PD184352 (CI-1040)

For research use only.

Catalog No.S1020

89 publications

PD184352 (CI-1040) Chemical Structure

Molecular Weight(MW): 478.67

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. Phase 2.

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Selleck's PD184352 (CI-1040) has been cited by 89 publications

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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. Phase 2.
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

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]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
H9 MmnmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3niTmlEPTB;MD6wNlI4PiEQvF2= NXjXc2xLW0GQR1XS
CHP-212 Ml3MS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{DKSmlEPTB;MD6wNlg5PSEQvF2= NG\0e|hUSU6JRWK=
EoL-1-cell MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlXlTWM2OD1yLkC0NVUzKM7:TR?= MoDHV2FPT0WU
DU-4475 M4XjTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVOzVG1{UUN3ME2wMlA4PTl7IN88US=> NE\WTndUSU6JRWK=
MMAC-SF MmG4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3LFO2lEPTB;MD6xNFk4PCEQvF2= M{G3RnNCVkeHUh?=
AGS NYXZ[3RYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXLWNWF4UUN3ME2wMlEyPzF|IN88US=> MV3TRW5ITVJ?
M14 MnLDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHHJN5FKSzVyPUCuNVU1PjhizszN NYf0SWg3W0GQR1XS
CP50-MEL-B NXjHV|FJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnHMTWM2OD1yLkG3NlU1KM7:TR?= MmHtV2FPT0WU
C32 MmTnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mmf0TWM2OD1yLkG5NFczKM7:TR?= NEH6NohUSU6JRWK=
KMOE-2 MoK1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYnJR|UxRTBwMUm3PVUh|ryP MX\TRW5ITVJ?
A101D M3nh[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYXQTWZRUUN3ME2wMlIyPCEQvF2= M2DjSXNCVkeHUh?=
KM12 M1rTWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXvJR|UxRTBwMkSwOVch|ryP M{DucHNCVkeHUh?=
HSC-4 NX7QUno5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWHJR|UxRTBwMkSzPVUh|ryP NVvIeYJxW0GQR1XS
NOMO-1 NEDHcZhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVnJR|UxRTBwMkW3OFIh|ryP NYD5TpVkW0GQR1XS
MZ7-mel MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmjxTWM2OD1yLkK2N|Qh|ryP NXPBZZRMW0GQR1XS
ACN M2LPemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4P0[2lEPTB;MD6yOlc{PyEQvF2= M2OwTnNCVkeHUh?=
MEL-HO MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4faV2lEPTB;MD6yO|Y2OiEQvF2= NIHz[pJUSU6JRWK=
BHT-101 Ml65S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYLTbJlVUUN3ME2wMlI5PjB4IN88US=> MXfTRW5ITVJ?
SK-MEL-28 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{D6TmlEPTB;MD6zNFQxQSEQvF2= NUTDdYJjW0GQR1XS
KG-1 MlrBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4D5TGlEPTB;MD6zNFY3QCEQvF2= NHP2bnhUSU6JRWK=
COLO-679 NXm0eGVUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnvHTWM2OD1yLkOyO|Ih|ryP MmK0V2FPT0WU
SK-MEL-24 NXjGc3VXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlroTWM2OD1yLkOyPFE{KM7:TR?= NELPSGxUSU6JRWK=
G-361 NGDFU3NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4qyOGlEPTB;MD6zOlc6PSEQvF2= MULTRW5ITVJ?
KY821 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{KxUmlEPTB;MD6zO|kyKM7:TR?= MYXTRW5ITVJ?
KASUMI-1 NGLqW5hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4XmbWlEPTB;MD6zPVkh|ryP M1TJfnNCVkeHUh?=
HL-60 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFzEVHlKSzVyPUCuOFEyODdizszN MnfhV2FPT0WU
K5 NX[4Z|RHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYXJR|UxRTBwNEOxNVch|ryP M4jId3NCVkeHUh?=
KU812 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmrsTWM2OD1yLkS1Nlk6KM7:TR?= MXvTRW5ITVJ?
