- 阻害剤
- 研究分野別
- PI3K/Akt/mTOR
- Epigenetics
- Methylation
- Immunology & Inflammation
- Protein Tyrosine Kinase
- Angiogenesis
- Apoptosis
- Autophagy
- ER stress & UPR
- JAK/STAT
- MAPK
- Cytoskeletal Signaling
- Cell Cycle
- TGF-beta/Smad
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BI 2536
BI-2536 is a potent Plk1 inhibitor with IC50 of 0.83 nM in a cell-free assay. BI-2536 inhibits Bromodomain 4 (BRD4) with Kd of 37 nM and potently suppresses c-Myc expression. BI-2536 induces apoptosis and attenuates autophagy. Phase 2.
CAS No. 755038-02-9
文献中Selleckの製品使用例（280）
製品安全説明書
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BI 2536関連製品
シグナル伝達経路
PLK阻害剤の選択性比較
Cell Data
| Cell Lines | Assay Type | Concentration | Incubation Time | 活性情報 | PMID |
|---|---|---|---|---|---|
| Y79 | Apoptosis Assay | 1-50 nM | 12/24 h | induced apoptosis which can be enhanced by HT | 24366665 |
| WER-Rb-1 | Apoptosis Assay | 1-50 nM | 12/24 h | induced apoptosis which can be enhanced by HT | 24366665 |
| SF188 | Growth Inhibition Assay | 10-100 nM | 24-96 h | inhibits cell growth in both time- and concentration- depedent manner | 23887645 |
| T98G | Growth Inhibition Assay | 10-100 nM | 24-96 h | inhibits cell growth in concentration- depedent manner | 23887645 |
| MCF7 | Function Assay | 100 nM | 1 h | reduces the induction of Greb1, Sgk1, Ps2, Serpina3, and Wisp2 | 23770244 |
| MDA-MB-468 | Apoptosis Assay | 1/5/10 nM | 24/48/72 h | induces apoptosis in a dose-dependent manner | 23144294 |
| MCF10A | Apoptosis Assay | 1/5/10 nM | 24/48/72 h | 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 | IC50=5 nM | 22390279 |
| ONS-76 | Growth Inhibition Assay | 1.875-240 nM | 72 h | 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 | IC50=52.9 nM | 22080235 |
| HeLa | Growth Inhibition Assay | 10-100 nM | 72 h | IC50=50.5 nM | 22080235 |
| 786-O | Growth Inhibition Assay | 5-80 nM | 96 h | 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 | 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 | 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 | 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 | 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 | inhibits the cell proliferation in both time- and dose-dependent manne | 19458358 |
| U937 | Growth Inhibition Assay | 1/10/100 nM | 72 h | inhibits the cell proliferation in both time- and dose-dependent manne | 19458358 |
| CAL62 | Growth Inhibition Assay | 0.1-100 nM | 72 h | EC50=1.4 nM | 19223553 |
| OCUT-1 | Growth Inhibition Assay | 0.1-100 nM | 72 h | EC50=2.3 nM | 19223553 |
| 8505C | Growth Inhibition Assay | 0.1-100 nM | 72 h | EC50=3.2 nM | 19223553 |
| ACT-1 | Growth Inhibition Assay | 0.1-100 nM | 72 h | EC50=5.4 nM | 19223553 |
| SW1736 | Growth Inhibition Assay | 0.1-100 nM | 72 h | EC50=5.6 nM | 19223553 |
| 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 | 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 |
| 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 | |
| DU145 | Function assay | 100 nM | Inhibition of PLK1 Thr210 phosphorylation in human DU145 cells at 100 nM by immunoblotting method | 25685941 | |
| 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 | |
