BI 2536
BI-2536是一种有效的Plk1抑制剂，无细胞试验中IC50为0.83 nM。BI-2536可抑制 Bromodomain 4 (BRD4) ，其Kd值为37 nM，并有效地抑制 c-Myc 的表达。BI-2536可诱导凋亡而减弱自噬。Phase 2。
BI 2536 Chemical Structure
CAS: 755038-02-9
客户使用Selleck的BI 2536发表文献280篇
产品质控
批次：
纯度：
99.9%
99.9
BI 2536相关产品
| 相关靶点 | PLK1 PLK2 PLK3 PLK4 | 点击展开 |
|---|---|---|
| 相关产品 | Volasertib Rigosertib (ON-01910) GSK461364 Onvansertib (NMS-P937) SBE 13 HCl Ro3280 CFI-400945 HMN-214 MLN0905 Poloxin | 点击展开 |
| 相关化合物库 | 激酶抑制剂库 PI3K/Akt 抑制剂库 MAPK抑制剂库 DNA损伤/ DNA修复化合物库 细胞周期化合物库 | 点击展开 |
相关信号通路图
PLK抑制剂选择性比较
细胞实验数据示例
| 细胞系 | 实验类型 | 给药浓度 | 孵育时间 | 活性描述 | 文献信息 |
|---|---|---|---|---|---|
| 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 | ||
| 点击查看更多细胞系数据 | |||||
生物活性
| 产品描述 | BI-2536是一种有效的Plk1抑制剂，无细胞试验中IC50为0.83 nM。BI-2536可抑制 Bromodomain 4 (BRD4) ，其Kd值为37 nM，并有效地抑制 c-Myc 的表达。BI-2536可诱导凋亡而减弱自噬。Phase 2。 | ||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|
| 特性 | BI 2536是第一个有效的Plk1选择性抑制剂，抑制 Plk1的标记。 | ||||||||||
| 靶点 |
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| 体外研究(In Vitro) | ||||
| 体外研究活性 | 除了Plk1, BI 2536也抑制 Plk2 和Plk3活性，只是抑制程度低点,IC50分别为3.5 nM和9.0 nM。BI 2536比一组63种其他蛋白激酶（IC50>10 μM）选择性高1000多倍。BI 2536 按10 nM 到 100 nM剂量作用于HeLa细胞，抑制有丝分裂中心体中γ-微管蛋白招募和Apc6 磷酸化，抑制染色体臂中释放黏结蛋白, 诱导产生单极主轴，及一些依赖Plk1的其他有丝分裂过程。与作用于Plk1 RNAi效果相一致, BI 2536处理HeLa细胞，使细胞周期停在G2/M期, 随后DNA分解及凋亡，且累积断裂的PARP p85片段，这种作用存在浓度依赖性。BI 2536抑制一组32种人肿瘤细胞系生长，EC50为2-25 nM,抑制指数生长的hTERT-RPE1,人脐静脉内皮细胞 (HUVECs),和正常大鼠肾脏(NRK) 细胞的增殖，EC50为12-31 nM。[1] BI 2536 抑制Plk1，降低甲状腺未分化癌(ATC)细胞如 CAL62, OCUT-1, SW1736, 8505C,和 ACT-1 的生长的生长和活力，EC50为1.4-5.6 nM。[2] |
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|---|---|---|---|---|
| 激酶实验 | 体外Plk1激酶实验 | |||
| 重组人Plk1 (1-603残基) 作为氮端，携带杆状病毒表达系统的GST-标记的融合蛋白通过亲和层析，使用谷胱甘肽-琼脂糖而纯化。在梯度稀释的BI 2536存在时，使用 20 ng 重组激酶，及10 μg牛奶中的酪蛋白作为底物进行Plk1 酶活性实验。在终体积为60 μL 的混合物(15 mM MgCl2, 25 mM MOPS [pH 7.0], 1 mM DTT, 1% DMSO, 7.5 mM ATP, 0.3 μCi γ-33P-ATP)中30oC下进行激酶反应45分钟。加入 125 μL 冰冻的5% TCA终止反应。沉淀物转移到混合酯纤维素的多屏过滤板上，使用1% TCA冲洗实验板，然后利用放射性进行测量。绘制剂量反应曲线，而计算IC50值。 | ||||
| 细胞实验 | 细胞系 | HeLa, A43, SKOV-3, HT-29, K562, A549, Saos-2, MCF7, HCT116, COLO 205, Hep G2, Raji, PC-3,等等 | ||
| 浓度 | 溶于DMSO, 终浓度为~1 μM | |||
| 孵育时间 | 24,和72小时 | |||
| 方法 | 使用不同浓度BI 2536处理细胞24和72小时。 在荧光分光光度计中测量Alamar Blue染料转换而测定细胞生长。为了测定培养基中DNA含量，细胞悬液在80%乙醇中混合, 使用溶于PBS的0.25% Triton X-100处理5分钟，然后与0.1% RNase 和溶于PBS的 10 μg/mL碘化丙啶在室温下温育20分钟。通过流式细胞仪分析而测定细胞周期谱。 |
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| 实验图片 | 检测方法 | 检测指标 | 实验图片 | 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 | |
| 体内研究(In Vivo) | ||
| 体内研究活性 |
BI 2536静脉注射给药多种移植瘤模型，每周一次或两次，效果都很好，通过使细胞周期停滞而抑制细胞增殖，随后诱导肿瘤细胞死亡。BI 2536按 50 mg/kg剂量处理HCT 116移植瘤，每周一次或两次，显著抑制肿瘤生长，T/C 分别为15%和0.3%。BI 2536每周处理两次BxPC-3和A549模型，也显著抑制肿瘤生长，T/C分别为5% 和14%。[1] |
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|---|---|---|
| 动物实验 | Animal Models | 皮下注射HCT 116, NCI-H460, 或A549 细胞的雌性BomTac:NMRI-Foxn1nu 小鼠 |
| Dosages | ~50 mg/kg | |
| Administration | 静脉注射，每周一到两次 | |
| 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 |
化学信息&溶解度
| 分子量 | 521.66 | 分子式 | C28H39N7O3 |
| CAS号 | 755038-02-9 | SDF | Download BI 2536 SDF |
| Smiles | CCC1C(=O)N(C2=CN=C(N=C2N1C3CCCC3)NC4=C(C=C(C=C4)C(=O)NC5CCN(CC5)C)OC)C | ||
| 储存条件(自收到货起) | |||
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体外溶解度 |
DMSO : 104 mg/mL ( (199.36 mM)； DMSO吸湿会降低化合物溶解度，请使用新开封DMSO) Ethanol : 104 mg/mL Water : Insoluble |
摩尔浓度计算器 |
|
体内溶解度 现配现用，请按从左到右的顺序依次添加，澄清后再加入下一溶剂 |
动物体内配方计算器 | ||||
实验计算
动物体内配方计算器（澄清溶液）
第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）
mg/kg
g
μL
只
第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系Selleck为您提供正确的澄清溶液配方）
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
计算结果：
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于μL DMSO溶液（母液浓度mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系Selleck）；
体内配方配制方法：取μL DMSO母液，加入μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入μL ddH2O，混匀澄清。
体内配方配制方法：取μL DMSO母液，加入μL Corn oil，混匀澄清。
注意：1. 首先保证母液是澄清的；
2.一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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常见问题及建议解决方法
问题 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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