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PD184352 (CI-1040) MEK inhibitor
Kat.-Nr.S1020
Chemische Struktur
Molekulargewicht: 478.67
Springe zu
Qualitätskontrolle
Charge:
Reinheit:
99.96%
99.96
| Verwandte Ziele | ERK p38 MAPK Raf JNK Ras KRas S6 Kinase MAP4K TAK1 Mixed Lineage Kinase |
|---|---|
| Weitere MEK Inhibitoren | PD0325901 (Mirdametinib) U0126-EtOH PD 98059 BIX 02189 Pimasertib (AS-703026) Refametinib (RDEA119) TAK-733 AZD8330 SL-327 BIX 02188 |
Zellkultur, Behandlung & Arbeitskonzentration
| Zelllinien | Assay-Typ | Konzentration | Inkubationszeit | Formulierung | Aktivitätsbeschreibung | PMID |
|---|---|---|---|---|---|---|
| PC-3 | Growth Inhibition Assay | IC50=24.0526 μM | SANGER | |||
| VM-CUB-1 | Growth Inhibition Assay | IC50=23.7341 μM | SANGER | |||
| LC-2-ad | Growth Inhibition Assay | IC50=23.6147 μM | SANGER | |||
| A704 | Growth Inhibition Assay | IC50=23.6103 μM | SANGER | |||
| DMS-114 | Growth Inhibition Assay | IC50=23.5765 μM | SANGER | |||
| EKVX | Growth Inhibition Assay | IC50=23.3909 μM | SANGER | |||
| SNU-449 | Growth Inhibition Assay | IC50=23.329 μM | SANGER | |||
| HCC1806 | Growth Inhibition Assay | IC50=23.0583 μM | SANGER | |||
| CaR-1 | Growth Inhibition Assay | IC50=23.0213 μM | SANGER | |||
| NCI-H441 | Growth Inhibition Assay | IC50=22.5689 μM | SANGER | |||
| TI-73 | Growth Inhibition Assay | IC50=22.328 μM | SANGER | |||
| NCI-H1755 | Growth Inhibition Assay | IC50=21.6741 μM | SANGER | |||
| A498 | Growth Inhibition Assay | IC50=21.5312 μM | SANGER | |||
| CFPAC-1 | Growth Inhibition Assay | IC50=21.3858 μM | SANGER | |||
| ChaGo-K-1 | Growth Inhibition Assay | IC50=21.3627 μM | SANGER | |||
| KP-4 | Growth Inhibition Assay | IC50=21.1196 μM | SANGER | |||
| Becker | Growth Inhibition Assay | IC50=21.1118 μM | SANGER | |||
| UMC-11 | Growth Inhibition Assay | IC50=20.9164 μM | SANGER | |||
| TE-6 | Growth Inhibition Assay | IC50=20.8067 μM | SANGER | |||
| SF539 | Growth Inhibition Assay | IC50=20.5172 μM | SANGER | |||
| FTC-133 | Growth Inhibition Assay | IC50=20.4703 μM | SANGER | |||
| NCI-H226 | Growth Inhibition Assay | IC50=20.4399 μM | SANGER | |||
| NCI-H1048 | Growth Inhibition Assay | IC50=20.3266 μM | SANGER | |||
| Calu-3 | Growth Inhibition Assay | IC50=19.4237 μM | SANGER | |||
| SF126 | Growth Inhibition Assay | IC50=19.3502 μM | SANGER | |||
| NTERA-S-cl-D1 | Growth Inhibition Assay | IC50=19.2007 μM | SANGER | |||
| SW1573 | Growth Inhibition Assay | IC50=19.1969 μM | SANGER | |||
| SNU-387 | Growth Inhibition Assay | IC50=19.1889 μM | SANGER | |||
| ETK-1 | Growth Inhibition Assay | IC50=19.1827 μM | SANGER | |||
| HuO9 | Growth Inhibition Assay | IC50=19.1379 μM | SANGER | |||
| RO82-W-1 | Growth Inhibition Assay | IC50=18.8288 μM | SANGER | |||
| D-502MG | Growth Inhibition Assay | IC50=18.8139 μM | SANGER | |||
| LS-123 | Growth Inhibition Assay | IC50=18.7901 μM | SANGER | |||