| 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 | |
| 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 | |
| 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 | |
| A3-KAW | Growth Inhibition Assay | IC50=0.25341 μM | SANGER | ||
| CTB-1 | Growth Inhibition Assay | IC50=0.24493 μM | SANGER | ||
| LB1047-RCC | Growth Inhibition Assay | IC50=0.2441 μM | SANGER | ||
| OPM-2 | Growth Inhibition Assay | IC50=0.23882 μM | SANGER | ||
| NCI-H345 | Growth Inhibition Assay | IC50=0.23805 μM | SANGER | ||
| SIG-M5 | Growth Inhibition Assay | IC50=0.22727 μM | SANGER | ||
| BC-1 | Growth Inhibition Assay | IC50=0.22616 μM | SANGER | ||
| GR-ST | Growth Inhibition Assay | IC50=0.21488 μM | SANGER | ||
| NCI-H1436 | Growth Inhibition Assay | IC50=0.21464 μM | SANGER | ||
| HH | Growth Inhibition Assay | IC50=0.21405 μM | SANGER | ||
| GAK | Growth Inhibition Assay | IC50=0.21189 μM | SANGER | ||
| NCI-H720 | Growth Inhibition Assay | IC50=0.20525 μM | SANGER | ||
| JiyoyeP-2003 | Growth Inhibition Assay | IC50=0.20477 μM | SANGER | ||
| EVSA-T | Growth Inhibition Assay | IC50=0.20312 μM | SANGER | ||
| UACC-257 | Growth Inhibition Assay | IC50=0.19947 μM | SANGER | ||
| LC4-1 | Growth Inhibition Assay | IC50=0.19502 μM | SANGER | ||
| KARPAS-299 | Growth Inhibition Assay | IC50=0.19241 μM | SANGER | ||
| NCI-H2141 | Growth Inhibition Assay | IC50=0.19011 μM | SANGER | ||
| SNB75 | Growth Inhibition Assay | IC50=0.18824 μM | SANGER | ||
| L-428 | Growth Inhibition Assay | IC50=0.18813 μM | SANGER | ||
| NB6 | Growth Inhibition Assay | IC50=0.18566 μM | SANGER | ||
| COLO-320-HSR | Growth Inhibition Assay | IC50=0.18154 μM | SANGER | ||
| DOHH-2 | Growth Inhibition Assay | IC50=0.17672 μM | SANGER | ||
| ARH-77 | Growth Inhibition Assay | IC50=0.17379 μM | SANGER | ||
| LOXIMVI | Growth Inhibition Assay | IC50=0.16949 μM | SANGER | ||
| HCE-T | Growth Inhibition Assay | IC50=0.16504 μM | SANGER | ||
| NCI-H64 | Growth Inhibition Assay | IC50=0.16347 μM | SANGER | ||
| SU-DHL-1 | Growth Inhibition Assay | IC50=0.16206 μM | SANGER | ||
| MC116 | Growth Inhibition Assay | IC50=0.16158 μM | SANGER | ||
| LS-123 | Growth Inhibition Assay | IC50=0.15917 μM | SANGER | ||
| KINGS-1 | Growth Inhibition Assay | IC50=0.1591 μM | SANGER | ||
| COLO-684 | Growth Inhibition Assay | IC50=0.15721 μM | SANGER | ||
| SCLC-21H | Growth Inhibition Assay | IC50=0.15702 μM | SANGER | ||
| TGBC24TKB | Growth Inhibition Assay | IC50=0.15659 μM | SANGER | ||
| EM-2 | Growth Inhibition Assay | IC50=0.15467 μM | SANGER | ||
| SH-4 | Growth Inhibition Assay | IC50=0.15466 μM | SANGER | ||
| NB5 | Growth Inhibition Assay | IC50=0.15462 μM | SANGER | ||
| NKM-1 | Growth Inhibition Assay | IC50=0.14906 μM | SANGER | ||
| COR-L88 | Growth Inhibition Assay | IC50=0.14802 μM | SANGER | ||
| GB-1 | Growth Inhibition Assay | IC50=0.14526 μM | SANGER | ||
| CAL-148 | Growth Inhibition Assay | IC50=0.14483 μM | SANGER | ||
| LP-1 | Growth Inhibition Assay | IC50=0.1424 μM | SANGER | ||
| MLMA | Growth Inhibition Assay | IC50=0.14167 μM | SANGER | ||
| NCCIT | Growth Inhibition Assay | IC50=0.13939 μM | SANGER | ||
| NCI-H747 | Growth Inhibition Assay | IC50=0.137 μM | SANGER | ||
| KP-N-RT-BM-1 | Growth Inhibition Assay | IC50=0.13612 μM | SANGER | ||
