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) Chemical Structure

PD184352 (CI-1040) Chemical Structure

CAS: 212631-79-3

Selleck's PD184352 (CI-1040) has been cited by 133 publications

Purity & Quality Control

Batch: Purity: 99.96%
99.96

PD184352 (CI-1040) Related Products

Signaling Pathway

Choose Selective MEK Inhibitors

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description 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
Click to View More Cell Line Experimental Data

Biological Activity

Description 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.
Features 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.
Cell Research Cell lines Colon 26 carcinoma cells
Concentrations 0.1-10 μM
Incubation Time 24 hours
Method

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.

Experimental Result Images Methods Biomarkers Images 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]
Animal Research Animal Models PTC cells in athymic mice
Dosages 150 mg/kg
Administration Orally twice daily

Chemical Information & Solubility

Molecular Weight 478.67 Formula

C17H14ClF2IN2O2

CAS No. 212631-79-3 SDF Download PD184352 (CI-1040) SDF
Smiles C1CC1CONC(=O)C2=C(C(=C(C=C2)F)F)NC3=C(C=C(C=C3)I)Cl
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 96 mg/mL ( (200.55 mM); Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 14 mg/mL

Water : Insoluble


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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