| OC-314 | Growth Inhibition Assay | IC50=18.7384 μM | SANGER | |||
| Ramos-2G6-4C10 | Growth Inhibition Assay | IC50=18.5927 μM | SANGER | |||
| SW962 | Growth Inhibition Assay | IC50=18.5702 μM | SANGER | |||
| SW982 | Growth Inhibition Assay | IC50=18.5649 μM | SANGER | |||
| KYSE-410 | Growth Inhibition Assay | IC50=18.4577 μM | SANGER | |||
| HT-3 | Growth Inhibition Assay | IC50=18.3977 μM | SANGER | |||
| CAL-85-1 | Growth Inhibition Assay | IC50=18.1809 μM | SANGER | |||
| BB30-HNC | Growth Inhibition Assay | IC50=18.0318 μM | SANGER | |||
| D-247MG | Growth Inhibition Assay | IC50=17.9247 μM | SANGER | |||
| SCC-15 | Growth Inhibition Assay | IC50=17.8473 μM | SANGER | |||
| BB49-HNC | Growth Inhibition Assay | IC50=17.5686 μM | SANGER | |||
| KYSE-70 | Growth Inhibition Assay | IC50=17.289 μM | SANGER | |||
| NKM-1 | Growth Inhibition Assay | IC50=17.0189 μM | SANGER | |||
| NCI-H23 | Growth Inhibition Assay | IC50=16.6078 μM | SANGER | |||
| NCI-H2228 | Growth Inhibition Assay | IC50=16.5158 μM | SANGER | |||
| BxPC-3 | Growth Inhibition Assay | IC50=16.2856 μM | SANGER | |||
| VMRC-RCZ | Growth Inhibition Assay | IC50=16.2592 μM | SANGER | |||
| NCI-H1299 | Growth Inhibition Assay | IC50=16.2291 μM | SANGER | |||
| A204 | Growth Inhibition Assay | IC50=16.2006 μM | SANGER | |||
| NCI-H28 | Growth Inhibition Assay | IC50=16.0856 μM | SANGER | |||
| G-401 | Growth Inhibition Assay | IC50=15.9649 μM | SANGER | |||
| HOP-62 | Growth Inhibition Assay | IC50=15.9597 μM | SANGER | |||
| TGBC11TKB | Growth Inhibition Assay | IC50=15.9414 μM | SANGER | |||
| SAS | Growth Inhibition Assay | IC50=15.9373 μM | SANGER | |||
| LU-134-A | Growth Inhibition Assay | IC50=15.9018 μM | SANGER | |||
| OCI-AML2 | Growth Inhibition Assay | IC50=15.7614 μM | SANGER | |||
| ES3 | Growth Inhibition Assay | IC50=15.536 μM | SANGER | |||
| PC-14 | Growth Inhibition Assay | IC50=15.4866 μM | SANGER | |||
| Detroit562 | Growth Inhibition Assay | IC50=15.4547 μM | SANGER | |||
| SCC-4 | Growth Inhibition Assay | IC50=15.4103 μM | SANGER | |||
| NCI-H1563 | Growth Inhibition Assay | IC50=15.349 μM | SANGER | |||
| AM-38 | Growth Inhibition Assay | IC50=15.2717 μM | SANGER | |||
| EC-GI-10 | Growth Inhibition Assay | IC50=15.2357 μM | SANGER | |||
| OE33 | Growth Inhibition Assay | IC50=15.1711 μM | SANGER | |||
| OVCAR-4 | Growth Inhibition Assay | IC50=15.1424 μM | SANGER | |||
| U-87-MG | Growth Inhibition Assay | IC50=15.0897 μM | SANGER | |||
| MKN7 | Growth Inhibition Assay | IC50=15.0093 μM | SANGER | |||
| NCI-H661 | Growth Inhibition Assay | IC50=14.959 μM | SANGER | |||
| LB831-BLC | Growth Inhibition Assay | IC50=14.8934 μM | SANGER | |||
| BT-549 | Growth Inhibition Assay | IC50=14.8284 μM | SANGER | |||
| NCI-H2347 | Growth Inhibition Assay | IC50=14.823 μM | SANGER | |||
| OVCAR-8 | Growth Inhibition Assay | IC50=14.7201 μM | SANGER | |||
