Inhibition Assay | DMSO | IC50∼60 nM | 23884428 | ||
| LNCaP | Growth Inhibition Assay | DMSO | IC50∼75 nM | 23884428 | ||
| PC3 | Growth Inhibition Assay | DMSO | IC50∼175 nM | 23884428 | ||
| RT4 | Growth Inhibition Assay | IC50=27.21 nM | 23792639 | |||
| 5637 | Growth Inhibition Assay | IC50=45.47 nM | 23792639 | |||
| T24 | Growth Inhibition Assay | IC50=79.12 nM | 23792639 | |||
| MCF7 | Function Assay | 100 nM | 1 h | DMSO | reduces the induction of Greb1, Sgk1, Ps2, Serpina3, and Wisp2 | 23770244 |
| KB-V1 | Growth Inhibition Assay | IC50=3.92 μM | 23593196 | |||
| Hec50co | Growth Inhibition Assay | IC50=5 nM | 23146687 | |||
| MDA-MB-468 | Apoptosis Assay | 1/5/10 nM | 24/48/72 h | DMSO | induces apoptosis in a dose-dependent manner | 23144294 |
| MCF10A | Apoptosis Assay | 1/5/10 nM | 24/48/72 h | DMSO | induces apoptosis in a dose-dependent manner | 23144294 |
| Huh-7 | Growth Inhibition Assay | 1/10/100/1000 nM | 48 h | decreases the cell viability dose-dependently | 22745587 | |
| Daoy | Growth Inhibition Assay | 1.875-240 nM | 72 h | DMSO | IC50=5 nM | 22390279 |
| ONS-76 | Growth Inhibition Assay | 1.875-240 nM | 72 h | DMSO | IC50=7.5 nM | 22390279 |
| SUM 149 | Growth Inhibition Assay | 0-100 nM | 72 h | inhibits the cell viability in a dose-dependent mannar | 22309939 | |
| MDA-MB-231 | Growth Inhibition Assay | 0-100 nM | 72 h | inhibits the cell viability in a dose-dependent mannar | 22309939 | |
| HR5 | Growth Inhibition Assay | 0-100 nM | 72 h | inhibits the cell viability in a dose-dependent mannar | 22309939 | |
| BT-474-M1 | Growth Inhibition Assay | 0-100 nM | 72 h | inhibits the cell viability in a dose-dependent mannar | 22309939 | |
| AU565 | Growth Inhibition Assay | 0-100 nM | 72 h | inhibits the cell viability in a dose-dependent mannar | 22309939 | |
| T47D | Growth Inhibition Assay | 0-100 nM | 72 h | inhibits the cell viability in a dose-dependent mannar | 22309939 | |
| MCF7 | Growth Inhibition Assay | 0-100 nM | 72 h | inhibits the cell viability in a dose-dependent mannar | 22309939 | |
| HCT116p53(+/+) | Growth Inhibition Assay | 10-1000 nM | 24/48 h | inhibits cell proliferation completely at 25 nM | 22262171 | |
| HCT116p53(-/-) | Growth Inhibition Assay | 10-1000 nM | 24/48 h | inhibits cell proliferation completely at 25 nM | 22262171 | |
| HeLa | Growth Inhibition Assay | 10-100 nM | 48 h | DMSO | IC50=52.9 nM | 22080235 |
| HeLa | Growth Inhibition Assay | 10-100 nM | 72 h | DMSO | IC50=50.5 nM | 22080235 |
| GBC | Growth Inhibition Assay | 72 h | IC50=14.78 nM | 21965739 | ||
| GB-CL-1 | Growth Inhibition Assay | 72 h | IC50=5.22 nM | 21965739 | ||
| Mz-ChA-2 | Growth Inhibition Assay | 72 h | IC50=3.31 nM | 21965739 | ||
| TGBC1-TKB | Growth Inhibition Assay | 144 h | IC50=6.72 nM | 21965739 | ||
| Wittier | Growth Inhibition Assay | 72 h | IC50=3.26 nM | 21965739 | ||
| H-1 | Growth Inhibition Assay | 72 h | IC50=9.54 nM | 21965739 | ||
| HuH-28 | Growth Inhibition Assay | 72 h | IC50=11.19 nM | 21965739 | ||
| NEC | Growth Inhibition Assay | 72 h | IC50=9.98 nM | 21965739 | ||
| REB | Growth Inhibition Assay | 72 h | IC50=13.51 nM | 21965739 | ||
| CC-LP-1 | Growth Inhibition Assay | 72 h | IC50=5.84 nM | 21965739 | ||
| CC-SW-1 | Growth Inhibition Assay | 72 h | IC50=9.55 nM | 21965739 | ||
| EGI-1 | Growth Inhibition Assay | 72 h | IC50=10.72 nM | 21965739 | ||
| Sk-ChA-1 | Growth Inhibition Assay | 72 h | IC50=17.2 nM | 21965739 | ||
| TFK-1 | Growth Inhibition Assay | 72 h | IC50=13.45 nM | 21965739 | ||
| 786-O | Growth Inhibition Assay | 5-80 nM | 96 h | HCl | suppresses the proliferation in a dose-dependent manner with IC50 values of 2 to 20 nM | 21642374 |
| A498 | Growth Inhibition Assay | 5-80 nM | 96 h | HCl | suppresses the proliferation in a dose-dependent manner with IC50 values of 2 to 20 nM | 21642374 |