SH-4 Mlj4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVvJR|UxRTBwNE[yOVYh|ryP NFHWdGhUSU6JRWK=
HTC-C3 NH3LRWdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NILhUoVKSzVyPUCuOFY2OzFizszN NEi3Z3lUSU6JRWK=
CP66-MEL MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MljSTWM2OD1yLkS4PFA6KM7:TR?= NGnVV2VUSU6JRWK=
WM-115 NVLPXJR[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWDJR|UxRTBwNEmyOVch|ryP MnKwV2FPT0WU
A2780 NGjrc3hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXfJR|UxRTBwNEm4NlMh|ryP MXvTRW5ITVJ?
P12-ICHIKAWA NFf6N5BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYrJR|UxRTBwNkGyNlEh|ryP Mm\xV2FPT0WU
HMV-II M{O5Z2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmTuTWM2OD1yLk[0OFY2KM7:TR?= MUTTRW5ITVJ?
HT-144 NHnFdZlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3TqbmlEPTB;MD62OFY2PyEQvF2= NYHnO3N6W0GQR1XS
LB2518-MEL M3izV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2j5ZmlEPTB;MD63NVY{OiEQvF2= NH3seldUSU6JRWK=
NCI-SNU-1 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoXiTWM2OD1yLke1OFM{KM7:TR?= NGiyPY1USU6JRWK=
C2BBe1 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmnlTWM2OD1yLkixNFI{KM7:TR?= M2S0SXNCVkeHUh?=
PSN1 NXnKRnhUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVXJR|UxRTBwOU[xPVYh|ryP NXKzWYttW0GQR1XS
UACC-257 NGK2dFBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mo[3TWM2OD1yLkm2OFc{KM7:TR?= M{e2fnNCVkeHUh?=
RVH-421 NYXRR2VrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX\qVoZJUUN3ME2wMlk4OThizszN NF7pVVhUSU6JRWK=
GP5d MofUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYLoVVRsUUN3ME2wMlk5OzB6IN88US=> NVj3RYNbW0GQR1XS
TYK-nu MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIjnPZFKSzVyPUGuNFMyPzJizszN NF;TcHNUSU6JRWK=
SK-N-AS NWTUPZA6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnToTWM2OD1zLkC3PVQ4KM7:TR?= MV\TRW5ITVJ?
SW620 MmLKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHTscnRKSzVyPUGuNVM2OzRizszN MljOV2FPT0WU
HuP-T4 NYTpS|U5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHH2VYdKSzVyPUGuNVg{PTlizszN MknoV2FPT0WU
A549 NGDocWpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYDJR|UxRTFwMUm1O|Yh|ryP NVjuOW5zW0GQR1XS
Mewo NXHBc4RVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3\jeWlEPTB;MT6yNFI4PiEQvF2= MnXjV2FPT0WU
ONS-76 MniyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFHMcIxKSzVyPUGuNlIxPDlizszN NH\ido1USU6JRWK=
SK-MEL-1 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXXJR|UxRTFwMkO0NVkh|ryP NULmT2VmW0GQR1XS
RCM-1 NVvrd|NjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXPJR|UxRTFwMkSwOFch|ryP NWnjS3h[W0GQR1XS
H-EMC-SS M2m1Z2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1\ZSGlEPTB;MT6yPVYxQCEQvF2= NGL2bHFUSU6JRWK=
NCI-H2291 NUfDV4dOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYnJR|UxRTFwM{K1N|Yh|ryP NHLueZBUSU6JRWK=
SW1463 MlHyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVnJR|UxRTFwM{O3NlEh|ryP NYPxUVd5W0GQR1XS
LS-411N MlTOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWfJR|UxRTFwNEC1NVch|ryP NF;wNphUSU6JRWK=
BV-173 M{fzOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXTJR|UxRTFwNESwNVUh|ryP NVPofI1HW0GQR1XS
LS-513 MoXGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGPrZo9KSzVyPUGuOFUyQTJizszN MkPQV2FPT0WU
LoVo NXjvUnE3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIeyV2tKSzVyPUGuOFY{QTlizszN NEHVfWFUSU6JRWK=
HO-1-N-1 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3LNR2lEPTB;MT61NVY{PCEQvF2= NHHnNIpUSU6JRWK=
ML-2 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFT0fVlKSzVyPUGuOVI5PjhizszN Mn62V2FPT0WU
