- 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
- 化合物ライブラリー
- 抗体
- 新製品
- お問い合わせ
PD184352 (CI-1040)
PD184352 (CI-1040) is an ATP non-competitive MEK1/2 inhibitor with IC50 of 17 nM in cell-based assays, 100-fold more selective for MEK1/2 than MEK5. PD184352 (CI-1040) selectively induces apoptosis.
CAS No. 212631-79-3
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PD184352 (CI-1040)関連製品
シグナル伝達経路
MEK阻害剤の選択性比較
Cell Data
| Cell Lines | Assay Type | Concentration | Incubation Time | 活性情報 | PMID |
|---|---|---|---|---|---|
| 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 | ||
| 他の多くの細胞株試験データをご覧になる場合はこちらをクリックして下さい | |||||
生物活性
| 製品説明 | PD184352 (CI-1040) is an ATP non-competitive MEK1/2 inhibitor with IC50 of 17 nM in cell-based assays, 100-fold more selective for MEK1/2 than MEK5. PD184352 (CI-1040) selectively induces apoptosis. | ||||
|---|---|---|---|---|---|
| 特性 | First MEK inhibitor to begin clinical development. | ||||
| Targets |
|
| In Vitro | ||||
| In vitro | CI-1040 treatment produces a reduction of pMAPK levels in multiple tumor cells including Colon 26, BX-PC3 pancreatic, A431 cervical, HT-29 colon, ZR-25-1 breast and SKOV-3 ovarian carcinomas. This compound treatment doesn't inhibit the phosphorylation of Jun kinase, p38 kinase or Akt, indicating it specifically targets MEK. Inhibition of MAPK activation by this chemical prevents cell cycle progression and induces a G1 block. [1] The IC50 for inhibition of MEK1 by this inhibitor is 0.3 μM, 15-fold higher than the concentration required to inhibit the EGF-induced activation of ERK2 in Swiss 3T3 cells. These results indicate this agent exerts its effects on cells by suppressing the activation of MKK1, and not by blocking its activity. 2 nM this compound inhibits the activation of MKK1 in Swiss 3T3 cells by 50%, while over 100-fold concentration of it inhibits MEK1 in vitro. It also inhibits the Raf-catalysed phosphorylation of MEK1 without any effect on the Raf-catalysed phosphorylation of myelin basic protein. [2] This chemical inhibits 86% of papillary thyroid carcinoma (PTC) cell growth with the RET/PTC1 rearrangement at 10μM compared with cells treated with DMSO only. It shows potent inhibition to PTC cells (BRAF mutation) with GI50 of 52 nM, but low activity to RET/PTC1 rearrangement type with GI50 of 1.1 μM. [3] A recent research indicates this agent increases the apoptotic effect of BMS-214662 in a CML blast crisis cell line, K562, and in primary chronic phase CD34+ CML cells. [4] | |||
|---|---|---|---|---|
| Kinase Assay | MEK1 Assay | |||
| MAP kinase is activated after phosphorylation by MEK; the activated MAP kinase subsequently phosphorylates myelin basic protein (MBP).Incorporation of 32P into myelin basic protein (MBP) is assayed in the presence of glutathione S-transferase (GST) fusion proteins containing the 44-kDa MAPK (GST-MAPK) or the 45-kDa MEK (GST-MEK1). Assays are conducted in 50μL of 50 mM Tris, pH 7.4/10 mM MgCl2 /2 mM EGTA/10 μM [γ-32P]ATP containing 10 μg of GST-MEK1, 0.5 μg of GST-MAPK, and 40 μg of MBP. After incubation at 30°C for 15 minutes, reactions are stopped by addition of Laemmli SDS sample buffer. Phosphorylated MBP is resolved by SDS/10% PAGE. This screening effort leads to the discovery of several small-molecule inhibitors of MEK, i.e. PD184352 (CI-1040). Experiments assessing the order of addition shows that this compound directly inhibits MEK1 with a 50% inhibitory concentration (IC50) of 17 nM, without affecting the activity of MAPK. | ||||
| 細胞実験 | 細胞株 | Colon 26 carcinoma cells | ||
| 濃度 | 0.1-10 μM | |||
| 反応時間 | 24 hours | |||
| 実験の流れ | Cells are planted seeded in T-75 cm 2 flasks and treated the next day for 24 hous with either DMSO or this compound. Single-cell suspensions are collected, and pellets are fixed in ice-cold ethanol (70%) for 30 minutes. After centrifugation of the samples, propidium iodide (50 μg/mL) and RNase (30 units/mL) are added to the pellets for 20 minutes at 37 °C. After filtration, samples are analyzed by flow cytometry. |
|||
| 実験結果図 | Methods | Biomarkers | 結果図 | PMID |
| Western blot | p-ERK1/2 / ERK1/2 p-ERK5 / ERK5 |
|
21762482 | |
| Growth inhibition assay | Cell viability |
|
29989268 | |
| In Vivo | ||
| In Vivo | Oral dosing of CI-1040 impairs the growth of colon tumor xenografts of mouse and human with a wide dose range of 48-200 mg/kg per dose, but not of P388 leukemia. [1] This compound inhibits the tumor xenografts from PTC cells carrying a BRAF mutation with 31.3% reduction, carrying the RET/PTC1 rearrangement with 47.5% reduction than in untreated (vehicle) mice after 3 weeks of oral administration (300 mg/kg/d). No toxic effects are observed in any mice when they are treated with this chemical. [2] Transient exposure of mammary tumors to this compound and UCN-01 causes tumor cell death in vivo and prolonged suppression of tumor regrowth. Combined treatment with this chemical (25 mg/kg) and UCN-01 (0.1-0.2 mg/kg) significantly reduces MDA-MB-231, and largely abolishs MCF7 tumor growth in implanted athymic mice, while either single treatment has no significant activity. The drug combination leads to profound tumor cell death which correlates with a reduction in the phosphorylation of ERK1/2 and the immuno-reactivity of Ki67 and of CD31. [5] | |
|---|---|---|
| 動物実験 | 動物モデル | PTC cells in athymic mice |
| 投与量 | 150 mg/kg | |
| 投与経路 | Orally twice daily | |
|
化学情報
| 分子量 | 478.67 | 化学式 | C17H14ClF2IN2O2 |
| CAS No. | 212631-79-3 | SDF | Download PD184352 (CI-1040) SDFをダウンロードする |
| Smiles | C1CC1CONC(=O)C2=C(C(=C(C=C2)F)F)NC3=C(C=C(C=C3)I)Cl | ||
| 保管 | |||
|
In vitro |
DMSO : 96 mg/mL ( (200.55 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。) Ethanol : 14 mg/mL 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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