| ACHN | Growth Inhibition Assay | 5-80 nM | 96 h | HCl | suppresses the proliferation in a dose-dependent manner with IC50 values of 2 to 20 nM | 21642374 |
| Caki-1 | Growth Inhibition Assay | 5-80 nM | 96 h | HCl | suppresses the proliferation in a dose-dependent manner with IC50 values of 2 to 20 nM | 21642374 |
| SN12C | Growth Inhibition Assay | 5-80 nM | 96 h | HCl | suppresses the proliferation in a dose-dependent manner with IC50 values of 2 to 20 nM | 21642374 |
| HMC-1.1 | Growth Inhibition Assay | 1-1000 nM | 72 h | inhibits the cell proliferation in a dose-dependent manne | 21242189 | |
| HMC-1.2 | Growth Inhibition Assay | 1-1000 nM | 72 h | inhibits the cell proliferation in a dose-dependent manne | 21242189 | |
| C2 | Growth Inhibition Assay | 1-1000 nM | 72 h | inhibits the cell proliferation in a dose-dependent manne | 21242189 | |
| CHP-212 | Growth Inhibition Assay | 1-125 nM | 24-120 h | inhibits the cell proliferation in both time- and dose-dependent manne | 21169242 | |
| IMR-32 | Growth Inhibition Assay | 1-125 nM | 24-120 h | inhibits the cell proliferation in both time- and dose-dependent manne | 21169242 | |
| Kelly | Growth Inhibition Assay | 1-125 nM | 24-120 h | inhibits the cell proliferation in both time- and dose-dependent manne | 21169242 | |
| SH-EP | Growth Inhibition Assay | 1-125 nM | 24-120 h | inhibits the cell proliferation in both time- and dose-dependent manne | 21169242 | |
| SH-SY5Y | Growth Inhibition Assay | 1-125 nM | 24-120 h | inhibits the cell proliferation in both time- and dose-dependent manne | 21169242 | |
| SK-N-AS | Growth Inhibition Assay | 1-125 nM | 24-120 h | inhibits the cell proliferation in both time- and dose-dependent manne | 21169242 | |
| SK-N-BE | Growth Inhibition Assay | 1-125 nM | 24-120 h | inhibits the cell proliferation in both time- and dose-dependent manne | 21169242 | |
| KG1 | Growth Inhibition Assay | 1/10/100 nM | 72 h | DMSO | inhibits the cell proliferation in both time- and dose-dependent manne | 19458358 |
| U937 | Growth Inhibition Assay | 1/10/100 nM | 72 h | DMSO | inhibits the cell proliferation in both time- and dose-dependent manne | 19458358 |
| CAL62 | Growth Inhibition Assay | 0.1-100 nM | 72 h | DMSO | EC50=1.4 nM | 19223553 |
| OCUT-1 | Growth Inhibition Assay | 0.1-100 nM | 72 h | DMSO | EC50=2.3 nM | 19223553 |
| 8505C | Growth Inhibition Assay | 0.1-100 nM | 72 h | DMSO | EC50=3.2 nM | 19223553 |
| ACT-1 | Growth Inhibition Assay | 0.1-100 nM | 72 h | DMSO | EC50=5.4 nM | 19223553 |
| SW1736 | Growth Inhibition Assay | 0.1-100 nM | 72 h | DMSO | EC50=5.6 nM | 19223553 |
| HEK293 | Function assay | 1 hr | Binding affinity to PLK1 (unknown origin) expressed in HEK293 cells after 1 hr by proprietary competition assay, Ki = 0.00022 μM. | 26191363 | ||
| HEK293T | Antiproliferative assay | 72 hrs | Antiproliferative activity against HEK293T cells measured after 72 hrs by CellTiter-Blue assay, IC50 = 0.001 μM. | 28792760 | ||
| MDA-MB-231 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human MDA-MB-231 cells measured after 72 hrs by CellTiter-Blue assay, IC50 = 0.001 μM. | 28792760 | ||
| MM1S | Antiproliferative assay | 72 hrs | Antiproliferative activity against human MM1S cells measured after 72 hrs by CellTiter-Blue assay, IC50 = 0.001 μM. | 28792760 | ||
| TY82 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human TY82 cells after 72 hrs by CCK8 assay, IC50 = 0.001 μM. | 28586718 | ||
| NMC-797 | Cytotoxicity assay | 3 days | Cytotoxicity against BRD4 dependent human NMC-797 cells assessed as cell viability after 3 days by ATPlite assay, IC50 = 0.0107 μM. | 26985285 | ||
| MV4-11 | Cytotoxicity assay | 24 hrs | Cytotoxicity against human MV4-11 cells after 24 hrs by CellTiter-Blue assay, GI50 = 0.0152 μM. | 26191363 | ||
