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PD184352 (CI-1040)
PD184352 (CI-1040) 是一種ATP非競爭性的MEK1/2抑制劑，細胞試驗中IC50為17 nM，對MEK1/2的選擇性比MEK5高100倍。PD184352 (CI-1040)可選擇性地誘導凋亡。
PD184352 (CI-1040) Chemical Structure
CAS: 212631-79-3
產品質控
批次：
純度：
99.96%
99.96
PD184352 (CI-1040)相關產品
相關信號通路圖
細胞實驗數據示例
| 細胞系 | 實驗類型 | 給藥濃度 | 孵育時間 | 活性描述 | 文獻信息 |
|---|---|---|---|---|---|
| U937 | Cytotoxicity assay | 30 uM | Cytotoxicity against human U937 cells assessed as inhibition of [3H]thymidine incorporation at 30 uM by MTS assay | 20580230 | |
| U937 | Function assay | 3 uM | Inhibition of ERK phosphorylation in human U937 cells at 3 uM by Western blotting | 20580230 | |
| U937 | Function assay | 3 uM | Inhibition of RSK1 phosphorylation in human U937 cells at 3 uM by Western blotting | 20580230 | |
| U937 | Cytotoxicity assay | 10 uM | Cytotoxicity against human U937 cells assessed as cell death at 10 uM by 7-AAD assay | 20580230 | |
| K-Balb | Function assay | 1 hr | Inhibition of MEK-mediated ERK phosphorylation in PDGF-stimulated mouse K-Balb cells treated as single oral dose preincubated for 1 hr before PDGF challenge by whole cell assay, IC50=0.00245μM | 18952427 | |
| K-Balb | Function assay | 24 hrs | Inhibition of MEK-mediated ERK phosphorylation in PDGF-stimulated mouse K-Balb cells treated as single oral dose preincubated for 24 hrs before PDGF challenge by whole cell assay, IC50=0.0354μM | 18952427 | |
| U937 | Cell cycle assay | 24 hrs | Cell cycle arrest in human U937 cells assessed as decrease in S-phase population after 24 hrs by propidium iodide staining-based flow cytometric analysis in presence of MEK inhibitor PD184352 | 22074985 | |
| U937 | Cell cycle assay | 24 hrs | Cell cycle arrest in human U937 cells assessed as accumulation at G2/M-phase after 24 hrs by propidium iodide staining-based flow cytometric analysis in presence of MEK inhibitor PD184352 | 22074985 | |
| 786-0 | Function assay | 24 hrs | Inhibition of CK2 in human 786-0 cells assessed as decrease in Akt1 phosphorylation at Ser129 after 24 hrs by Western blot analysis, EC50=0.1μM | 30689946 | |
| NCI-H1355 | Growth Inhibition Assay | IC50=7.58635 μM | SANGER | ||
| NB14 | Growth Inhibition Assay | IC50=7.66642 μM | SANGER | ||
| SCC-25 | Growth Inhibition Assay | IC50=7.709 μM | SANGER | ||
| COLO-678 | Growth Inhibition Assay | IC50=7.71076 μM | SANGER | ||
| TGBC1TKB | Growth Inhibition Assay | IC50=7.89398 μM | SANGER | ||
| IST-MEL1 | Growth Inhibition Assay | IC50=8.00406 μM | SANGER | ||
| ECC10 | Growth Inhibition Assay | IC50=8.03395 μM | SANGER | ||
| EW-16 | Growth Inhibition Assay | IC50=8.08445 μM | SANGER | ||
| DOHH-2 | Growth Inhibition Assay | IC50=8.20095 μM | SANGER | ||
| NCI-H1581 | Growth Inhibition Assay | IC50=8.26323 μM | SANGER | ||
| TE-5 | Growth Inhibition Assay | IC50=8.42429 μM | SANGER | ||
| CAKI-1 | Growth Inhibition Assay | IC50=8.57222 μM | SANGER | ||
| A673 | Growth Inhibition Assay | IC50=8.63202 μM | SANGER | ||
| CAL-12T | Growth Inhibition Assay | IC50=8.65753 μM | SANGER | ||
| DBTRG-05MG | Growth Inhibition Assay | IC50=8.74859 μM | SANGER | ||
| SK-N-FI | Growth Inhibition Assay | IC50=8.81379 μM | SANGER | ||
| K-562 | Growth Inhibition Assay | IC50=8.83957 μM | SANGER | ||
| SBC-1 | Growth Inhibition Assay | IC50=8.86645 μM | SANGER | ||
| ES4 | Growth Inhibition Assay | IC50=8.86884 μM | SANGER | ||
| MS-1 | Growth Inhibition Assay | IC50=8.87517 μM | SANGER | ||
| RKO | Growth Inhibition Assay | IC50=8.89057 μM | SANGER | ||
| NCI-H1693 | Growth Inhibition Assay | IC50=8.9217 μM | SANGER | ||
| SW954 | Growth Inhibition Assay | IC50=8.96978 μM | SANGER | ||
| SK-UT-1 | Growth Inhibition Assay | IC50=8.97683 μM | SANGER | ||
| T98G | Growth Inhibition Assay | IC50=8.99846 μM | SANGER | ||
| NCI-H2126 | Growth Inhibition Assay | IC50=9.00826 μM | SANGER | ||
| TE-12 | Growth Inhibition Assay | IC50=9.03367 μM | SANGER | ||
| DK-MG | Growth Inhibition Assay | IC50=9.21191 μM | SANGER | ||
| MEG-01 | Growth Inhibition Assay | IC50=9.24931 μM | SANGER | ||
| HCC1937 | Growth Inhibition Assay | IC50=9.29091 μM | SANGER | ||
| MKN45 | Growth Inhibition Assay | IC50=9.45065 μM | SANGER | ||
| NCI-H1792 | Growth Inhibition Assay | IC50=9.45219 μM | SANGER | ||
| SW1417 | Growth Inhibition Assay | IC50=9.56837 μM | SANGER | ||
| 639-V | Growth Inhibition Assay | IC50=9.64388 μM | SANGER | ||
| P30-OHK | Growth Inhibition Assay | IC50=9.65316 μM | SANGER | ||
| YKG-1 | Growth Inhibition Assay | IC50=9.75033 μM | SANGER | ||
| KGN | Growth Inhibition Assay | IC50=9.83795 μM | SANGER | ||
| MSTO-211H | Growth Inhibition Assay | IC50=9.95529 μM | SANGER | ||
| NCI-H1573 | Growth Inhibition Assay | IC50=10.1574 μM | SANGER | ||