| NCI-H630 | Growth Inhibition Assay | IC50=14.6568 μM | SANGER | |||
| U-118-MG | Growth Inhibition Assay | IC50=14.631 μM | SANGER | |||
| LS-1034 | Growth Inhibition Assay | IC50=14.6152 μM | SANGER | |||
| BALL-1 | Growth Inhibition Assay | IC50=14.4665 μM | SANGER | |||
| Capan-2 | Growth Inhibition Assay | IC50=14.3714 μM | SANGER | |||
| QIMR-WIL | Growth Inhibition Assay | IC50=14.3412 μM | SANGER | |||
| HC-1 | Growth Inhibition Assay | IC50=14.2087 μM | SANGER | |||
| NCI-H2030 | Growth Inhibition Assay | IC50=14.1465 μM | SANGER | |||
| NB17 | Growth Inhibition Assay | IC50=14.085 μM | SANGER | |||
| GCT | Growth Inhibition Assay | IC50=13.9697 μM | SANGER | |||
| OS-RC-2 | Growth Inhibition Assay | IC50=13.9501 μM | SANGER | |||
| GCIY | Growth Inhibition Assay | IC50=13.6927 μM | SANGER | |||
| SF268 | Growth Inhibition Assay | IC50=13.6326 μM | SANGER | |||
| NCI-H2009 | Growth Inhibition Assay | IC50=13.5919 μM | SANGER | |||
| CAPAN-1 | Growth Inhibition Assay | IC50=13.5514 μM | SANGER | |||
| NCI-H2452 | Growth Inhibition Assay | IC50=13.2175 μM | SANGER | |||
| OAW-42 | Growth Inhibition Assay | IC50=13.1937 μM | SANGER | |||
| NCI-H1092 | Growth Inhibition Assay | IC50=13.162 μM | SANGER | |||
| SW13 | Growth Inhibition Assay | IC50=13.1165 μM | SANGER | |||
| 8-MG-BA | Growth Inhibition Assay | IC50=13.0455 μM | SANGER | |||
| ATN-1 | Growth Inhibition Assay | IC50=13.0184 μM | SANGER | |||
| OVCAR-3 | Growth Inhibition Assay | IC50=12.9567 μM | SANGER | |||
| LXF-289 | Growth Inhibition Assay | IC50=12.9531 μM | SANGER | |||
| HT | Growth Inhibition Assay | IC50=12.8346 μM | SANGER | |||
| 769-P | Growth Inhibition Assay | IC50=12.7924 μM | SANGER | |||
| BEN | Growth Inhibition Assay | IC50=12.6143 μM | SANGER | |||
| HSC-2 | Growth Inhibition Assay | IC50=12.5996 μM | SANGER | |||
| TCCSUP | Growth Inhibition Assay | IC50=12.5757 μM | SANGER | |||
| BHY | Growth Inhibition Assay | IC50=12.5307 μM | SANGER | |||
| KYSE-510 | Growth Inhibition Assay | IC50=12.5079 μM | SANGER | |||
| ES7 | Growth Inhibition Assay | IC50=12.2724 μM | SANGER | |||
| NCI-H1703 | Growth Inhibition Assay | IC50=12.2616 μM | SANGER | |||
| GI-ME-N | Growth Inhibition Assay | IC50=12.2163 μM | SANGER | |||
| NOS-1 | Growth Inhibition Assay | IC50=12.1352 μM | SANGER | |||
| SW1990 | Growth Inhibition Assay | IC50=12.0911 μM | SANGER | |||
| SJSA-1 | Growth Inhibition Assay | IC50=12.0735 μM | SANGER | |||
| HLE | Growth Inhibition Assay | IC50=12.0585 μM | SANGER | |||
| LB373-MEL-D | Growth Inhibition Assay | IC50=12.0533 μM | SANGER | |||
| KALS-1 | Growth Inhibition Assay | IC50=12.0016 μM | SANGER | |||
| D-336MG | Growth Inhibition Assay | IC50=11.9075 μM | SANGER | |||
| KYSE-270 | Growth Inhibition Assay | IC50=11.8745 μM | SANGER | |||
| KOSC-2 | Growth Inhibition Assay | IC50=11.6222 μM | SANGER | |||