NCI-H1437 NWW4SGFET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlHLTWM2OD1zLkW1Nlc2KM7:TR?= MlzZV2FPT0WU
SW1116 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXHJR|UxRTFwNU[zPVgh|ryP MVzTRW5ITVJ?
A4-Fuk NHrVOnFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFPKUmtKSzVyPUGuOVcxPDVizszN NWP3fZZbW0GQR1XS
HD-MY-Z MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4G0XmlEPTB;MT61O|M4PiEQvF2= NFW0[nFUSU6JRWK=
SK-MEL-2 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MULJR|UxRTFwNUe0OVkh|ryP M{[yOHNCVkeHUh?=
RT-112 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVHJR|UxRTFwNUi5OVIh|ryP NUPQcG1UW0GQR1XS
COLO-829 NXHUZZU{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3PIemlEPTB;MT62NlI{OiEQvF2= NXqwUnhoW0GQR1XS
OVCAR-5 Ml;HS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV;JR|UxRTFwN{e2PFch|ryP NVu5Om5qW0GQR1XS
NB69 NHTzc4lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmixTWM2OD1zLke4OFY6KM7:TR?= Mm\qV2FPT0WU
NCI-H292 M13hVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1zSZmlEPTB;MT64OlY6QSEQvF2= MYXTRW5ITVJ?
LOXIMVI M3v6WWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnL4TWM2OD1zLki5OFI4KM7:TR?= MorhV2FPT0WU
BPH-1 M3fv[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3XNZWlEPTB;MT64PVU6OSEQvF2= Moe4V2FPT0WU
A375 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWfJR|UxRTFwOEm3NVQh|ryP NXjCcWpqW0GQR1XS
LCLC-97TM1 M1\OPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGHITpJKSzVyPUGuPVIzPTZizszN M3\pPHNCVkeHUh?=
RXF393 NUTh[25MT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX;JR|UxRTFwOUe4PFch|ryP NXrudYtVW0GQR1XS
HCC70 NFn5V3hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHfx[YJKSzVyPUKuNFI1OjZizszN MX;TRW5ITVJ?
EM-2 Mn62S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWry[HFnUUN3ME2yMlA4OTl6IN88US=> NWHQTVB2W0GQR1XS
MZ2-MEL MmnJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYL2dnRpUUN3ME2yMlEyOTJ5IN88US=> MXvTRW5ITVJ?
HN M2TR[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{HofmlEPTB;Mj6xOlI4QCEQvF2= MkjDV2FPT0WU
A2058 NFW1V21Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYnJR|UxRTJwMUmyO|kh|ryP NFOwTVdUSU6JRWK=
NB7 Mm\RS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHntO5pKSzVyPUKuN|QxQDZizszN MYHTRW5ITVJ?
DOK NHzX[GpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGGwNlhKSzVyPUKuN|U4PzNizszN M{iwRXNCVkeHUh?=
CAL-27 M3m4Omdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEfiT2lKSzVyPUKuN|kzOzZizszN MmDvV2FPT0WU
BB65-RCC NGnQT4FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3fmV2lEPTB;Mj60NFY4PCEQvF2= NEjjdHNUSU6JRWK=
RD NY\jcJE5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXflVlNyUUN3ME2yMlQ1PzJ|IN88US=> MoS3V2FPT0WU
KNS-62 NGn0O41Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVHJR|UxRTJwNUGxOlQh|ryP M1rEdnNCVkeHUh?=
EW-13 NIq3NFdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVX6UYU{UUN3ME2yMlU3OzN7IN88US=> NIPRNpdUSU6JRWK=
DB NFjKU3BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{HJU2lEPTB;Mj61PFc5QCEQvF2= NYTxXmZoW0GQR1XS
HCC2218 NWLKWFZyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFL6S|hKSzVyPUKuOlQ4PzhizszN MnXYV2FPT0WU
L-363 NEPVe4FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH:0eFVKSzVyPUKuO|Q{PyEQvF2= NXzsN45DW0GQR1XS
CHL-1 M4PCR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M13sdWlEPTB;Mj64NFc5PSEQvF2= MWTTRW5ITVJ?
BFTC-905 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGG2VnlKSzVyPUKuPFI2OyEQvF2= M2DQW3NCVkeHUh?=
HCE-T NVT0SoFZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV\JR|UxRTJwOEOyOlQh|ryP M1joV3NCVkeHUh?=