| NCI-H720 | Growth Inhibition Assay | IC50=10.1989 μM | SANGER | ||
| KARPAS-45 | Growth Inhibition Assay | IC50=10.2795 μM | SANGER | ||
| MDA-MB-175-VII | Growth Inhibition Assay | IC50=10.48 μM | SANGER | ||
| SK-NEP-1 | Growth Inhibition Assay | IC50=10.4981 μM | SANGER | ||
| MKN28 | Growth Inhibition Assay | IC50=10.518 μM | SANGER | ||
| KYSE-520 | Growth Inhibition Assay | IC50=10.52 μM | SANGER | ||
| KE-37 | Growth Inhibition Assay | IC50=10.5272 μM | SANGER | ||
| VA-ES-BJ | Growth Inhibition Assay | IC50=10.567 μM | SANGER | ||
| CCRF-CEM | Growth Inhibition Assay | IC50=10.5684 μM | SANGER | ||
| GMS-10 | Growth Inhibition Assay | IC50=10.6094 μM | SANGER | ||
| NCI-H1623 | Growth Inhibition Assay | IC50=10.6379 μM | SANGER | ||
| NEC8 | Growth Inhibition Assay | IC50=10.7773 μM | SANGER | ||
| MOLT-16 | Growth Inhibition Assay | IC50=10.8113 μM | SANGER | ||
| DJM-1 | Growth Inhibition Assay | IC50=11.0379 μM | SANGER | ||
| U251 | Growth Inhibition Assay | IC50=11.042 μM | SANGER | ||
| SBC-5 | Growth Inhibition Assay | IC50=11.1467 μM | SANGER | ||
| SW756 | Growth Inhibition Assay | IC50=11.2154 μM | SANGER | ||
| KS-1 | Growth Inhibition Assay | IC50=11.2619 μM | SANGER | ||
| SF295 | Growth Inhibition Assay | IC50=11.3104 μM | SANGER | ||
| YH-13 | Growth Inhibition Assay | IC50=11.3267 μM | SANGER | ||
| SW837 | Growth Inhibition Assay | IC50=11.3506 μM | SANGER | ||
| KYSE-450 | Growth Inhibition Assay | IC50=11.4057 μM | SANGER | ||
| KYSE-180 | Growth Inhibition Assay | IC50=11.482 μM | SANGER | ||
| S-117 | Growth Inhibition Assay | IC50=11.4896 μM | SANGER | ||
| KOSC-2 | Growth Inhibition Assay | IC50=11.6222 μM | SANGER | ||
| KYSE-270 | Growth Inhibition Assay | IC50=11.8745 μM | SANGER | ||
| D-336MG | Growth Inhibition Assay | IC50=11.9075 μM | SANGER | ||
| KALS-1 | Growth Inhibition Assay | IC50=12.0016 μM | SANGER | ||
| LB373-MEL-D | Growth Inhibition Assay | IC50=12.0533 μM | SANGER | ||
| HLE | Growth Inhibition Assay | IC50=12.0585 μM | SANGER | ||
| SJSA-1 | Growth Inhibition Assay | IC50=12.0735 μM | SANGER | ||
| SW1990 | Growth Inhibition Assay | IC50=12.0911 μM | SANGER | ||
| NOS-1 | Growth Inhibition Assay | IC50=12.1352 μM | SANGER | ||
| GI-ME-N | Growth Inhibition Assay | IC50=12.2163 μM | SANGER | ||
| NCI-H1703 | Growth Inhibition Assay | IC50=12.2616 μM | SANGER | ||
| ES7 | Growth Inhibition Assay | IC50=12.2724 μM | SANGER | ||
| KYSE-510 | Growth Inhibition Assay | IC50=12.5079 μM | SANGER | ||
| BHY | Growth Inhibition Assay | IC50=12.5307 μM | SANGER | ||
| TCCSUP | Growth Inhibition Assay | IC50=12.5757 μM | SANGER | ||
| HSC-2 | Growth Inhibition Assay | IC50=12.5996 μM | SANGER | ||
| BEN | Growth Inhibition Assay | IC50=12.6143 μM | SANGER | ||
| 769-P | Growth Inhibition Assay | IC50=12.7924 μM | SANGER | ||
| HT | Growth Inhibition Assay | IC50=12.8346 μM | SANGER | ||
| LXF-289 | Growth Inhibition Assay | IC50=12.9531 μM | SANGER | ||
| OVCAR-3 | Growth Inhibition Assay | IC50=12.9567 μM | SANGER | ||
| ATN-1 | Growth Inhibition Assay | IC50=13.0184 μM | SANGER | ||
| 8-MG-BA | Growth Inhibition Assay | IC50=13.0455 μM | SANGER | ||
| SW13 | Growth Inhibition Assay | IC50=13.1165 μM | SANGER | ||
| NCI-H1092 | Growth Inhibition Assay | IC50=13.162 μM | SANGER | ||
| OAW-42 | Growth Inhibition Assay | IC50=13.1937 μM | SANGER | ||
| NCI-H2452 | Growth Inhibition Assay | IC50=13.2175 μM | SANGER | ||
| CAPAN-1 | Growth Inhibition Assay | IC50=13.5514 μM | SANGER | ||
| NCI-H2009 | Growth Inhibition Assay | IC50=13.5919 μM | SANGER | ||
| SF268 | Growth Inhibition Assay | IC50=13.6326 μM | SANGER | ||
| GCIY | Growth Inhibition Assay | IC50=13.6927 μM | SANGER | ||
| OS-RC-2 | Growth Inhibition Assay | IC50=13.9501 μM | SANGER | ||
| GCT | Growth Inhibition Assay | IC50=13.9697 μM | SANGER | ||
| NB17 | Growth Inhibition Assay | IC50=14.085 μM | SANGER | ||
| NCI-H2030 | Growth Inhibition Assay | IC50=14.1465 μM | SANGER | ||
| HC-1 | Growth Inhibition Assay | IC50=14.2087 μM | SANGER | ||
| QIMR-WIL | Growth Inhibition Assay | IC50=14.3412 μM | SANGER | ||
| Capan-2 | Growth Inhibition Assay | IC50=14.3714 μM | SANGER | ||
| BALL-1 | Growth Inhibition Assay | IC50=14.4665 μM | SANGER | ||
| LS-1034 | Growth Inhibition Assay | IC50=14.6152 μM | SANGER | ||
| U-118-MG | Growth Inhibition Assay | IC50=14.631 μM | SANGER | ||
| NCI-H630 | Growth Inhibition Assay | IC50=14.6568 μM | SANGER | ||
| OVCAR-8 | Growth Inhibition Assay | IC50=14.7201 μM | SANGER | ||
| NCI-H2347 | Growth Inhibition Assay | IC50=14.823 μM | SANGER | ||
| BT-549 | Growth Inhibition Assay | IC50=14.8284 μM | SANGER | ||
| LB831-BLC | Growth Inhibition Assay | IC50=14.8934 μM | SANGER | ||