| S-117 | Growth Inhibition Assay | IC50=11.4896 μM | SANGER | |||
| KYSE-180 | Growth Inhibition Assay | IC50=11.482 μM | SANGER | |||
| KYSE-450 | Growth Inhibition Assay | IC50=11.4057 μM | SANGER | |||
| SW837 | Growth Inhibition Assay | IC50=11.3506 μM | SANGER | |||
| YH-13 | Growth Inhibition Assay | IC50=11.3267 μM | SANGER | |||
| SF295 | Growth Inhibition Assay | IC50=11.3104 μM | SANGER | |||
| KS-1 | Growth Inhibition Assay | IC50=11.2619 μM | SANGER | |||
| SW756 | Growth Inhibition Assay | IC50=11.2154 μM | SANGER | |||
| SBC-5 | Growth Inhibition Assay | IC50=11.1467 μM | SANGER | |||
| U251 | Growth Inhibition Assay | IC50=11.042 μM | SANGER | |||
| DJM-1 | Growth Inhibition Assay | IC50=11.0379 μM | SANGER | |||
| MOLT-16 | Growth Inhibition Assay | IC50=10.8113 μM | SANGER | |||
| NEC8 | Growth Inhibition Assay | IC50=10.7773 μM | SANGER | |||
| NCI-H1623 | Growth Inhibition Assay | IC50=10.6379 μM | SANGER | |||
| GMS-10 | Growth Inhibition Assay | IC50=10.6094 μM | SANGER | |||
| CCRF-CEM | Growth Inhibition Assay | IC50=10.5684 μM | SANGER | |||
| VA-ES-BJ | Growth Inhibition Assay | IC50=10.567 μM | SANGER | |||
| KE-37 | Growth Inhibition Assay | IC50=10.5272 μM | SANGER | |||
| KYSE-520 | Growth Inhibition Assay | IC50=10.52 μM | SANGER | |||
| MKN28 | Growth Inhibition Assay | IC50=10.518 μM | SANGER | |||
| SK-NEP-1 | Growth Inhibition Assay | IC50=10.4981 μM | SANGER | |||
| MDA-MB-175-VII | Growth Inhibition Assay | IC50=10.48 μM | SANGER | |||
| KARPAS-45 | Growth Inhibition Assay | IC50=10.2795 μM | SANGER | |||
| NCI-H720 | Growth Inhibition Assay | IC50=10.1989 μM | SANGER | |||
| NCI-H1573 | Growth Inhibition Assay | IC50=10.1574 μM | SANGER | |||
| MSTO-211H | Growth Inhibition Assay | IC50=9.95529 μM | SANGER | |||
| KGN | Growth Inhibition Assay | IC50=9.83795 μM | SANGER | |||
| YKG-1 | Growth Inhibition Assay | IC50=9.75033 μM | SANGER | |||
| P30-OHK | Growth Inhibition Assay | IC50=9.65316 μM | SANGER | |||
| 639-V | Growth Inhibition Assay | IC50=9.64388 μM | SANGER | |||
| SW1417 | Growth Inhibition Assay | IC50=9.56837 μM | SANGER | |||
| NCI-H1792 | Growth Inhibition Assay | IC50=9.45219 μM | SANGER | |||
| MKN45 | Growth Inhibition Assay | IC50=9.45065 μM | SANGER | |||
| HCC1937 | Growth Inhibition Assay | IC50=9.29091 μM | SANGER | |||
| MEG-01 | Growth Inhibition Assay | IC50=9.24931 μM | SANGER | |||
| DK-MG | Growth Inhibition Assay | IC50=9.21191 μM | SANGER | |||
| TE-12 | Growth Inhibition Assay | IC50=9.03367 μM | SANGER | |||
| NCI-H2126 | Growth Inhibition Assay | IC50=9.00826 μM | SANGER | |||
| T98G | Growth Inhibition Assay | IC50=8.99846 μM | SANGER | |||
| SK-UT-1 | Growth Inhibition Assay | IC50=8.97683 μM | SANGER | |||
| SW954 | Growth Inhibition Assay | IC50=8.96978 μM | SANGER | |||
| NCI-H1693 | Growth Inhibition Assay | IC50=8.9217 μM | SANGER | |||