| BL21(DE3) | Function assay | 60 mins | Inhibition of recombinant human N-terminal His6-tagged BRD4 expressed in Escherichia coli BL21(DE3) cells using biotinylated histone H4 peptide as substrate after 60 mins by AlphaScreen assay, IC50 = 0.025 μM. | 28195723 | ||
| BL21(DE3) | Function assay | Inhibition of human N-terminal His6-tagged BRD4-BD1 (44 to 168 residues) expressed in Escherichia coli BL21 (DE3) cells using protein thermal shift dye as fluorescence probe by differential scanning fluorimetry, IC50 = 0.025 μM. | 28586718 | |||
| HuH7 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human HuH7 cells after 72 hrs by CCK8 assay, GI50 = 0.028 μM. | 29220793 | ||
| HeLa | Antiproliferative assay | 72 hrs | Antiproliferative activity against human HeLa cells after 72 hrs by CCK8 assay, GI50 = 0.034 μM. | 29220793 | ||
| HL60 | Cytotoxicity assay | 3 days | Cytotoxicity against BRD4 dependent human HL60 cells assessed as cell viability after 3 days by ATPlite assay, IC50 = 0.0365 μM. | 26985285 | ||
| A549 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human A549 cells after 72 hrs by CCK8 assay, GI50 = 0.057 μM. | 29220793 | ||
| MCF7 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human MCF7 cells after 72 hrs by CCK8 assay, GI50 = 0.067 μM. | 29220793 | ||
| K562 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human K562 cells after 72 hrs by CCK8 assay, GI50 = 0.068 μM. | 29220793 | ||
| MDA-MB-23 | Function assay | 6 hrs | Inhibition of PLK1 in human MDA-MB-23 cells assessed as decrease in TCTP phosphorylation after 6 hrs by Western blot method, IC50 = 0.1 μM. | 28792760 | ||
| HEK293T | Function assay | 6 hrs | Inhibition of PLK1 in HEK293T cells assessed as decrease in TCTP phosphorylation after 6 hrs by Western blot method, IC50 = 0.1 μM. | 28792760 | ||
| NCI-H1975 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human NCI-H1975 cells after 72 hrs by CCK8 assay, GI50 = 0.23 μM. | 29220793 | ||
| BL21(DE3) | Function assay | 4 hrs | Inhibition of JQ1-FITC binding to His6-tagged BRD4-BD1 (unknown origin) expressed in Escherichia coli BL21 (DE3)-codon plus-RIL cells incubated in dark for 4 hrs by fluorescence anisotropy assay, IC50 = 0.25 μM. | 28586718 | ||
| TC32 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells | 29435139 | |||
| U-2 OS | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells | 29435139 | |||
| A673 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells | 29435139 | |||
| Saos-2 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells | 29435139 | |||
| BT-37 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells | 29435139 | |||
| RD | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells | 29435139 | |||
| SK-N-SH | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells | 29435139 | |||
| BT-12 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells | 29435139 | |||
| NB1643 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells | 29435139 | |||
| OHS-50 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells | 29435139 | |||
| BT-12 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-12 cells | 29435139 | |||
| LAN-5 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for LAN-5 cells | 29435139 | |||
| Fibroblast cells | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells | 29435139 | |||
| NB-EBc1 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB-EBc1 cells | 29435139 | |||
| SK-N-SH | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-SH cells | 29435139 | |||
| A673 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for A673 cells) | 29435139 | |||
| BT-37 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-37 cells | 29435139 | |||