| NCI-H661 | Growth Inhibition Assay | IC50=14.959 μM | SANGER | ||
| MKN7 | Growth Inhibition Assay | IC50=15.0093 μM | SANGER | ||
| U-87-MG | Growth Inhibition Assay | IC50=15.0897 μM | SANGER | ||
| OVCAR-4 | Growth Inhibition Assay | IC50=15.1424 μM | SANGER | ||
| OE33 | Growth Inhibition Assay | IC50=15.1711 μM | SANGER | ||
| EC-GI-10 | Growth Inhibition Assay | IC50=15.2357 μM | SANGER | ||
| AM-38 | Growth Inhibition Assay | IC50=15.2717 μM | SANGER | ||
| NCI-H1563 | Growth Inhibition Assay | IC50=15.349 μM | SANGER | ||
| SCC-4 | Growth Inhibition Assay | IC50=15.4103 μM | SANGER | ||
| Detroit562 | Growth Inhibition Assay | IC50=15.4547 μM | SANGER | ||
| PC-14 | Growth Inhibition Assay | IC50=15.4866 μM | SANGER | ||
| ES3 | Growth Inhibition Assay | IC50=15.536 μM | SANGER | ||
| OCI-AML2 | Growth Inhibition Assay | IC50=15.7614 μM | SANGER | ||
| LU-134-A | Growth Inhibition Assay | IC50=15.9018 μM | SANGER | ||
| SAS | Growth Inhibition Assay | IC50=15.9373 μM | SANGER | ||
| TGBC11TKB | Growth Inhibition Assay | IC50=15.9414 μM | SANGER | ||
| HOP-62 | Growth Inhibition Assay | IC50=15.9597 μM | SANGER | ||
| G-401 | Growth Inhibition Assay | IC50=15.9649 μM | SANGER | ||
| NCI-H28 | Growth Inhibition Assay | IC50=16.0856 μM | SANGER | ||
| A204 | Growth Inhibition Assay | IC50=16.2006 μM | SANGER | ||
| NCI-H1299 | Growth Inhibition Assay | IC50=16.2291 μM | SANGER | ||
| VMRC-RCZ | Growth Inhibition Assay | IC50=16.2592 μM | SANGER | ||
| BxPC-3 | Growth Inhibition Assay | IC50=16.2856 μM | SANGER | ||
| NCI-H2228 | Growth Inhibition Assay | IC50=16.5158 μM | SANGER | ||
| NCI-H23 | Growth Inhibition Assay | IC50=16.6078 μM | SANGER | ||
| NKM-1 | Growth Inhibition Assay | IC50=17.0189 μM | SANGER | ||
| KYSE-70 | Growth Inhibition Assay | IC50=17.289 μM | SANGER | ||
| BB49-HNC | Growth Inhibition Assay | IC50=17.5686 μM | SANGER | ||
| SCC-15 | Growth Inhibition Assay | IC50=17.8473 μM | SANGER | ||
| D-247MG | Growth Inhibition Assay | IC50=17.9247 μM | SANGER | ||
| BB30-HNC | Growth Inhibition Assay | IC50=18.0318 μM | SANGER | ||
| CAL-85-1 | Growth Inhibition Assay | IC50=18.1809 μM | SANGER | ||
| HT-3 | Growth Inhibition Assay | IC50=18.3977 μM | SANGER | ||
| KYSE-410 | Growth Inhibition Assay | IC50=18.4577 μM | SANGER | ||
| SW982 | Growth Inhibition Assay | IC50=18.5649 μM | SANGER | ||
| SW962 | Growth Inhibition Assay | IC50=18.5702 μM | SANGER | ||
| Ramos-2G6-4C10 | Growth Inhibition Assay | IC50=18.5927 μM | SANGER | ||
| OC-314 | Growth Inhibition Assay | IC50=18.7384 μM | SANGER | ||
| LS-123 | Growth Inhibition Assay | IC50=18.7901 μM | SANGER | ||
| D-502MG | Growth Inhibition Assay | IC50=18.8139 μM | SANGER | ||
| RO82-W-1 | Growth Inhibition Assay | IC50=18.8288 μM | SANGER | ||
| HuO9 | Growth Inhibition Assay | IC50=19.1379 μM | SANGER | ||
| ETK-1 | Growth Inhibition Assay | IC50=19.1827 μM | SANGER | ||
| SNU-387 | Growth Inhibition Assay | IC50=19.1889 μM | SANGER | ||
| SW1573 | Growth Inhibition Assay | IC50=19.1969 μM | SANGER | ||
| NTERA-S-cl-D1 | Growth Inhibition Assay | IC50=19.2007 μM | SANGER | ||
| SF126 | Growth Inhibition Assay | IC50=19.3502 μM | SANGER | ||
| Calu-3 | Growth Inhibition Assay | IC50=19.4237 μM | SANGER | ||
| NCI-H1048 | Growth Inhibition Assay | IC50=20.3266 μM | SANGER | ||
| NCI-H226 | Growth Inhibition Assay | IC50=20.4399 μM | SANGER | ||
| FTC-133 | Growth Inhibition Assay | IC50=20.4703 μM | SANGER | ||
| SF539 | Growth Inhibition Assay | IC50=20.5172 μM | SANGER | ||
| TE-6 | Growth Inhibition Assay | IC50=20.8067 μM | SANGER | ||
| UMC-11 | Growth Inhibition Assay | IC50=20.9164 μM | SANGER | ||
| Becker | Growth Inhibition Assay | IC50=21.1118 μM | SANGER | ||
| KP-4 | Growth Inhibition Assay | IC50=21.1196 μM | SANGER | ||
| ChaGo-K-1 | Growth Inhibition Assay | IC50=21.3627 μM | SANGER | ||
| CFPAC-1 | Growth Inhibition Assay | IC50=21.3858 μM | SANGER | ||
| A498 | Growth Inhibition Assay | IC50=21.5312 μM | SANGER | ||
| NCI-H1755 | Growth Inhibition Assay | IC50=21.6741 μM | SANGER | ||
| TI-73 | Growth Inhibition Assay | IC50=22.328 μM | SANGER | ||
| NCI-H441 | Growth Inhibition Assay | IC50=22.5689 μM | SANGER | ||
| CaR-1 | Growth Inhibition Assay | IC50=23.0213 μM | SANGER | ||
| HCC1806 | Growth Inhibition Assay | IC50=23.0583 μM | SANGER | ||
| SNU-449 | Growth Inhibition Assay | IC50=23.329 μM | SANGER | ||
| EKVX | Growth Inhibition Assay | IC50=23.3909 μM | SANGER | ||
| DMS-114 | Growth Inhibition Assay | IC50=23.5765 μM | SANGER | ||
| A704 | Growth Inhibition Assay | IC50=23.6103 μM | SANGER | ||
| LC-2-ad | Growth Inhibition Assay | IC50=23.6147 μM | SANGER | ||