| RKO | Growth Inhibition Assay | IC50=8.89057 μM | SANGER | |||
| MS-1 | Growth Inhibition Assay | IC50=8.87517 μM | SANGER | |||
| ES4 | Growth Inhibition Assay | IC50=8.86884 μM | SANGER | |||
| SBC-1 | Growth Inhibition Assay | IC50=8.86645 μM | SANGER | |||
| K-562 | Growth Inhibition Assay | IC50=8.83957 μM | SANGER | |||
| SK-N-FI | Growth Inhibition Assay | IC50=8.81379 μM | SANGER | |||
| DBTRG-05MG | Growth Inhibition Assay | IC50=8.74859 μM | SANGER | |||
| CAL-12T | Growth Inhibition Assay | IC50=8.65753 μM | SANGER | |||
| A673 | Growth Inhibition Assay | IC50=8.63202 μM | SANGER | |||
| CAKI-1 | Growth Inhibition Assay | IC50=8.57222 μM | SANGER | |||
| TE-5 | Growth Inhibition Assay | IC50=8.42429 μM | SANGER | |||
| NCI-H1581 | Growth Inhibition Assay | IC50=8.26323 μM | SANGER | |||
| DOHH-2 | Growth Inhibition Assay | IC50=8.20095 μM | SANGER | |||
| EW-16 | Growth Inhibition Assay | IC50=8.08445 μM | SANGER | |||
| ECC10 | Growth Inhibition Assay | IC50=8.03395 μM | SANGER | |||
| IST-MEL1 | Growth Inhibition Assay | IC50=8.00406 μM | SANGER | |||
| TGBC1TKB | Growth Inhibition Assay | IC50=7.89398 μM | SANGER | |||
| COLO-678 | Growth Inhibition Assay | IC50=7.71076 μM | SANGER | |||
| SCC-25 | Growth Inhibition Assay | IC50=7.709 μM | SANGER | |||
| NB14 | Growth Inhibition Assay | IC50=7.66642 μM | SANGER | |||
| NCI-H1355 | Growth Inhibition Assay | IC50=7.58635 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 | |||
| 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 | ||
| 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 | |||
| 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 | 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 | ||
| 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 | ||
| 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 | |||
| 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 | ||
| Klicken Sie hier, um weitere experimentelle Daten zu Zelllinien anzuzeigen | ||||||
Chemische Informationen, Lagerung & Stabilität
| Molekulargewicht | 478.67 | Formel | C17H14ClF2IN2O2 |
Lagerung (Ab dem Eingangsdatum) | |
|---|---|---|---|---|---|
| CAS-Nr. | 212631-79-3 | SDF herunterladen | Lagerung von Stammlösungen |
|
|
| Synonyme | N/A | Smiles | C1CC1CONC(=O)C2=C(C(=C(C=C2)F)F)NC3=C(C=C(C=C3)I)Cl | ||
Löslichkeit
|
In vitro |
DMSO
: 96 mg/mL
(200.55 mM)
Ethanol : 14 mg/mL Water : Insoluble |
Molaritätsrechner
Verdünnungsrechner
Molekulargewichtsrechner
|
In vivo |
|||||
In-vivo-Formulierungsrechner (Klare Lösung)
Schritt 1: Geben Sie die untenstehenden Informationen ein (Empfohlen: Ein zusätzliches Tier zur Berücksichtigung von Verlusten während des Experiments)
mg/kg
g
μL
Schritt 2: Geben Sie die In-vivo-Formulierung ein (Dies ist nur der Rechner, keine Formulierung. Bitte kontaktieren Sie uns zuerst, wenn es im Abschnitt "Löslichkeit" keine In-vivo-Formulierung gibt.)