| HT | Growth Inhibition Assay | IC50=0.13574 μM | SANGER | ||
| LAMA-84 | Growth Inhibition Assay | IC50=0.13187 μM | SANGER | ||
| EW-3 | Growth Inhibition Assay | IC50=0.12893 μM | SANGER | ||
| no-11 | Growth Inhibition Assay | IC50=0.12869 μM | SANGER | ||
| RPMI-6666 | Growth Inhibition Assay | IC50=0.12743 μM | SANGER | ||
| SR | Growth Inhibition Assay | IC50=0.12441 μM | SANGER | ||
| SK-PN-DW | Growth Inhibition Assay | IC50=0.12287 μM | SANGER | ||
| MZ7-mel | Growth Inhibition Assay | IC50=0.12237 μM | SANGER | ||
| RPMI-8226 | Growth Inhibition Assay | IC50=0.12052 μM | SANGER | ||
| KU812 | Growth Inhibition Assay | IC50=0.12044 μM | SANGER | ||
| TK10 | Growth Inhibition Assay | IC50=0.11728 μM | SANGER | ||
| K052 | Growth Inhibition Assay | IC50=0.11712 μM | SANGER | ||
| EoL-1-cell | Growth Inhibition Assay | IC50=0.11672 μM | SANGER | ||
| NCI-H524 | Growth Inhibition Assay | IC50=0.11274 μM | SANGER | ||
| BV-173 | Growth Inhibition Assay | IC50=0.11243 μM | SANGER | ||
| L-363 | Growth Inhibition Assay | IC50=0.11079 μM | SANGER | ||
| MZ2-MEL | Growth Inhibition Assay | IC50=0.1105 μM | SANGER | ||
| JAR | Growth Inhibition Assay | IC50=0.10925 μM | SANGER | ||
| K-562 | Growth Inhibition Assay | IC50=0.10858 μM | SANGER | ||
| HD-MY-Z | Growth Inhibition Assay | IC50=0.10856 μM | SANGER | ||
| NCI-SNU-16 | Growth Inhibition Assay | IC50=0.10742 μM | SANGER | ||
| L-540 | Growth Inhibition Assay | IC50=0.10708 μM | SANGER | ||
| NCI-H1304 | Growth Inhibition Assay | IC50=0.10594 μM | SANGER | ||
| NEC8 | Growth Inhibition Assay | IC50=0.10525 μM | SANGER | ||
| NCI-H526 | Growth Inhibition Assay | IC50=0.1044 μM | SANGER | ||
| DU-4475 | Growth Inhibition Assay | IC50=0.10407 μM | SANGER | ||
| BB65-RCC | Growth Inhibition Assay | IC50=0.10294 μM | SANGER | ||
| NCI-H1882 | Growth Inhibition Assay | IC50=0.09809 μM | SANGER | ||
| NCI-H2126 | Growth Inhibition Assay | IC50=0.09791 μM | SANGER | ||
| BC-3 | Growth Inhibition Assay | IC50=0.09662 μM | SANGER | ||
| Calu-6 | Growth Inhibition Assay | IC50=0.09598 μM | SANGER | ||
| COR-L279 | Growth Inhibition Assay | IC50=0.09556 μM | SANGER | ||
| NCI-H446 | Growth Inhibition Assay | IC50=0.09462 μM | SANGER | ||
| ONS-76 | Growth Inhibition Assay | IC50=0.09276 μM | SANGER | ||
| NCI-SNU-5 | Growth Inhibition Assay | IC50=0.09258 μM | SANGER | ||
| MOLT-4 | Growth Inhibition Assay | IC50=0.08983 μM | SANGER | ||
| DG-75 | Growth Inhibition Assay | IC50=0.08922 μM | SANGER | ||
| A253 | Growth Inhibition Assay | IC50=0.08822 μM | SANGER | ||
| KGN | Growth Inhibition Assay | IC50=0.08759 μM | SANGER | ||
| NCI-H1694 | Growth Inhibition Assay | IC50=0.08744 μM | SANGER | ||
| LU-134-A | Growth Inhibition Assay | IC50=0.08708 μM | SANGER | ||
| HEL | Growth Inhibition Assay | IC50=0.08668 μM | SANGER | ||
| LB831-BLC | Growth Inhibition Assay | IC50=0.08561 μM | SANGER | ||
| NCI-H510A | Growth Inhibition Assay | IC50=0.08336 μM | SANGER | ||
| Daudi | Growth Inhibition Assay | IC50=0.08256 μM | SANGER | ||
| Ramos-2G6-4C10 | Growth Inhibition Assay | IC50=0.08225 μM | SANGER | ||
| CMK | Growth Inhibition Assay | IC50=0.08225 μM | SANGER | ||