| VM-CUB-1 | Growth Inhibition Assay | IC50=23.7341 μM | SANGER | ||
| PC-3 | Growth Inhibition Assay | IC50=24.0526 μM | SANGER | ||
| U-266 | Growth Inhibition Assay | IC50=7.56286 μM | SANGER | ||
| LU-135 | Growth Inhibition Assay | IC50=7.55939 μM | SANGER | ||
| GR-ST | Growth Inhibition Assay | IC50=7.40174 μM | SANGER | ||
| BE-13 | Growth Inhibition Assay | IC50=7.33834 μM | SANGER | ||
| SK-MEL-30 | Growth Inhibition Assay | IC50=7.25083 μM | SANGER | ||
| COR-L23 | Growth Inhibition Assay | IC50=7.2442 μM | SANGER | ||
| DoTc2-4510 | Growth Inhibition Assay | IC50=7.1215 μM | SANGER | ||
| 8305C | Growth Inhibition Assay | IC50=7.09995 μM | SANGER | ||
| ACHN | Growth Inhibition Assay | IC50=7.02943 μM | SANGER | ||
| HuCCT1 | Growth Inhibition Assay | IC50=7.01037 μM | SANGER | ||
| SW48 | Growth Inhibition Assay | IC50=6.9451 μM | SANGER | ||
| SW1088 | Growth Inhibition Assay | IC50=6.91913 μM | SANGER | ||
| MFE-280 | Growth Inhibition Assay | IC50=6.85983 μM | SANGER | ||
| MHH-NB-11 | Growth Inhibition Assay | IC50=6.85002 μM | SANGER | ||
| HCT-116 | Growth Inhibition Assay | IC50=6.81264 μM | SANGER | ||
| Calu-6 | Growth Inhibition Assay | IC50=6.79698 μM | SANGER | ||
| AN3-CA | Growth Inhibition Assay | IC50=6.68641 μM | SANGER | ||
| COR-L105 | Growth Inhibition Assay | IC50=6.65275 μM | SANGER | ||
| NCI-H2122 | Growth Inhibition Assay | IC50=6.61528 μM | SANGER | ||
| D-566MG | Growth Inhibition Assay | IC50=6.54303 μM | SANGER | ||
| A172 | Growth Inhibition Assay | IC50=6.49176 μM | SANGER | ||
| NCI-H1975 | Growth Inhibition Assay | IC50=6.47215 μM | SANGER | ||
| TK10 | Growth Inhibition Assay | IC50=6.32604 μM | SANGER | ||
| PANC-10-05 | Growth Inhibition Assay | IC50=6.28363 μM | SANGER | ||
| A431 | Growth Inhibition Assay | IC50=6.24296 μM | SANGER | ||
| MV-4-11 | Growth Inhibition Assay | IC50=6.23199 μM | SANGER | ||
| RPMI-8866 | Growth Inhibition Assay | IC50=6.21313 μM | SANGER | ||
| NCI-H1304 | Growth Inhibition Assay | IC50=6.1994 μM | SANGER | ||
| NCI-H1666 | Growth Inhibition Assay | IC50=6.08461 μM | SANGER | ||
| KYSE-140 | Growth Inhibition Assay | IC50=6.02182 μM | SANGER | ||
| HT-29 | Growth Inhibition Assay | IC50=5.98118 μM | SANGER | ||
| SK-HEP-1 | Growth Inhibition Assay | IC50=5.93471 μM | SANGER | ||
| NB10 | Growth Inhibition Assay | IC50=5.8946 μM | SANGER | ||
| D-263MG | Growth Inhibition Assay | IC50=5.88351 μM | SANGER | ||
| SK-MES-1 | Growth Inhibition Assay | IC50=5.83528 μM | SANGER | ||
| MEL-JUSO | Growth Inhibition Assay | IC50=5.7378 μM | SANGER | ||
| RERF-LC-MS | Growth Inhibition Assay | IC50=5.68803 μM | SANGER | ||
| TE-8 | Growth Inhibition Assay | IC50=5.68537 μM | SANGER | ||
| RS4-11 | Growth Inhibition Assay | IC50=5.66775 μM | SANGER | ||
| LU-99A | Growth Inhibition Assay | IC50=5.66451 μM | SANGER | ||
| PA-1 | Growth Inhibition Assay | IC50=5.64265 μM | SANGER | ||
| HOS | Growth Inhibition Assay | IC50=5.62923 μM | SANGER | ||
| HuP-T3 | Growth Inhibition Assay | IC50=5.62029 μM | SANGER | ||
| SW1710 | Growth Inhibition Assay | IC50=5.61654 μM | SANGER | ||
| ME-180 | Growth Inhibition Assay | IC50=5.58092 μM | SANGER | ||
| NBsusSR | Growth Inhibition Assay | IC50=5.57155 μM | SANGER | ||
| FADU | Growth Inhibition Assay | IC50=5.55726 μM | SANGER | ||
| Hs-578-T | Growth Inhibition Assay | IC50=5.53794 μM | SANGER | ||
| NUGC-3 | Growth Inhibition Assay | IC50=5.49302 μM | SANGER | ||
| HCC2998 | Growth Inhibition Assay | IC50=5.49109 μM | SANGER | ||
| GT3TKB | Growth Inhibition Assay | IC50=5.46598 μM | SANGER | ||
| NCI-H1155 | Growth Inhibition Assay | IC50=5.40051 μM | SANGER | ||
| AsPC-1 | Growth Inhibition Assay | IC50=5.36763 μM | SANGER | ||
| BCPAP | Growth Inhibition Assay | IC50=5.32969 μM | SANGER | ||
| HuH-7 | Growth Inhibition Assay | IC50=5.27147 μM | SANGER | ||
| UM-UC-3 | Growth Inhibition Assay | IC50=5.18047 μM | SANGER | ||
| 23132-87 | Growth Inhibition Assay | IC50=5.16872 μM | SANGER | ||
| CAL-33 | Growth Inhibition Assay | IC50=5.12317 μM | SANGER | ||
| MOLT-13 | Growth Inhibition Assay | IC50=5.06776 μM | SANGER | ||
| H4 | Growth Inhibition Assay | IC50=5.04255 μM | SANGER | ||
| CAL-54 | Growth Inhibition Assay | IC50=5.02695 μM | SANGER | ||
| EPLC-272H | Growth Inhibition Assay | IC50=4.99669 μM | SANGER | ||
| EFO-27 | Growth Inhibition Assay | IC50=4.78667 μM | SANGER | ||
| LB1047-RCC | Growth Inhibition Assay | IC50=4.73815 μM | SANGER | ||
| NH-12 | Growth Inhibition Assay | IC50=4.71625 μM | SANGER | ||
| NCI-H747 | Growth Inhibition Assay | IC50=4.68807 μM | SANGER | ||
| NB5 | Growth Inhibition Assay | IC50=4.60369 μM | SANGER | ||
| NCI-H358 | Growth Inhibition Assay | IC50=4.45385 μM | SANGER | ||
