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.

PD184352 (CI-1040)化学構造

CAS No. 212631-79-3

サイズ 価格(税別) 在庫状況
10mM (1mL in DMSO) JPY 25200 国内在庫あり
JPY 13600 国内在庫あり
JPY 21900 国内在庫あり
JPY 46800 国内在庫あり
JPY 113200 国内在庫あり

代表番号: 045-509-1970|電子メール:[email protected]
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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
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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
MEK1 [1]
(Cell-free assay)
MEK2 [1]
(Cell-free assay)
17 nM 17 nM
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. CI-1040 treatment doesn't inhibit the phosphorylation of Jun kinase, p38 kinase or Akt, indicating CI-1040 specifically targets MEK. Inhibition of MAPK activation by CI-1040 prevents cell cycle progression and induces a G1 block. [1] The IC50 for inhibition of MEK1 by CI-1040 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 CI-1040 exerts its effects on cells by suppressing the activation of MKK1, and not by blocking its activity. 2 nM PD184352 inhibits the activation of MKK1 in Swiss 3T3 cells by 50%, while over 100-fold concentration of CI-1040 inhibits MEK1 in vitro. PD184352 also inhibits the Raf-catalysed phosphorylation of MEK1 without any effect on the Raf-catalysed phosphorylation of myelin basic protein. [2] CI-1040 inhibits 86% of papillary thyroid carcinoma (PTC) cell growth with the RET/PTC1 rearrangement at 10μM compared with cells treated with DMSO only. CI-1040 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 CI-1040 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. CI-1040. Experiments assessing the order of addition shows that CI-1040 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 CI-1040. 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] CI-1040 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 CI-1040. [2] Transient exposure of mammary tumors to CI-1040 and UCN-01 causes tumor cell death in vivo and prolonged suppression of tumor regrowth. Combined treatment with CI-1040 (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
Batch:

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
Batch:

Add solvents to the product individually and in order.

投与溶液組成計算機

実験計算

モル濃度計算器

質量 濃度 体積 分子量

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

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。

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