| KNS-42 | Growth Inhibition Assay | IC50=0.08161 μM | SANGER | ||
| MOLT-16 | Growth Inhibition Assay | IC50=0.08121 μM | SANGER | ||
| MONO-MAC-6 | Growth Inhibition Assay | IC50=0.07986 μM | SANGER | ||
| SW962 | Growth Inhibition Assay | IC50=0.07839 μM | SANGER | ||
| NCI-H187 | Growth Inhibition Assay | IC50=0.07726 μM | SANGER | ||
| DMS-114 | Growth Inhibition Assay | IC50=0.07528 μM | SANGER | ||
| U-266 | Growth Inhibition Assay | IC50=0.07497 μM | SANGER | ||
| NCI-H1581 | Growth Inhibition Assay | IC50=0.07478 μM | SANGER | ||
| VA-ES-BJ | Growth Inhibition Assay | IC50=0.07475 μM | SANGER | ||
| GI-ME-N | Growth Inhibition Assay | IC50=0.07286 μM | SANGER | ||
| IST-SL2 | Growth Inhibition Assay | IC50=0.07004 μM | SANGER | ||
| RXF393 | Growth Inhibition Assay | IC50=0.06764 μM | SANGER | ||
| KS-1 | Growth Inhibition Assay | IC50=0.06748 μM | SANGER | ||
| NB1 | Growth Inhibition Assay | IC50=0.06613 μM | SANGER | ||
| CPC-N | Growth Inhibition Assay | IC50=0.06524 μM | SANGER | ||
| BB30-HNC | Growth Inhibition Assay | IC50=0.06436 μM | SANGER | ||
| ATN-1 | Growth Inhibition Assay | IC50=0.06345 μM | SANGER | ||
| MHH-PREB-1 | Growth Inhibition Assay | IC50=0.06319 μM | SANGER | ||
| RS4-11 | Growth Inhibition Assay | IC50=0.06304 μM | SANGER | ||
| SF268 | Growth Inhibition Assay | IC50=0.06286 μM | SANGER | ||
| KM-H2 | Growth Inhibition Assay | IC50=0.06221 μM | SANGER | ||
| HT-144 | Growth Inhibition Assay | IC50=0.0613 μM | SANGER | ||
| LB771-HNC | Growth Inhibition Assay | IC50=0.05979 μM | SANGER | ||
| NALM-6 | Growth Inhibition Assay | IC50=0.05973 μM | SANGER | ||
| 8-MG-BA | Growth Inhibition Assay | IC50=0.05851 μM | SANGER | ||
| EW-1 | Growth Inhibition Assay | IC50=0.05837 μM | SANGER | ||
| SK-LMS-1 | Growth Inhibition Assay | IC50=0.05805 μM | SANGER | ||
| TE-6 | Growth Inhibition Assay | IC50=0.05722 μM | SANGER | ||
| DEL | Growth Inhibition Assay | IC50=0.05709 μM | SANGER | ||
| TALL-1 | Growth Inhibition Assay | IC50=0.05708 μM | SANGER | ||
| KY821 | Growth Inhibition Assay | IC50=0.05632 μM | SANGER | ||
| TE-12 | Growth Inhibition Assay | IC50=0.05613 μM | SANGER | ||
| HC-1 | Growth Inhibition Assay | IC50=0.05597 μM | SANGER | ||
| SJSA-1 | Growth Inhibition Assay | IC50=0.0552 μM | SANGER | ||
| CTV-1 | Growth Inhibition Assay | IC50=0.05502 μM | SANGER | ||
| no-10 | Growth Inhibition Assay | IC50=0.05474 μM | SANGER | ||
| ML-2 | Growth Inhibition Assay | IC50=0.05414 μM | SANGER | ||
| TGBC1TKB | Growth Inhibition Assay | IC50=0.05405 μM | SANGER | ||
| KARPAS-45 | Growth Inhibition Assay | IC50=0.05358 μM | SANGER | ||
| NB17 | Growth Inhibition Assay | IC50=0.05207 μM | SANGER | ||
| DJM-1 | Growth Inhibition Assay | IC50=0.05142 μM | SANGER | ||
| TE-5 | Growth Inhibition Assay | IC50=0.05063 μM | SANGER | ||
| IMR-5 | Growth Inhibition Assay | IC50=0.05021 μM | SANGER | ||
| MFH-ino | Growth Inhibition Assay | IC50=0.05003 μM | SANGER | ||
| MS-1 | Growth Inhibition Assay | IC50=0.04701 μM | SANGER | ||
| LU-139 | Growth Inhibition Assay | IC50=0.04442 μM | SANGER | ||
| IST-MEL1 | Growth Inhibition Assay | IC50=0.04442 μM | SANGER | ||
| HCC1599 | Growth Inhibition Assay | IC50=0.04258 μM | SANGER | ||