| IGROV-1 | Growth Inhibition Assay | IC50=4.45171 μM | SANGER | ||
| HH | Growth Inhibition Assay | IC50=4.41597 μM | SANGER | ||
| ALL-PO | Growth Inhibition Assay | IC50=4.36156 μM | SANGER | ||
| LAN-6 | Growth Inhibition Assay | IC50=4.31637 μM | SANGER | ||
| MDA-MB-231 | Growth Inhibition Assay | IC50=4.29223 μM | SANGER | ||
| HOP-92 | Growth Inhibition Assay | IC50=4.2567 μM | SANGER | ||
| RPMI-7951 | Growth Inhibition Assay | IC50=4.25589 μM | SANGER | ||
| MHH-PREB-1 | Growth Inhibition Assay | IC50=4.12111 μM | SANGER | ||
| CAL-62 | Growth Inhibition Assay | IC50=4.0743 μM | SANGER | ||
| SW626 | Growth Inhibition Assay | IC50=4.0448 μM | SANGER | ||
| GAMG | Growth Inhibition Assay | IC50=4.02377 μM | SANGER | ||
| 8505C | Growth Inhibition Assay | IC50=3.90078 μM | SANGER | ||
| CGTH-W-1 | Growth Inhibition Assay | IC50=3.85725 μM | SANGER | ||
| SK-MEL-3 | Growth Inhibition Assay | IC50=3.85154 μM | SANGER | ||
| NCI-H2087 | Growth Inhibition Assay | IC50=3.84672 μM | SANGER | ||
| HPAF-II | Growth Inhibition Assay | IC50=3.7549 μM | SANGER | ||
| 697 | Growth Inhibition Assay | IC50=3.69603 μM | SANGER | ||
| SK-LU-1 | Growth Inhibition Assay | IC50=3.68798 μM | SANGER | ||
| NCI-SNU-5 | Growth Inhibition Assay | IC50=3.6773 μM | SANGER | ||
| U-2-OS | Growth Inhibition Assay | IC50=3.67256 μM | SANGER | ||
| EGI-1 | Growth Inhibition Assay | IC50=3.60583 μM | SANGER | ||
| A427 | Growth Inhibition Assay | IC50=3.59556 μM | SANGER | ||
| CTB-1 | Growth Inhibition Assay | IC50=3.47047 μM | SANGER | ||
| PANC-03-27 | Growth Inhibition Assay | IC50=3.35045 μM | SANGER | ||
| GAK | Growth Inhibition Assay | IC50=3.32561 μM | SANGER | ||
| 786-0 | Growth Inhibition Assay | IC50=3.27243 μM | SANGER | ||
| SN12C | Growth Inhibition Assay | IC50=3.24701 μM | SANGER | ||
| HSC-3 | Growth Inhibition Assay | IC50=3.23151 μM | SANGER | ||
| COLO-741 | Growth Inhibition Assay | IC50=3.18673 μM | SANGER | ||
| KU-19-19 | Growth Inhibition Assay | IC50=3.17034 μM | SANGER | ||
| SW780 | Growth Inhibition Assay | IC50=3.14229 μM | SANGER | ||
| LAMA-84 | Growth Inhibition Assay | IC50=3.1358 μM | SANGER | ||
| D-423MG | Growth Inhibition Assay | IC50=3.07753 μM | SANGER | ||
| HT-1080 | Growth Inhibition Assay | IC50=3.01997 μM | SANGER | ||
| MIA-PaCa-2 | Growth Inhibition Assay | IC50=3.00781 μM | SANGER | ||
| Ca9-22 | Growth Inhibition Assay | IC50=2.97255 μM | SANGER | ||
| NCI-H727 | Growth Inhibition Assay | IC50=2.91796 μM | SANGER | ||
| T-24 | Growth Inhibition Assay | IC50=2.91112 μM | SANGER | ||
| CAL-39 | Growth Inhibition Assay | IC50=2.89999 μM | SANGER | ||
| LB2241-RCC | Growth Inhibition Assay | IC50=2.85893 μM | SANGER | ||
| COLO-792 | Growth Inhibition Assay | IC50=2.84027 μM | SANGER | ||
| HCE-T | Growth Inhibition Assay | IC50=2.83264 μM | SANGER | ||
| BFTC-905 | Growth Inhibition Assay | IC50=2.8253 μM | SANGER | ||
| CHL-1 | Growth Inhibition Assay | IC50=2.80785 μM | SANGER | ||
| L-363 | Growth Inhibition Assay | IC50=2.7437 μM | SANGER | ||
| HCC2218 | Growth Inhibition Assay | IC50=2.64778 μM | SANGER | ||
| DB | Growth Inhibition Assay | IC50=2.58788 μM | SANGER | ||
| EW-13 | Growth Inhibition Assay | IC50=2.56339 μM | SANGER | ||
| KNS-62 | Growth Inhibition Assay | IC50=2.51164 μM | SANGER | ||
| RD | Growth Inhibition Assay | IC50=2.44723 μM | SANGER | ||
| BB65-RCC | Growth Inhibition Assay | IC50=2.40674 μM | SANGER | ||
| CAL-27 | Growth Inhibition Assay | IC50=2.39236 μM | SANGER | ||
| DOK | Growth Inhibition Assay | IC50=2.35773 μM | SANGER | ||
| NB7 | Growth Inhibition Assay | IC50=2.34086 μM | SANGER | ||
| A2058 | Growth Inhibition Assay | IC50=2.19279 μM | SANGER | ||
| HN | Growth Inhibition Assay | IC50=2.16278 μM | SANGER | ||
| MZ2-MEL | Growth Inhibition Assay | IC50=2.11127 μM | SANGER | ||
| EM-2 | Growth Inhibition Assay | IC50=2.07198 μM | SANGER | ||
| HCC70 | Growth Inhibition Assay | IC50=2.02426 μM | SANGER | ||
| RXF393 | Growth Inhibition Assay | IC50=1.97887 μM | SANGER | ||
| LCLC-97TM1 | Growth Inhibition Assay | IC50=1.92256 μM | SANGER | ||
| A375 | Growth Inhibition Assay | IC50=1.89714 μM | SANGER | ||
| BPH-1 | Growth Inhibition Assay | IC50=1.89591 μM | SANGER | ||
| LOXIMVI | Growth Inhibition Assay | IC50=1.89427 μM | SANGER | ||
| NCI-H292 | Growth Inhibition Assay | IC50=1.86699 μM | SANGER | ||
| NB69 | Growth Inhibition Assay | IC50=1.78469 μM | SANGER | ||
| OVCAR-5 | Growth Inhibition Assay | IC50=1.77687 μM | SANGER | ||
| COLO-829 | Growth Inhibition Assay | IC50=1.62232 μM | SANGER | ||
| RT-112 | Growth Inhibition Assay | IC50=1.58952 μM | SANGER | ||
| SK-MEL-2 | Growth Inhibition Assay | IC50=1.57459 μM | SANGER | ||
