연구용
PD184352 (CI-1040) MEK 억제제
제품 번호S1020
화학 구조
분자량: 478.67
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품질 관리
배치:
순도:
99.96%
99.96
세포 배양, 처리 및 작업 농도
| 세포주 | 분석 유형 | 농도 | 배양 시간 | 제형 | 활성 설명 | 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 | ||
| 클릭하여 더 많은 세포주 실험 데이터 보기 | ||||||
화학 정보, 보관 및 안정성
| 분자량 | 478.67 | 화학식 | C17H14ClF2IN2O2 |
보관 (수령일로부터) | |
|---|---|---|---|---|---|
| CAS 번호 | 212631-79-3 | SDF 다운로드 | 원액 보관 |
|
|
| 동의어 | N/A | Smiles | C1CC1CONC(=O)C2=C(C(=C(C=C2)F)F)NC3=C(C=C(C=C3)I)Cl | ||
용해도
|
In vitro |
DMSO
: 96 mg/mL
(200.55 mM)
Ethanol : 14 mg/mL Water : Insoluble |
몰농도 계산기
희석 계산기
분자량 계산기
|
In vivo |
|||||
생체 내 제형 계산기 (투명한 용액)
1단계: 아래 정보 입력 (권장: 실험 중 손실을 고려하여 추가 동물 포함)
mg/kg
g
μL
2단계: 생체 내 제형 입력 (이것은 계산기일 뿐 제형이 아닙니다. 용해도 섹션에 생체 내 제형이 없는 경우 먼저 당사에 문의하십시오.)
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
계산 결과:
작업 농도: mg/ml;
DMSO 원액 준비 방법: mg 약물 사전 용해 μL DMSO ( 원액 농도 mg/mL, 농도가 해당 약물 배치의 DMSO 용해도를 초과하는 경우 먼저 당사에 문의하십시오. )
생체 내 제형 준비 방법: 취하다 μL DMSO 원액, 다음 추가μL PEG300, 혼합하고 투명하게 한 다음 추가μL Tween 80, 혼합하고 투명하게 한 다음 추가 μL ddH2O, 혼합하고 투명하게 합니다.
생체 내 제형 준비 방법: 취하다 μL DMSO 원액, 다음 추가 μL 옥수수 기름, 혼합하고 투명하게 합니다.
참고: 1. 다음 용매를 추가하기 전에 액체가 투명한지 확인하십시오.
2. 용매를 순서대로 추가해야 합니다. 다음 용매를 추가하기 전에 이전 추가에서 얻은 용액이 투명한 용액인지 확인해야 합니다. 와동, 초음파 또는 뜨거운 물 중탕과 같은 물리적 방법을 사용하여 용해를 도울 수 있습니다.
작용 메커니즘
| 특징 |
First MEK inhibitor to begin clinical development.
|
|---|---|
| Targets/IC50/Ki |
MEK1
(Cell-free assay) 17 nM
MEK2
(Cell-free assay) 17 nM
|
| 시험관 내(In vitro) |
CI-1040 치료는 Colon 26, BX-PC3 췌장암, A431 자궁경부암, HT-29 결장암, ZR-25-1 유방암 및 SKOV-3 난소암을 포함한 여러 종양 세포에서 pMAPK 수준의 감소를 유발합니다. 이 화합물 치료는 Jun 키나아제, p38 키나아제 또는 Akt의 인산화를 억제하지 않으며, 이는 MEK를 특이적으로 표적화함을 나타냅니다. 이 화학 물질에 의한 MAPK 활성화 억제는 세포 주기 진행을 막고 G1 블록을 유도합니다. 이 억제제에 의한 MEK1 억제에 대한 IC50은 0.3 μM이며, Swiss 3T3 세포에서 EGF 유도 ERK2 활성화를 억제하는 데 필요한 농도보다 15배 높습니다. 이 결과는 이 물질이 MKK1의 활성화를 억제함으로써 세포에 영향을 미치며, 그 활성을 차단함으로써 작용하는 것이 아님을 나타냅니다. 2 nM의 이 화합물은 Swiss 3T3 세포에서 MKK1의 활성화를 50% 억제하는 반면, 100배 이상의 농도는 시험관 내에서 MEK1을 억제합니다. 또한 Raf가 촉매하는 MEK1의 인산화를 억제하며, Raf가 촉매하는 미엘린 기본 단백질의 인산화에는 아무런 영향을 미치지 않습니다. 이 화학물질은 RET/PTC1 재배열을 가진 유두상 갑상선암(PTC) 세포 성장 중 86%를 10μM에서 DMSO만 처리한 세포와 비교하여 억제합니다. BRAF 돌연변이를 가진 PTC 세포에 대해 52 nM의 GI50으로 강력한 억제를 보이지만, RET/PTC1 재배열 유형에 대해서는 1.1 μM의 GI50으로 낮은 활성을 보입니다. 최근 연구에 따르면 이 물질은 CML blast crisis 세포주인 K562와 원발성 만성기 CD34+ CML 세포에서 BMS-214662의 apoptosis 효과를 증가시킵니다.