| MOLT-13 | Growth Inhibition Assay | IC50=0.04238 μM | SANGER | ||
| PF-382 | Growth Inhibition Assay | IC50=0.04198 μM | SANGER | ||
| MZ1-PC | Growth Inhibition Assay | IC50=0.04127 μM | SANGER | ||
| BL-41 | Growth Inhibition Assay | IC50=0.04125 μM | SANGER | ||
| KP-N-YS | Growth Inhibition Assay | IC50=0.04085 μM | SANGER | ||
| OVCAR-4 | Growth Inhibition Assay | IC50=0.04059 μM | SANGER | ||
| TE-10 | Growth Inhibition Assay | IC50=0.04046 μM | SANGER | ||
| SW982 | Growth Inhibition Assay | IC50=0.0379 μM | SANGER | ||
| SK-UT-1 | Growth Inhibition Assay | IC50=0.03774 μM | SANGER | ||
| A101D | Growth Inhibition Assay | IC50=0.03748 μM | SANGER | ||
| Becker | Growth Inhibition Assay | IC50=0.03555 μM | SANGER | ||
| SK-NEP-1 | Growth Inhibition Assay | IC50=0.03499 μM | SANGER | ||
| ES4 | Growth Inhibition Assay | IC50=0.03463 μM | SANGER | ||
| NTERA-S-cl-D1 | Growth Inhibition Assay | IC50=0.03399 μM | SANGER | ||
| NCI-H82 | Growth Inhibition Assay | IC50=0.03343 μM | SANGER | ||
| ST486 | Growth Inhibition Assay | IC50=0.03337 μM | SANGER | ||
| NB13 | Growth Inhibition Assay | IC50=0.03316 μM | SANGER | ||
| LB647-SCLC | Growth Inhibition Assay | IC50=0.03195 μM | SANGER | ||
| GT3TKB | Growth Inhibition Assay | IC50=0.02953 μM | SANGER | ||
| ES6 | Growth Inhibition Assay | IC50=0.02881 μM | SANGER | ||
| BL-70 | Growth Inhibition Assay | IC50=0.02857 μM | SANGER | ||
| TE-11 | Growth Inhibition Assay | IC50=0.02809 μM | SANGER | ||
| NCI-H1355 | Growth Inhibition Assay | IC50=0.02783 μM | SANGER | ||
| KE-37 | Growth Inhibition Assay | IC50=0.02741 μM | SANGER | ||
| BE-13 | Growth Inhibition Assay | IC50=0.0274 μM | SANGER | ||
| TE-15 | Growth Inhibition Assay | IC50=0.02738 μM | SANGER | ||
| ETK-1 | Growth Inhibition Assay | IC50=0.02736 μM | SANGER | ||
| HCE-4 | Growth Inhibition Assay | IC50=0.02682 μM | SANGER | ||
| NCI-H1648 | Growth Inhibition Assay | IC50=0.02647 μM | SANGER | ||
| HUTU-80 | Growth Inhibition Assay | IC50=0.02624 μM | SANGER | ||
| CCRF-CEM | Growth Inhibition Assay | IC50=0.02543 μM | SANGER | ||
| TE-1 | Growth Inhibition Assay | IC50=0.02512 μM | SANGER | ||
| RPMI-8402 | Growth Inhibition Assay | IC50=0.02508 μM | SANGER | ||
| HOP-62 | Growth Inhibition Assay | IC50=0.0242 μM | SANGER | ||
| KALS-1 | Growth Inhibition Assay | IC50=0.02338 μM | SANGER | ||
| KURAMOCHI | Growth Inhibition Assay | IC50=0.02285 μM | SANGER | ||
| TE-9 | Growth Inhibition Assay | IC50=0.02261 μM | SANGER | ||
| A388 | Growth Inhibition Assay | IC50=0.02227 μM | SANGER | ||
| A4-Fuk | Growth Inhibition Assay | IC50=0.02218 μM | SANGER | ||
| NOS-1 | Growth Inhibition Assay | IC50=0.02093 μM | SANGER | ||
| LOUCY | Growth Inhibition Assay | IC50=0.0205 μM | SANGER | ||
| RKO | Growth Inhibition Assay | IC50=0.01987 μM | SANGER | ||
| OCUB-M | Growth Inhibition Assay | IC50=0.01826 μM | SANGER | ||
| LXF-289 | Growth Inhibition Assay | IC50=0.0177 μM | SANGER | ||
| RL95-2 | Growth Inhibition Assay | IC50=0.01738 μM | SANGER | ||
| SW954 | Growth Inhibition Assay | IC50=0.01705 μM | SANGER | ||
| IA-LM | Growth Inhibition Assay | IC50=0.01688 μM | SANGER | ||
| NCI-H1963 | Growth Inhibition Assay | IC50=0.01673 μM | SANGER | ||
| 697 | Growth Inhibition Assay | IC50=0.01668 μM | SANGER | ||