| HD-MY-Z | Growth Inhibition Assay | IC50=1.57376 μM | SANGER | ||
| A4-Fuk | Growth Inhibition Assay | IC50=1.57045 μM | SANGER | ||
| SW1116 | Growth Inhibition Assay | IC50=1.56398 μM | SANGER | ||
| NCI-H1437 | Growth Inhibition Assay | IC50=1.55275 μM | SANGER | ||
| ML-2 | Growth Inhibition Assay | IC50=1.52868 μM | SANGER | ||
| HO-1-N-1 | Growth Inhibition Assay | IC50=1.51634 μM | SANGER | ||
| LoVo | Growth Inhibition Assay | IC50=1.46399 μM | SANGER | ||
| LS-513 | Growth Inhibition Assay | IC50=1.45192 μM | SANGER | ||
| BV-173 | Growth Inhibition Assay | IC50=1.44015 μM | SANGER | ||
| LS-411N | Growth Inhibition Assay | IC50=1.40517 μM | SANGER | ||
| SW1463 | Growth Inhibition Assay | IC50=1.33721 μM | SANGER | ||
| NCI-H2291 | Growth Inhibition Assay | IC50=1.32536 μM | SANGER | ||
| H-EMC-SS | Growth Inhibition Assay | IC50=1.29608 μM | SANGER | ||
| RCM-1 | Growth Inhibition Assay | IC50=1.24047 μM | SANGER | ||
| SK-MEL-1 | Growth Inhibition Assay | IC50=1.23419 μM | SANGER | ||
| ONS-76 | Growth Inhibition Assay | IC50=1.22049 μM | SANGER | ||
| Mewo | Growth Inhibition Assay | IC50=1.20276 μM | SANGER | ||
| A549 | Growth Inhibition Assay | IC50=1.19576 μM | SANGER | ||
| HuP-T4 | Growth Inhibition Assay | IC50=1.18359 μM | SANGER | ||
| SW620 | Growth Inhibition Assay | IC50=1.13534 μM | SANGER | ||
| SK-N-AS | Growth Inhibition Assay | IC50=1.07947 μM | SANGER | ||
| TYK-nu | Growth Inhibition Assay | IC50=1.03172 μM | SANGER | ||
| GP5d | Growth Inhibition Assay | IC50=0.98308 μM | SANGER | ||
| RVH-421 | Growth Inhibition Assay | IC50=0.9718 μM | SANGER | ||
| UACC-257 | Growth Inhibition Assay | IC50=0.96473 μM | SANGER | ||
| PSN1 | Growth Inhibition Assay | IC50=0.96196 μM | SANGER | ||
| C2BBe1 | Growth Inhibition Assay | IC50=0.81023 μM | SANGER | ||
| NCI-SNU-1 | Growth Inhibition Assay | IC50=0.75433 μM | SANGER | ||
| LB2518-MEL | Growth Inhibition Assay | IC50=0.71632 μM | SANGER | ||
| HT-144 | Growth Inhibition Assay | IC50=0.64657 μM | SANGER | ||
| HMV-II | Growth Inhibition Assay | IC50=0.64465 μM | SANGER | ||
| P12-ICHIKAWA | Growth Inhibition Assay | IC50=0.61221 μM | SANGER | ||
| A2780 | Growth Inhibition Assay | IC50=0.49823 μM | SANGER | ||
| WM-115 | Growth Inhibition Assay | IC50=0.49257 μM | SANGER | ||
| CP66-MEL | Growth Inhibition Assay | IC50=0.48809 μM | SANGER | ||
| HTC-C3 | Growth Inhibition Assay | IC50=0.46531 μM | SANGER | ||
| SH-4 | Growth Inhibition Assay | IC50=0.46256 μM | SANGER | ||
| KU812 | Growth Inhibition Assay | IC50=0.45299 μM | SANGER | ||
| K5 | Growth Inhibition Assay | IC50=0.43117 μM | SANGER | ||
| HL-60 | Growth Inhibition Assay | IC50=0.41107 μM | SANGER | ||
| KASUMI-1 | Growth Inhibition Assay | IC50=0.399 μM | SANGER | ||
| KY821 | Growth Inhibition Assay | IC50=0.3791 μM | SANGER | ||
| G-361 | Growth Inhibition Assay | IC50=0.36795 μM | SANGER | ||
| SK-MEL-24 | Growth Inhibition Assay | IC50=0.32813 μM | SANGER | ||
| COLO-679 | Growth Inhibition Assay | IC50=0.3272 μM | SANGER | ||
| KG-1 | Growth Inhibition Assay | IC50=0.30668 μM | SANGER | ||
| SK-MEL-28 | Growth Inhibition Assay | IC50=0.30409 μM | SANGER | ||
| BHT-101 | Growth Inhibition Assay | IC50=0.28606 μM | SANGER | ||
| MEL-HO | Growth Inhibition Assay | IC50=0.27652 μM | SANGER | ||
| ACN | Growth Inhibition Assay | IC50=0.26737 μM | SANGER | ||
| MZ7-mel | Growth Inhibition Assay | IC50=0.2634 μM | SANGER | ||
| NOMO-1 | Growth Inhibition Assay | IC50=0.25742 μM | SANGER | ||
| HSC-4 | Growth Inhibition Assay | IC50=0.24395 μM | SANGER | ||
| KM12 | Growth Inhibition Assay | IC50=0.24057 μM | SANGER | ||
| A101D | Growth Inhibition Assay | IC50=0.214 μM | SANGER | ||
| KMOE-2 | Growth Inhibition Assay | IC50=0.19795 μM | SANGER | ||
| C32 | Growth Inhibition Assay | IC50=0.19072 μM | SANGER | ||
| CP50-MEL-B | Growth Inhibition Assay | IC50=0.17254 μM | SANGER | ||
| M14 | Growth Inhibition Assay | IC50=0.15468 μM | SANGER | ||
| AGS | Growth Inhibition Assay | IC50=0.11713 μM | SANGER | ||
| MMAC-SF | Growth Inhibition Assay | IC50=0.10974 μM | SANGER | ||
| DU-4475 | Growth Inhibition Assay | IC50=0.07599 μM | SANGER | ||
| EoL-1-cell | Growth Inhibition Assay | IC50=0.04152 μM | SANGER | ||
| CHP-212 | Growth Inhibition Assay | IC50=0.02885 μM | SANGER | ||
| H9 | Growth Inhibition Assay | IC50=0.02276 μM | SANGER | ||
| HEL | Growth Inhibition Assay | IC50=24.0865 μM | SANGER | ||
| ABC-1 | Growth Inhibition Assay | IC50=24.2729 μM | SANGER | ||
| COLO-680N | Growth Inhibition Assay | IC50=24.4764 μM | SANGER | ||
| MZ1-PC | Growth Inhibition Assay | IC50=24.687 μM | SANGER | ||
| NCI-H69 | Growth Inhibition Assay | IC50=24.7354 μM | SANGER | ||
| TE-1 | Growth Inhibition Assay | IC50=25.0499 μM | SANGER | ||