|
| 키나아제 분석 |
MEK1 분석
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MAP 키나아제는 MEK에 의한 인산화 후 활성화됩니다. 활성화된 MAP 키나아제는 이어서 미엘린 기본 단백질(MBP)을 인산화합니다. 미엘린 기본 단백질(MBP)로의 32P 통합은 44-kDa MAPK(GST-MAPK) 또는 45-kDa MEK(GST-MEK1)를 포함하는 글루타티온 S-트랜스퍼라제(GST) 융합 단백질의 존재 하에 분석됩니다. 분석은 50μL의 50mM Tris, pH 7.4/10mM MgCl2 /2mM EGTA/10μM [γ-32P]ATP에 10μg의 GST-MEK1, 0.5μg의 GST-MAPK, 40μg의 MBP를 포함하여 수행됩니다. 30°C에서 15분간 인큐베이션 후, Laemmli SDS 샘플 완충액을 첨가하여 반응을 중단시킵니다. 인산화된 MBP는 SDS/10% PAGE로 분리됩니다. 이 스크리닝 노력은 PD184352 (CI-1040)와 같은 여러 MEK 소분자 억제제의 발견으로 이어집니다. 첨가 순서를 평가하는 실험은 이 화합물이 MAP 키나아제 활성에 영향을 미치지 않고 17 nM의 50% 억제 농도(IC50)로 MEK1을 직접 억제한다는 것을 보여줍니다.
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| 생체 내(In vivo) |
CI-1040 경구 투여는 48-200 mg/kg 용량 범위로 마우스 및 인간의 대장 종양 이종이식편 성장을 손상시키지만, P388 백혈병은 손상시키지 않습니다. 이 화합물은 BRAF 돌연변이를 가진 PTC 세포의 종양 이종이식편을 31.3% 감소시키고, RET/PTC1 재배열을 가진 종양 이종이식편을 경구 투여(300 mg/kg/d) 3주 후 미처리(부형제) 마우스보다 47.5% 감소시킵니다. 이 화학 물질로 치료된 마우스에서는 독성 효과가 관찰되지 않았습니다. 유방암에 대한 이 화합물과 UCN-01의 일시적인 노출은 생체 내에서 종양 세포 사멸을 유발하고 종양 재성장을 장기간 억제합니다. 이 화학 물질(25 mg/kg)과 UCN-01(0.1-0.2 mg/kg)의 병용 치료는 이식된 무흉선 마우스에서 MDA-MB-231을 유의하게 감소시키고 MCF7 종양 성장을 크게 억제하는 반면, 단일 치료는 유의한 활성을 나타내지 않습니다. 약물 조합은 ERK1/2 인산화 및 Ki67 및 CD31의 면역 반응성 감소와 상관관계가 있는 심각한 종양 세포 사멸을 유발합니다.
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적용 분야
| 방법 | 바이오마커 | 이미지 | PMID |
|---|---|---|---|
| Western blot | p-ERK5 / ERK5 p-ERK1/2 / ERK1/2 |
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21762482 |
| Growth inhibition assay | Cell viability |
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29989268 |
기술 지원
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