| CESS | Growth Inhibition Assay | IC50=0.01602 μM | SANGER | ||
| SNU-C2B | Growth Inhibition Assay | IC50=0.01526 μM | SANGER | ||
| ES8 | Growth Inhibition Assay | IC50=0.01494 μM | SANGER | ||
| LS-411N | Growth Inhibition Assay | IC50=0.01407 μM | SANGER | ||
| GI-1 | Growth Inhibition Assay | IC50=0.01383 μM | SANGER | ||
| KM12 | Growth Inhibition Assay | IC50=0.01348 μM | SANGER | ||
| EW-16 | Growth Inhibition Assay | IC50=0.01336 μM | SANGER | ||
| ALL-PO | Growth Inhibition Assay | IC50=0.013 μM | SANGER | ||
| LC-2-ad | Growth Inhibition Assay | IC50=0.01093 μM | SANGER | ||
| TE-8 | Growth Inhibition Assay | IC50=0.00941 μM | SANGER | ||
| ACN | Growth Inhibition Assay | IC50=0.00843 μM | SANGER | ||
| PSN1 | Growth Inhibition Assay | IC50=0.00776 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 | ||
| 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 | ||
| DU145 | Growth Inhibition Assay | IC50∼60 nM | 23884428 | ||
| LNCaP | Growth Inhibition Assay | IC50∼75 nM | 23884428 | ||
| PC3 | Growth Inhibition Assay | 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 | ||
| KB-V1 | Growth Inhibition Assay | IC50=3.92 μM | 23593196 | ||
| Hec50co | Growth Inhibition Assay | IC50=5 nM | 23146687 | ||
| 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 | ||
| 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 | ||
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生物活性
| 製品説明 | BI-2536 is a potent Plk1 inhibitor with IC50 of 0.83 nM in a cell-free assay. BI-2536 inhibits Bromodomain 4 (BRD4) with Kd of 37 nM and potently suppresses c-Myc expression. BI-2536 induces apoptosis and attenuates autophagy. Phase 2. | ||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|
| 特性 | The first potent and selective Plk1 inhibitor that induces all hallmarks of Plk1 inhibition. | ||||||||||
| Targets |
|
| In Vitro | ||||
| 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, BI 2536 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. BI 2536 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. BI 2536 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. [1] Plk1 inhibition by BI 2536 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. [2] |
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| Kinase Assay | Plk1 in vitro kinase assay | |||
| Recombinant human Plk1 (residues 1-603) is expressed as N-terminal, GST-tagged fusion protein with a baculoviral expression system and purified by affinity chromatography with Glutathione-agarose. Enzyme activity assays for Plk1 are performed in the presence of serially diluted BI 2536 with 20 ng of recombinant kinase and 10 μg casein from bovine milk as the substrate. Kinase reactions are performed in a final volume of 60 μL for 45 minutes at 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). Reactions are terminated by the addition of 125 μL of ice-cold 5% TCA. After transfer of the precipitates to Multi-Screen mixed ester cellulose filter plates, plates are washed with 1% TCA and quantified radiometrically. Dose-response curve is used for calculating IC50 value. | ||||
| 細胞実験 | 細胞株 | HeLa, A43, SKOV-3, HT-29, K562, A549, Saos-2, MCF7, HCT116, COLO 205, Hep G2, Raji and PC-3 cells, etc. | ||