| MG 63(6-TG R) | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for MG 63 (6-TG R) cells | 29435139 | |||
| Fibroblast cells | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for control Hh wild type fibroblast cells | 29435139 | |||
| OHS-50 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for OHS-50 cells | 29435139 | |||
| RD | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for RD cells | 29435139 | |||
| SJ-GBM2 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells | 29435139 | |||
| SK-N-MC | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells | 29435139 | |||
| NB-EBc1 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells | 29435139 | |||
| LAN-5 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells | 29435139 | |||
| Rh18 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells | 29435139 | |||
| NB1643 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB1643 cells | 29435139 | |||
| SK-N-MC | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-MC cells | 29435139 | |||
| SJ-GBM2 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SJ-GBM2 cells | 29435139 | |||
| TC32 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for TC32 cells | 29435139 | |||
| Rh18 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh18 cells | 29435139 | |||
| Saos-2 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Saos-2 cells | 29435139 | |||
| DU145 | Apoptosis assay | 100 nM | 24 hrs | Induction of apoptosis in human DU145 cells assessed as increase in PARP cleavage at 100 nM after 24 hrs by immunoblotting method | 25685941 | |
| HeLa | Function assay | 100 nM | Inhibition of PLK1 Thr210 phosphorylation in human HeLa cells at 100 nM by immunoblotting method | 25685941 | ||
| DU145 | Function assay | 100 nM | Inhibition of PLK1 protein accumulation in human DU145 cells at 100 nM by immunoblotting method | 25685941 | ||
| HeLa | Function assay | 100 nM | Inhibition of PLK1 protein accumulation in human HeLa cells at 100 nM by immunoblotting method | 25685941 | ||
| HeLa | Function assay | 100 nM | 18 hrs | Induction of monopolar mitotic spindles in human HeLa cells at 100 nM incubated for 18 hrs by indirect immunofluorescence microscopy | 25685941 | |
| HeLa | Apoptosis assay | 100 nM | 24 hrs | Induction of apoptosis in human HeLa cells assessed as increase in PARP cleavage at 100 nM after 24 hrs by immunoblotting method | 25685941 | |
| PC3 | Function assay | 100 nM | 18 hrs | Induction of monopolar mitotic spindles in human PC3 cells at 100 nM incubated for 18 hrs by indirect immunofluorescence microscopy | 25685941 | |
| DU145 | Function assay | 100 nM | Inhibition of PLK1 Thr210 phosphorylation in human DU145 cells at 100 nM by immunoblotting method | 25685941 | ||
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Informazioni chimiche, conservazione e stabilità (Chemical Information, Storage & Stability)
| Peso molecolare | 521.66 | Formula | C28H39N7O3 |
Conservazione (Dalla data di ricezione) | |
|---|---|---|---|---|---|
| N. CAS | 755038-02-9 | Scarica SDF | Conservazione delle soluzioni stock |
|
|
| Sinonimi | N/A | Smiles | CCC1C(=O)N(C2=CN=C(N=C2N1C3CCCC3)NC4=C(C=C(C=C4)C(=O)NC5CCN(CC5)C)OC)C | ||
Solubilità (Solubility)
|
In vitro |
Ethanol : 104 mg/mL
DMSO
: 96 mg/mL
(184.02 mM)
Water : Insoluble |
Calcolatore di Molarità
Calcolatore di Diluizione
Calcolatore del Peso Molecolare
|
In vivo |
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Calcolatore di formulazione in vivo (Soluzione chiara)
Passo 1: Inserire le informazioni di seguito (Consigliato: Un animale aggiuntivo per tenere conto della perdita durante l'esperimento)
mg/kg
g
μL
Passo 2: Inserire la formulazione in vivo (Questo è solo il calcolatore, non la formulazione. Contattateci prima se non c'è una formulazione in vivo nella sezione Solubilità.)