| EW-3 | Growth Inhibition Assay | IC50=25.113 μM | SANGER | ||
| PANC-08-13 | Growth Inhibition Assay | IC50=25.8103 μM | SANGER | ||
| NMC-G1 | Growth Inhibition Assay | IC50=26.0088 μM | SANGER | ||
| BT-20 | Growth Inhibition Assay | IC50=26.4543 μM | SANGER | ||
| TGBC24TKB | Growth Inhibition Assay | IC50=26.7331 μM | SANGER | ||
| TE-11 | Growth Inhibition Assay | IC50=26.9895 μM | SANGER | ||
| ESS-1 | Growth Inhibition Assay | IC50=27.3216 μM | SANGER | ||
| JVM-3 | Growth Inhibition Assay | IC50=27.6475 μM | SANGER | ||
| C3A | Growth Inhibition Assay | IC50=27.8496 μM | SANGER | ||
| MDA-MB-157 | Growth Inhibition Assay | IC50=27.8753 μM | SANGER | ||
| KLE | Growth Inhibition Assay | IC50=28.1058 μM | SANGER | ||
| ES1 | Growth Inhibition Assay | IC50=28.1838 μM | SANGER | ||
| CAL-120 | Growth Inhibition Assay | IC50=28.3999 μM | SANGER | ||
| NCI-N87 | Growth Inhibition Assay | IC50=28.5105 μM | SANGER | ||
| RPMI-8226 | Growth Inhibition Assay | IC50=29.1843 μM | SANGER | ||
| COR-L88 | Growth Inhibition Assay | IC50=29.2419 μM | SANGER | ||
| UACC-893 | Growth Inhibition Assay | IC50=29.3137 μM | SANGER | ||
| C8166 | Growth Inhibition Assay | IC50=29.9996 μM | SANGER | ||
| J82 | Growth Inhibition Assay | IC50=30.8147 μM | SANGER | ||
| PFSK-1 | Growth Inhibition Assay | IC50=31.0659 μM | SANGER | ||
| COLO-684 | Growth Inhibition Assay | IC50=31.4374 μM | SANGER | ||
| CAL-72 | Growth Inhibition Assay | IC50=31.5729 μM | SANGER | ||
| SNB75 | Growth Inhibition Assay | IC50=31.897 μM | SANGER | ||
| MDA-MB-415 | Growth Inhibition Assay | IC50=31.9762 μM | SANGER | ||
| SiHa | Growth Inhibition Assay | IC50=32.4711 μM | SANGER | ||
| NCI-H1648 | Growth Inhibition Assay | IC50=32.9345 μM | SANGER | ||
| EFO-21 | Growth Inhibition Assay | IC50=33.005 μM | SANGER | ||
| HCC38 | Growth Inhibition Assay | IC50=33.3841 μM | SANGER | ||
| IA-LM | Growth Inhibition Assay | IC50=33.7889 μM | SANGER | ||
| CTV-1 | Growth Inhibition Assay | IC50=33.9786 μM | SANGER | ||
| NCI-H446 | Growth Inhibition Assay | IC50=34.2689 μM | SANGER | ||
| IST-SL1 | Growth Inhibition Assay | IC50=34.7408 μM | SANGER | ||
| EW-22 | Growth Inhibition Assay | IC50=34.7759 μM | SANGER | ||
| JEG-3 | Growth Inhibition Assay | IC50=36.1766 μM | SANGER | ||
| LU-65 | Growth Inhibition Assay | IC50=36.2985 μM | SANGER | ||
| NCI-H596 | Growth Inhibition Assay | IC50=36.9591 μM | SANGER | ||
| KNS-81-FD | Growth Inhibition Assay | IC50=37.145 μM | SANGER | ||
| NCI-H1793 | Growth Inhibition Assay | IC50=37.7086 μM | SANGER | ||
| NCI-H460 | Growth Inhibition Assay | IC50=38.0873 μM | SANGER | ||
| MPP-89 | Growth Inhibition Assay | IC50=39.5886 μM | SANGER | ||
| D-542MG | Growth Inhibition Assay | IC50=39.8436 μM | SANGER | ||
| JAR | Growth Inhibition Assay | IC50=40.4705 μM | SANGER | ||
| NCI-H209 | Growth Inhibition Assay | IC50=40.677 μM | SANGER | ||
| G-402 | Growth Inhibition Assay | IC50=41.3993 μM | SANGER | ||
| IST-MES1 | Growth Inhibition Assay | IC50=42.1935 μM | SANGER | ||
| Daoy | Growth Inhibition Assay | IC50=42.5471 μM | SANGER | ||
| EW-11 | Growth Inhibition Assay | IC50=43.1211 μM | SANGER | ||
| Saos-2 | Growth Inhibition Assay | IC50=43.1537 μM | SANGER | ||
| no-10 | Growth Inhibition Assay | IC50=43.1702 μM | SANGER | ||
| HCC1395 | Growth Inhibition Assay | IC50=43.4644 μM | SANGER | ||
| HCE-4 | Growth Inhibition Assay | IC50=43.7664 μM | SANGER | ||
| EW-1 | Growth Inhibition Assay | IC50=43.8049 μM | SANGER | ||
| OCUB-M | Growth Inhibition Assay | IC50=44.3638 μM | SANGER | ||
| IGR-1 | Growth Inhibition Assay | IC50=44.4115 μM | SANGER | ||
| NCI-H1838 | Growth Inhibition Assay | IC50=44.4349 μM | SANGER | ||
| NCI-H2405 | Growth Inhibition Assay | IC50=44.534 μM | SANGER | ||
| GB-1 | Growth Inhibition Assay | IC50=44.7463 μM | SANGER | ||
| MG-63 | Growth Inhibition Assay | IC50=46.0696 μM | SANGER | ||
| KP-N-YN | Growth Inhibition Assay | IC50=46.4679 μM | SANGER | ||
| no-11 | Growth Inhibition Assay | IC50=47.0244 μM | SANGER | ||
| SW948 | Growth Inhibition Assay | IC50=47.3377 μM | SANGER | ||
| CAMA-1 | Growth Inhibition Assay | IC50=47.3438 μM | SANGER | ||
| HCC1187 | Growth Inhibition Assay | IC50=47.51 μM | SANGER | ||
| D-392MG | Growth Inhibition Assay | IC50=47.6516 μM | SANGER | ||
| 647-V | Growth Inhibition Assay | IC50=49.3414 μM | SANGER | ||
| HeLa | Function assay | Concentration-dependent inhibition of ERK5 phosphorylation shift in EGF-stimulated HeLa cells | 17850214 | ||
| HeLa | Function assay | Concentration-dependent inhibition of ERK1, ERK2 phosphorylation in EGF-stimulated HeLa cells | 17850214 | ||