| 濃度 | Dissolved in DMSO, final concentrations ~1 μM | |||
| 反応時間 | 24 and 72 hours | |||
| 実験の流れ | Cells are exposed to various concentrations of BI 2536 for 24, and 72 hours. Cell growth is assessed by the measurement of Alamar Blue dye conversion in a fluorescence spectrophotometer. For determining the DNA content of the cultures, cell suspensions are fixed in 80% ethanol, treated for 5 minutes with 0.25% Triton X-100 in PBS, and incubated with 0.1% RNase and 10 μg/mL propidium iodide (PI) in PBS for 20 minutes at RT. Cell-cycle profiles are determined by flow cytometric analysis. |
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| 実験結果図 | Methods | Biomarkers | 結果図 | PMID |
| Western blot | Aurora B / pAurora B / pAurora C / pH3 / Cyclin B1 / Securin / pBcl-XL / MPM2 pPlk1 / Plk1 / pMyt1 pMEK / MEK / pERK / ERK / pRSK1 / RSK1 p-HH3 / PARP / Myc / p-Myc pro-caspase-8 / cleaved caspase-8 / cleaved caspase-3 / cleaved caspase-9 |
|
25169932 | |
| Immunofluorescence | Pericentrin / α-tubulin p-H2AX / propidium iodide |
|
21772266 | |
| Growth inhibition assay | Cell viability |
|
21772266 | |
| In Vivo | ||
| 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 BI 2536 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. BI 2536 treatment twice-weekly also leads to excellent tumor-growth in BxPC-3 and A549 models with T/C of 5% and 14%, respectively. [1] |
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|---|---|---|
| 動物実験 | 動物モデル | Female BomTac:NMRI-Foxn1nu mice injected subcutaneously with HCT 116, NCI-H460, or A549 cells |
| 投与量 | ~50 mg/kg | |
| 投与経路 | Injection i.v. once or twice per week | |
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| 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 |
化学情報
| 分子量 | 521.66 | 化学式 | C28H39N7O3 |
| CAS No. | 755038-02-9 | SDF | Download BI 2536 SDFをダウンロードする |
| Smiles | CCC1C(=O)N(C2=CN=C(N=C2N1C3CCCC3)NC4=C(C=C(C=C4)C(=O)NC5CCN(CC5)C)OC)C | ||
| 保管 | |||
|
In vitro |
Ethanol : 104 mg/mL DMSO : 96 mg/mL ( (184.02 mM)； 吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。) Water : Insoluble |
モル濃度計算器 |
|
in vivo Add solvents to the product individually and in order. |
投与溶液組成計算機 | ||||
実験計算
投与溶液組成計算機(クリア溶液)
ステップ１：実験データを入力してください。（実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します）
mg/kg
g
μL
匹
ステップ２：投与溶媒の組成を入力してください。（ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください）
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
計算結果：
投与溶媒濃度： mg/ml;
DMSOストック溶液調製方法： mg 試薬を μL DMSOに溶解する（濃度 mg/mL, 注：濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )
投与溶媒調製方法：Take μL DMSOストック溶液に μL PEG300，を加え、完全溶解後μL Tween 80，を加えて完全溶解させた後 μL ddH2O，を加え完全に溶解させます。
投与溶媒調製方法：μL DMSOストック溶液に μL Corn oil，を加え、完全溶解。
注意：１.ストック溶液に沈殿、混濁などがないことをご確認ください；
２.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。
技術サポート
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* 必須
よくある質問（FAQ）
質問1:
We need to use BI 2536 in preclinical studies using mice, how to formulate the inhibitor for this in vivo study?
回答
For in vivo study, DMSO should not be more than 5% because the toxicity. You can formulated BI2536 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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