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
Berechnungsergebnisse:
Arbeitskonzentration: mg/ml;
Methode zur Herstellung der DMSO-Stammlösung: mg Wirkstoff vorgelöst in μL DMSO ( Konzentration der Stammlösung mg/mL, Bitte kontaktieren Sie uns zuerst, wenn die Konzentration die DMSO-Löslichkeit der Wirkstoffcharge überschreitet. )
Methode zur Herstellung der In-vivo-Formulierung: Nehmen Sie μL DMSO Stammlösung, dann hinzufügenμL PEG300, mischen und klären, dann hinzufügenμL Tween 80, mischen und klären, dann hinzufügen μL ddH2O, mischen und klären.
Methode zur Herstellung der In-vivo-Formulierung: Nehmen Sie μL DMSO Stammlösung, dann hinzufügen μL Maisöl, mischen und klären.
Hinweis: 1. Bitte stellen Sie sicher, dass die Flüssigkeit klar ist, bevor Sie das nächste Lösungsmittel hinzufügen.
2. Achten Sie darauf, das/die Lösungsmittel der Reihe nach hinzuzufügen. Sie müssen sicherstellen, dass die bei der vorherigen Zugabe erhaltene Lösung eine klare Lösung ist, bevor Sie mit der Zugabe des nächsten Lösungsmittels fortfahren. Physikalische Methoden wie Vortex, Ultraschall oder ein heißes Wasserbad können zur Unterstützung des Lösens verwendet werden.
Wirkmechanismus
| Merkmale |
First MEK inhibitor to begin clinical development.
|
|---|---|
| Targets/IC50/Ki |
MEK1
(Cell-free assay) 17 nM
MEK2
(Cell-free assay) 17 nM
|
| In vitro |
CI-1040-Behandlung führt zu einer Reduktion der pMAPK-Spiegel in mehreren Tumorzellen, einschließlich Kolon-26-, BX-PC3-Pankreas-, A431-Zervix-, HT-29-Kolon-, ZR-25-1-Brust- und SKOV-3-Ovarialkarzinomen. Die Behandlung mit dieser Verbindung hemmt nicht die Phosphorylierung von Jun-Kinase, p38-Kinase oder Akt, was darauf hindeutet, dass sie spezifisch MEK angreift. Die Hemmung der MAPK-Aktivierung durch diese Chemikalie verhindert den Zellzyklusfortschritt und induziert einen G1-Block. Die IC50 für die Hemmung von MEK1 durch diesen Inhibitor beträgt 0,3 μM, 15-mal höher als die Konzentration, die zur Hemmung der EGF-induzierten Aktivierung von ERK2 in Swiss 3T3-Zellen erforderlich ist. Diese Ergebnisse zeigen, dass dieser Wirkstoff seine Wirkung auf Zellen ausübt, indem er die Aktivierung von MKK1 unterdrückt und nicht, indem er deren Aktivität blockiert. 2 nM dieser Verbindung hemmt die Aktivierung von MKK1 in Swiss 3T3-Zellen um 50%, während eine über 100-fache Konzentration davon MEK1 in vitro hemmt. Es hemmt auch die Raf-katalysierte Phosphorylierung von MEK1 ohne Einfluss auf die Raf-katalysierte Phosphorylierung von Myelin-Basismembran-Protein. Diese Chemikalie hemmt 86% des Wachstums von papillären Schilddrüsenkarzinom (PTC)-Zellen mit der RET/PTC1-Rearrangement bei 10 μM im Vergleich zu Zellen, die nur mit DMSO behandelt wurden. Sie zeigt eine starke Hemmung von PTC-Zellen (BRAF-Mutation) mit einem GI50 von 52 nM, aber eine geringe Aktivität bei RET/PTC1-Rearrangement-Typ mit einem GI50 von 1,1 μM. Eine aktuelle Untersuchung zeigt, dass dieser Wirkstoff die apoptotische Wirkung von BMS-214662 in einer CML-Blastenkrisen-Zelllinie, K562, und in primären chronischen Phase CD34+ CML-Zellen verstärkt.