| Colon 26 | Function assay | Inhibition of MEK in mouse colon 26 carcinoma cells assessed as inhibition of ERK phosphorylation by ELISA, IC50=0.046μM | 17880056 | ||
| Colon 26 | Function assay | Inhibition of MEK in mouse Colon 26 cells by Western blot, IC50=0.053μM | 18951019 | ||
| C26 | Function assay | Inhibition of MEK-stimulated ERK phosphorylation in PDGF-stimulated mouse C26 cells treated as single oral dose before PDGF challenge by whole cell assay, IC50=0.0035μM | 18952427 | ||
| DAOY | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY 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 | ||
| A673 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 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 | ||
| BT-37 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 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 | ||
| 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 | ||
| Saos-2 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 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 | ||
| NB1643 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 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 | ||
| BT-12 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 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 | ||
| RD | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells | 29435139 | ||
| MG 63 (6-TG R) | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells | 29435139 | ||
| 點擊查看更多細胞系數據 | |||||
生物活性
| 產品描述 | PD184352 (CI-1040) 是一種ATP非競爭性的MEK1/2抑制劑，細胞試驗中IC50為17 nM，對MEK1/2的選擇性比MEK5高100倍。PD184352 (CI-1040)可選擇性地誘導凋亡。 | ||||
|---|---|---|---|---|---|
| 特性 | 首個開始臨床開發(fā)的MEK抑制劑。 | ||||
| 靶點 |
|
| 體外研究(In Vitro) | ||||
| 體外研究活性 | CI-1040治療使多重腫瘤細胞，包括結腸26，BX-PC3 胰腺癌，A431 子宮頸癌，HT-29結腸癌， ZR-25-1乳腺癌和SKOV-3 卵巢癌細胞中pMAPK 水平降低。CI-1040治療不抑制Jun激酶，p38 激酶或Akt的磷酸化作用，這表明CI-1040特定作用于MEK。CI-1040對MAPK活化的抑制阻止細胞周期進程，并誘導G1期阻滯。[1] CI-1040抑制MEK1的IC50為0.3 μM，比抑制Swiss 3T3細胞中EGF誘導的ERK2活化所需的濃度高15倍。這些結果表明CI-1040通過抑制MKK1活化，而不是通過阻斷MKK1活性對細胞發(fā)揮作用。2 nM PD184352抑制Swiss 3T3細胞中50%的MKK1活化，而超過100倍濃度的CI-1040在體外抑制MEK1。PD184352也會抑制Raf催化的MEK1磷酸化，而對Raf催化的髓鞘堿性蛋白磷酸化沒有作用。[2]與僅用DMSO處理的細胞相比，CI-1040抑制86%甲狀腺乳頭狀癌(PTC)細胞生長，10μM濃度時導致RET/PTC1重排。CI-1040對PTC細胞(BRAF 突變)表現(xiàn)出有效的抑制作用，GI50為52 nM，但是對RET/PTC1重排型活性較低，GI50 為1.1 μM。[3]一項最近的研究表明CI-1040增加CML 急變期細胞系，K562，和初級慢性期CD34+ CML細胞中BMS-214662的凋亡作用。[4] | |||
|---|---|---|---|---|
| 激酶實驗 | MEK1 試驗 | |||
| MAP激酶被MEK磷酸化后活化；活化的MAP激酶隨后使髓鞘堿性蛋白(MBP)磷酸化。32P整合到髓鞘堿性蛋白(MBP)的測定在包含44-kDa MAPK (GST-MAPK)或45-kDa MEK (GST-MEK1)的谷胱甘肽S-轉移酶(GST)融合蛋白存在下進行。試驗在包含10 μg GST-MEK1，0.5 μg GST-MAPK，和40 μg MBP的50μL 50 mM Tris，pH 7.4/10 mM MgCl2 /2 mM EGTA/10 μM [γ-32P]ATP中進行。30°C下培養(yǎng)15分鐘后，加入Laemmli SDS樣品緩沖液停止反應。磷酸化的MBP通過SDS/10% PAGE溶解。這種篩選作用使幾種小分子MEK抑制劑被發(fā)現(xiàn)，例如CI-1040。評估加入順序的實驗表明CI-1040直接抑制MEK1，50%抑制濃度(IC50)為17 nM，而不影響MAPK活性。 | ||||
| 細胞實驗 | 細胞系 | Colon 26腫瘤細胞 | ||
| 濃度 | 0.1-10 μM | |||
| 孵育時間 | 24小時 | |||
| 方法 | 將細胞接種在T-75 cm 2燒瓶，第二天用DMSO或CI-1040處理24小時。收集單細胞懸浮液，并且將沉淀在冰乙醇 (70%)中固定30分鐘。樣品離心后，將碘化丙啶(50μg/mL)和RNase (30 units/mL)加入沉淀物中，37℃下培養(yǎng)20分鐘。過濾后，樣品通過流式細胞儀分析。 | |||
| 實驗圖片 | 檢測方法 | 檢測指標 | 實驗圖片 | PMID |
| Western blot | p-ERK1/2 / ERK1/2 p-ERK5 / ERK5 |
|
21762482 | |
| Growth inhibition assay | Cell viability |
|
29989268 | |
| 體內研究(In Vivo) | ||
| 體內研究活性 | CI-1040口服給藥減弱小鼠和人結腸腫瘤異種移植物的生長，具有48-200 mg/kg每劑的廣泛劑量范圍，但是對P388白血病沒有作用。[1] CI-1040口服給藥(300 mg/kg/d)3周后，抑制來自PTC細胞的腫瘤異種移植物，與未處理的(僅載體處理)小鼠相比，使攜帶BRAF突變型的移植物減少31.3%，攜帶RET/PTC1重排型的移植物減少47.5%。小鼠用CI-1040處理時，沒有觀察到毒性作用。[2]乳腺腫瘤對CI-1040和UCN-01的瞬時暴露引起腫瘤細胞體內死亡，并延長對腫瘤再生長的抑制。CI-1040 (25 mg/kg) 和UCN-01 (0.1-0.2 mg/kg)的聯(lián)合治療顯著減少MDA-MB-231，并很大程度上廢除植入無胸腺小鼠的MCF7腫瘤生長，而任何單一治療都沒有顯著活性。聯(lián)合用藥引起顯著的腫瘤細胞死亡，這與ERK1/2的磷酸化和Ki67與CD31的免疫活性降低相一致。[5] | |
|---|---|---|
| 動物實驗 | Animal Models | 無胸腺小鼠的PTC細胞 |
| Dosages | 150 mg/kg | |
| Administration | 口服，一天兩次 | |
化學信息&溶解度
| 分子量 | 478.67 | 分子式 | C17H14ClF2IN2O2 |
| CAS號 | 212631-79-3 | SDF | Download PD184352 (CI-1040) SDF |
| Smiles | C1CC1CONC(=O)C2=C(C(=C(C=C2)F)F)NC3=C(C=C(C=C3)I)Cl | ||
| 儲存條件(自收到貨起) | |||
|
體外溶解度 |
DMSO : 96 mg/mL ( (200.55 mM) ；DMSO吸濕會降低化合物溶解度，請使用新開封DMSO) Ethanol : 14 mg/mL (29.24 mM) Water : Insoluble |
摩爾濃度計算器 |
|
體內溶解度 現(xiàn)配現(xiàn)用，請按從左到右的順序依次添加，澄清后再加入下一溶劑 |
動物體內配方計算器 | ||||
實驗計算
動物體內配方計算器（澄清溶液）
第一步：請輸入基本實驗信息（考慮到實驗過程中的損耗，建議多配一只動物的藥量）
mg/kg
g
μL
只
第二步：請輸入動物體內配方組成（配方適用于不溶于水的藥物；不同批次藥物配方比例不同，請聯(lián)系Selleck為您提供正確的澄清溶液配方）
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
計算結果：
工作液濃度： mg/ml；
DMSO母液配制方法： mg 藥物溶于μL DMSO溶液（母液濃度mg/mL，注：如該濃度超過該批次藥物DMSO溶解度，請先聯(lián)系Selleck）；
體內配方配制方法：取μL DMSO母液，加入μL PEG300，混勻澄清后加入μL Tween 80，混勻澄清后加入μL ddH2O，混勻澄清。
體內配方配制方法：取μL DMSO母液，加入μL Corn oil，混勻澄清。
注意：1. 首先保證母液是澄清的；
2.一定要按照順序依次將溶劑加入，進行下一步操作之前必須保證上一步操作得到的是澄清的溶液，可采用渦旋、超聲或水浴加熱等物理方法助溶。
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