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
Risultati del calcolo:
Concentrazione di lavoro: mg/ml;
Metodo per preparare il liquido master di DMSO: mg farmaco predissolto in μL DMSO ( Concentrazione del liquido master mg/mL, Vi preghiamo di contattarci prima se la concentrazione supera la solubilità del DMSO del lotto del farmaco. )
Metodo per preparare la formulazione in vivo: Prendere μL DMSO liquido master, quindi aggiungereμL PEG300, mescolare e chiarire, quindi aggiungereμL Tween 80, mescolare e chiarire, quindi aggiungere μL ddH2O, mescolare e chiarire.
Metodo per preparare la formulazione in vivo: Prendere μL DMSO liquido master, quindi aggiungere μL Olio di mais, mescolare e chiarire.
Nota: 1. Si prega di assicurarsi che il liquido sia limpido prima di aggiungere il solvente successivo.
2. Assicurarsi di aggiungere il/i solvente/i in ordine. È necessario assicurarsi che la soluzione ottenuta, nell'aggiunta precedente, sia una soluzione limpida prima di procedere all'aggiunta del solvente successivo. Metodi fisici come il vortex, gli ultrasuoni o il bagno d'acqua calda possono essere utilizzati per facilitare la dissoluzione.
Meccanismo d'azione (Mechanism of Action)
| Caratteristiche |
The first potent and selective Plk1 inhibitor that induces all hallmarks of Plk1 inhibition.
|
|---|---|
| Targets/IC50/Ki |
c-Myc
PLK1
(Cell-free assay) 0.83 nM
PLK2
(Cell-free assay) 3.5 nM
PLK3
(Cell-free assay) 9.0 nM
BRD4
(Cell-free assay) 37 nM(Kd)
|
| In vitro |
BI 2536 blocks the activities of Plk2 and Plk3 to a slightly lesser extent with IC50 of 3.5 nM and 9.0 nM, respectively. In HeLa cells, this compound treatment ranging from 10-100 nM leads to the blocking of the recruitment of γ-tubulin and phosphorylation of Apc6 at mitotic centrosomes, inhibition of cohesin release from chromosome arms, induction of monopolar spindles, as well as a range of other mitotic processes that are known to depend on Plk1. This chemical treatment leads to the HeLa cells arrested in G2/M, subsequently a sub-G1 DNA peak indicative of DNA breakdown and apoptosis, and accumulated cleaved PARP p85 fragments in a concentration-dependent manner. It inhibits the growth of a panel of 32 human cancer cell lines with EC50 of 2-25 nM, while blocking the proliferation of exponentially growing hTERT-RPE1, human umbilical vein endothelial cells (HUVECs), and normal rat kidney (NRK) cells with EC50 of 12-31 nM. Plk1 inhibition by this compound reduces the growth and viability of anaplastic thyroid carcinoma (ATC) cells such as CAL62, OCUT-1, SW1736, 8505C, and ACT-1 with EC50 values of 1.4-5.6 nM. |
| Saggio chinasico |
Saggio chinasi Plk1 in vitro
|
|
La Plk1 umana ricombinante (residui 1-603) è espressa come proteina di fusione N-terminale, con tag GST, utilizzando un sistema di espressione baculovirale e purificata mediante cromatografia di affinità con glutatione-agarosio. I saggi di attività enzimatica per Plk1 sono eseguiti in presenza di BI 2536 diluito in serie con 20 ng di chinasi ricombinante e 10 μg di caseina da latte bovino come substrato. Le reazioni chinasiche sono eseguite in un volume finale di 60 μL per 45 minuti a 30 °C (15 mM MgCl2, 25 mM MOPS [pH 7,0], 1 mM DTT, 1% DMSO, 7,5 mM ATP, 0,3 μCi γ-33P-ATP). Le reazioni sono terminate mediante l'aggiunta di 125 μL di TCA al 5% ghiacciato. Dopo il trasferimento dei precipitati su piastre filtranti Multi-Screen in estere di cellulosa misto, le piastre vengono lavate con TCA all'1% e quantificate radiometricamente. La curva dose-risposta viene utilizzata per calcolare il valore di IC50.