|
| Kinase-Assay |
MEK1 Assay
|
|
MAP kinase wird nach Phosphorylierung durch MEK aktiviert; die aktivierte MAP kinase phosphoryliert anschließend das Myelin-Basismembran-Protein (MBP). Der Einbau von 32P in das Myelin-Basismembran-Protein (MBP) wird in Gegenwart von Glutathion-S-Transferase (GST)-Fusionsproteinen, die die 44-kDa MAPK (GST-MAPK) oder die 45-kDa MEK (GST-MEK1) enthalten, gemessen. Die Assays werden in 50 μL 50 mM Tris, pH 7,4/10 mM MgCl2/2 mM EGTA/10 μM [γ-32P]ATP, enthaltend 10 μg GST-MEK1, 0,5 μg GST-MAPK und 40 μg MBP, durchgeführt. Nach Inkubation bei 30°C für 15 Minuten werden die Reaktionen durch Zugabe von Laemmli SDS-Probenpuffer gestoppt. Phosphoryliertes MBP wird mittels SDS/10% PAGE aufgetrennt. Diese Screening-Bemühungen führen zur Entdeckung mehrerer niedermolekularer Inhibitoren von MEK, d.h. PD184352 (CI-1040). Experimente zur Bestimmung der Zugabereihenfolge zeigen, dass diese Verbindung MEK1 direkt mit einer 50%igen Hemmkonzentration (IC50) von 17 nM hemmt, ohne die Aktivität von MAPK zu beeinflussen.
|
|
| In vivo |
Die orale Verabreichung von CI-1040 beeinträchtigt das Wachstum von Kolontumor-Xenotransplantaten von Maus und Mensch in einem breiten Dosisbereich von 48-200 mg/kg pro Dosis, jedoch nicht bei P388-Leukämie. Diese Verbindung hemmt die Tumorxenotransplantate von PTC-Zellen, die eine BRAF-Mutation tragen, mit einer Reduktion von 31,3% und von Zellen, die die RET/PTC1-Rearrangement tragen, mit einer Reduktion von 47,5% im Vergleich zu unbehandelten (Vehikel-)Mäusen nach 3 Wochen oraler Verabreichung (300 mg/kg/Tag). Es wurden keine toxischen Wirkungen bei Mäusen beobachtet, die mit dieser Chemikalie behandelt wurden. Eine vorübergehende Exposition von Mammakarzinomen gegenüber dieser Verbindung und UCN-01 führt zu Tumorzelltod in vivo und einer verlängerten Unterdrückung des Tumorwachstums. Die kombinierte Behandlung mit dieser Chemikalie (25 mg/kg) und UCN-01 (0,1-0,2 mg/kg) reduziert MDA-MB-231 signifikant und beseitigt weitgehend das MCF7-Tumorwachstum bei implantierten athymischen Mäusen, während jede Einzelbehandlung keine signifikante Aktivität aufweist. Die Medikamentenkombination führt zu einem tiefgreifenden Tumorzelltod, der mit einer Reduktion der Phosphorylierung von ERK1/2 und der Immunreaktivität von Ki67 und CD31 korreliert.
|
Literatur |
|
Anwendungen
| Methoden | Biomarker | Bilder | PMID |
|---|---|---|---|
| Western blot | p-ERK5 / ERK5 p-ERK1/2 / ERK1/2 |
|
21762482 |
| Growth inhibition assay | Cell viability |
|
29989268 |
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