nur für Forschungszwecke
BI 2536 PLK1/BRD4-Inhibitor
Kat.-Nr.S1109
Chemische Struktur
Molekulargewicht: 521.66
Springe zu
Qualitätskontrolle
Charge:
Reinheit:
99.88%
99.88
| Verwandte Ziele | CDK HSP PD-1/PD-L1 ROCK Wee1 DNA/RNA Synthesis Microtubule Associated Ras KRas Aurora Kinase |
|---|---|
| Weitere PLK Inhibitoren | Volasertib (BI6727) Rigosertib (ON-01910) GSK461364 Onvansertib (NMS-1286937, NMS-P937) CFI-400945 HMN-214 Ro3280 SBE 13 HCl MLN0905 Centrinone (LCR-263) |
Zellkultur, Behandlung & Arbeitskonzentration
| Zelllinien | Assay-Typ | Konzentration | Inkubationszeit | Formulierung | Aktivitätsbeschreibung | 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 | ||
| Klicken Sie hier, um weitere experimentelle Daten zu Zelllinien anzuzeigen | ||||||
Chemische Informationen, Lagerung & Stabilität
| Molekulargewicht | 521.66 | Formel | C28H39N7O3 |
Lagerung (Ab dem Eingangsdatum) | |
|---|---|---|---|---|---|
| CAS-Nr. | 755038-02-9 | SDF herunterladen | Lagerung von Stammlösungen |
|
|
| Synonyme | N/A | Smiles | CCC1C(=O)N(C2=CN=C(N=C2N1C3CCCC3)NC4=C(C=C(C=C4)C(=O)NC5CCN(CC5)C)OC)C | ||
Löslichkeit
|
In vitro |
Ethanol : 104 mg/mL
DMSO
: 96 mg/mL
(184.02 mM)
Water : Insoluble |
Molaritätsrechner
Verdünnungsrechner
Molekulargewichtsrechner
|
In vivo |
|||||
In-vivo-Formulierungsrechner (Klare Lösung)
Schritt 1: Geben Sie die untenstehenden Informationen ein (Empfohlen: Ein zusätzliches Tier zur Berücksichtigung von Verlusten während des Experiments)
mg/kg
g
μL
Schritt 2: Geben Sie die In-vivo-Formulierung ein (Dies ist nur der Rechner, keine Formulierung. Bitte kontaktieren Sie uns zuerst, wenn es im Abschnitt "Löslichkeit" keine In-vivo-Formulierung gibt.)
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
Berechnungsergebnisse:
Arbeitskonzentration: mg/ml;
Methode zur Herstellung der DMSO-Stammlösung: mg Wirkstoff vorgelöst in μL DMSO ( Konzentration der Stammlösung mg/mL, Bitte kontaktieren Sie uns zuerst, wenn die Konzentration die DMSO-Löslichkeit der Wirkstoffcharge überschreitet. )
Methode zur Herstellung der In-vivo-Formulierung: Nehmen Sie μL DMSO Stammlösung, dann hinzufügenμL PEG300, mischen und klären, dann hinzufügenμL Tween 80, mischen und klären, dann hinzufügen μL ddH2O, mischen und klären.
Methode zur Herstellung der In-vivo-Formulierung: Nehmen Sie μL DMSO Stammlösung, dann hinzufügen μL Maisöl, mischen und klären.
Hinweis: 1. Bitte stellen Sie sicher, dass die Flüssigkeit klar ist, bevor Sie das nächste Lösungsmittel hinzufügen.
2. Achten Sie darauf, das/die Lösungsmittel der Reihe nach hinzuzufügen. Sie müssen sicherstellen, dass die bei der vorherigen Zugabe erhaltene Lösung eine klare Lösung ist, bevor Sie mit der Zugabe des nächsten Lösungsmittels fortfahren. Physikalische Methoden wie Vortex, Ultraschall oder ein heißes Wasserbad können zur Unterstützung des Lösens verwendet werden.