|
|
| In vivo |
BI 2536 given i.v. once or twice per week is highly efficacious in diverse xenograft models with acceptable tolerability by inhibiting cell proliferation through a mitotic arrest, and subsequently induction of tumor-cell death. Administration of this compound at 50 mg/kg once or twice per week significantly inhibits growth of HCT 116 xenografts with T/C of 15% and 0.3%, respectively. This chemical treatment twice-weekly also leads to excellent tumor-growth in BxPC-3 and A549 models with T/C of 5% and 14%, respectively. |
Riferimenti |
|
Applicazioni (Applications)
| Metodi | Biomarcatori | Immagini | PMID |
|---|---|---|---|
| Western blot | pro-caspase-8 / cleaved caspase-8 / cleaved caspase-3 / cleaved caspase-9 p-HH3 / PARP / Myc / p-Myc pMEK / MEK / pERK / ERK / pRSK1 / RSK1 pPlk1 / Plk1 / pMyt1 Aurora B / pAurora B / pAurora C / pH3 / Cyclin B1 / Securin / pBcl-XL / MPM2 |
|
27699933 |
| Immunofluorescence | p-H2AX / propidium iodide Pericentrin / α-tubulin |
|
22309939 |
| Growth inhibition assay | Cell viability |
|
21772266 |
Informazioni sullo studio clinico (Clinical Trial Information)
(dati da https://clinicaltrials.gov, aggiornato il 2014-05-16)
| Numero NCT | Reclutamento | Condizioni | Sponsor/Collaboratori | Data di inizio | Fasi |
|---|---|---|---|---|---|
| NCT00701766 | COMPLETED | Leukemia, Myeloid, Acute |
Boehringer Ingelheim |
2006-10 | PHASE2 |
| NCT02211833 | COMPLETED | Carcinoma, Non-Small-Cell Lung |
Boehringer Ingelheim |
2006-10 | PHASE1 |
| NCT02215044 | TERMINATED | Pancreatic Neoplasms |
Boehringer Ingelheim |
2007-06 | PHASE1 |
| NCT00710710 | COMPLETED | Pancreatic Neoplasms |
Boehringer Ingelheim |
2006-08-01 | PHASE2 |
| NCT00526149 | COMPLETED | Breast Cancer; Endometrial Cancer; Head and Neck Cancer; Melanoma (Skin); Ovarian Cancer; Sarcoma |
European Organisation for Research and Treatment of Cancer - EORTC |
2007-07 | PHASE2 |
| NCT00243087 | COMPLETED | Lymphoma |
Boehringer Ingelheim |
2005-07 | PHASE1 |
Domande Frequenti (Frequently Asked Questions)
Domanda 1:
We need to use it in preclinical studies using mice; how to formulate this compound for the in vivo study?
Risposta:
For in vivo study, DMSO should not be more than 5% because of the toxicity. It can be formulated in hydrochloric acid (0.1 N), and diluted with 0.9% NaCl for animal study according to the reference: (Supplemental Data) http://linkinghub.elsevier.com/retrieve/pii/S0960-9822(06)02671-6
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