Wirkmechanismus
| Merkmale |
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 blockiert die Aktivitäten von Plk2 und Plk3 in geringerem Maße mit IC50-Werten von 3,5 nM bzw. 9,0 nM. In HeLa-Zellen führt die Behandlung mit dieser Verbindung im Bereich von 10-100 nM zur Blockierung der Rekrutierung von γ-Tubulin und der Phosphorylierung von Apc6 an mitotischen Zentrosomen, zur Hemmung der Kohäsinfreisetzung von Chromosomenarmen, zur Induktion monopolarer Spindeln sowie zu einer Reihe anderer mitotischer Prozesse, die bekanntermaßen von Plk1 abhängen. Diese chemische Behandlung führt dazu, dass HeLa-Zellen in G2/M arretiert werden, gefolgt von einem Sub-G1-DNA-Peak, der auf DNA-Abbau und Apoptose hinweist, und akkumulierten gespaltenen PARP-p85-Fragmenten in konzentrationsabhängiger Weise. Es hemmt das Wachstum einer Reihe von 32 menschlichen Krebszelllinien mit einer EC50 von 2-25 nM, während es die Proliferation von exponentiell wachsenden hTERT-RPE1-, humanen Nabelvenen-Endothelzellen (HUVECs) und normalen Rattennieren-(NRK)-Zellen mit einer EC50 von 12-31 nM blockiert. Die Plk1-Hemmung durch diese Verbindung reduziert das Wachstum und die Lebensfähigkeit von anaplastischen Schilddrüsenkarzinom-(ATC)-Zellen wie CAL62, OCUT-1, SW1736, 8505C und ACT-1 mit EC50-Werten von 1,4-5,6 nM. |
| Kinase-Assay |
Plk1 In-vitro-Kinase-Assay
|
|
Rekombinantes humanes Plk1 (Reste 1-603) wird als N-terminales, GST-markiertes Fusionsprotein mit einem baculoviralen Expressionssystem exprimiert und mittels Affinitätschromatographie mit Glutathion-Agarose gereinigt. Enzymaktivitätsassays für Plk1 werden in Gegenwart von seriell verdünntem BI 2536 mit 20 ng rekombinanter Kinase und 10 μg Kasein aus Kuhmilch als Substrat durchgeführt. Die Kinase-Reaktionen werden in einem Endvolumen von 60 μL für 45 Minuten bei 30 °C durchgeführt (15 mM MgCl2, 25 mM MOPS [pH 7.0], 1 mM DTT, 1% DMSO, 7.5 mM ATP, 0.3 μCi γ-33P-ATP). Die Reaktionen werden durch Zugabe von 125 μL eiskalter 5%iger TCA beendet. Nach Übertragung der Präzipitate auf Multi-Screen-Mischester-Cellulosefilterplatten werden die Platten mit 1%iger TCA gewaschen und radiometrisch quantifiziert. Die Dosis-Wirkungs-Kurve wird zur Berechnung des IC50-Wertes verwendet.
|
|
| In vivo |
BI 2536, i.v. einmal oder zweimal pro Woche verabreicht, ist in verschiedenen Xenograft-Modellen hochwirksam mit akzeptabler Verträglichkeit, indem es die Zellproliferation durch einen mitotischen Arrest und anschließende Induktion des Tumorzelltods hemmt. Die Verabreichung dieser Verbindung in einer Dosis von 50 mg/kg einmal oder zweimal pro Woche hemmt signifikant das Wachstum von HCT 116-Xenografts mit T/C von 15% bzw. 0,3%. Diese zweimal wöchentliche chemische Behandlung führt auch zu einem ausgezeichneten Tumorwachstum in BxPC-3- und A549-Modellen mit T/C von 5% bzw. 14%. |
Literatur |
|
Anwendungen
| Methoden | Biomarker | Bilder | 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 |
Klinische Studieninformationen
(Daten von https://clinicaltrials.gov, aktualisiert am 2024-05-22)
| NCT-Nummer | Rekrutierung | Erkrankungen | Sponsor/Kooperationspartner | Startdatum | Phasen |
|---|---|---|---|---|---|
| NCT02215044 | Terminated | Pancreatic Neoplasms |
Boehringer Ingelheim |
June 2007 | Phase 1 |
| NCT02211833 | Completed | Carcinoma Non-Small-Cell Lung |
Boehringer Ingelheim |
October 2006 | Phase 1 |
| NCT00701766 | Completed | Leukemia Myeloid Acute |
Boehringer Ingelheim |
October 2006 | Phase 2 |
| NCT00706498 | Completed | Prostatic Neoplasms |
Boehringer Ingelheim |
September 2006 | Phase 2 |
| NCT00376623 | Completed | Carcinoma Non-Small-Cell Lung |
Boehringer Ingelheim |
July 25 2006 | Phase 2 |
| NCT02211872 | Completed | Neoplasms |
Boehringer Ingelheim |
August 2004 | Phase 1 |
Technischer Support
Tel: +1-832-582-8158 Ext:3
Wenn Sie weitere Fragen haben, hinterlassen Sie bitte eine Nachricht.
Häufig gestellte Fragen
Frage 1:
We need to use it in preclinical studies using mice; how to formulate this compound for the in vivo study?
Antwort:
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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