COLO-792 NEf5PIJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml7xTWM2OD1{Lki0NFI4KM7:TR?= NWnld4ZEW0GQR1XS
LB2241-RCC M1;FcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHvqeVFKSzVyPUKuPFU5QTNizszN M3LYWXNCVkeHUh?=
CAL-39 MkLaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mm\pTWM2OD1{Lki5PVk6KM7:TR?= NGHyU2pUSU6JRWK=
T-24 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUTUS|BxUUN3ME2yMlkyOTF{IN88US=> M{O2enNCVkeHUh?=
NCI-H727 NG[wTnVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV;JR|UxRTJwOUG3PVYh|ryP MmOyV2FPT0WU
Ca9-22 NUfxc|QzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn3qTWM2OD1{Lkm3NlU2KM7:TR?= NE\5SVNUSU6JRWK=
MIA-PaCa-2 Ml6yS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkHMTWM2OD1|LkCwO|gyKM7:TR?= NVvyZY1pW0GQR1XS
HT-1080 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUnJR|UxRTNwMEG5PVch|ryP M{\1UnNCVkeHUh?=
D-423MG NWr3eHNUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUTJR|UxRTNwMEe3OVMh|ryP M3;TSHNCVkeHUh?=
LAMA-84 MnXmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4m5OGlEPTB;Mz6xN|U5KM7:TR?= NHX2bGRUSU6JRWK=
SW780 NXrLPZd{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkHxTWM2OD1|LkG0NlI6KM7:TR?= NWO3dldFW0GQR1XS
KU-19-19 NIXaTVhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWnJR|UxRTNwMUewN|Qh|ryP NYXaVGdFW0GQR1XS
COLO-741 NGHxe3NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYHRU3ZwUUN3ME2zMlE5Pjd|IN88US=> NXviXnVNW0GQR1XS
HSC-3 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWDJR|UxRTNwMkOxOVEh|ryP MWXTRW5ITVJ?
SN12C NFrmdWJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1vEOWlEPTB;Mz6yOFcxOSEQvF2= MmDYV2FPT0WU
786-0 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHXWVYhKSzVyPUOuNlczPDNizszN M1K3O3NCVkeHUh?=
GAK MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoXGTWM2OD1|LkOyOVYyKM7:TR?= NIHJXJJUSU6JRWK=
PANC-03-27 NUTofHVyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWLmNXNXUUN3ME2zMlM2ODR3IN88US=> MoL2V2FPT0WU
CTB-1 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVPxepFPUUN3ME2zMlQ4ODR5IN88US=> NVHkdVhOW0GQR1XS
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Hs-578-T MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkL4TWM2OD13LkWzO|k1KM7:TR?= MXnTRW5ITVJ?
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NCI-H1304 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M13TcGlEPTB;Nj6xPVk1KM7:TR?= NXjOclFTW0GQR1XS
RPMI-8866 M4HwPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYHGb2F3UUN3ME22MlIyOzF|IN88US=> Ml:5V2FPT0WU
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NCI-H1975 NGLCTm5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGPicY9KSzVyPU[uOFczOTVizszN Mn7WV2FPT0WU
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NCI-H2347 NFXyR|VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF[2T5hKSzVyPUG0MlgzOyEQvF2= MkjhV2FPT0WU
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OC-314 NV\0fHdJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYXLOWNkUUN3ME2xPE44Ozh2IN88US=> NIXjW5FUSU6JRWK=
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RO82-W-1 MnX6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2HwSGlEPTB;MUiuPFI5QCEQvF2= MV3TRW5ITVJ?
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NCI-H1048 M3jJfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mm\XTWM2OD1{MD6zNlY3KM7:TR?= M3vrSXNCVkeHUh?=
NCI-H226 NWO4ZnFIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1fpd2lEPTB;MkCuOFM6QSEQvF2= NIfXVIlUSU6JRWK=
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SF539 NYXSNnNpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3HWTGlEPTB;MkCuOVE4OiEQvF2= NV\5[mRWW0GQR1XS
TE-6 NV[1dVJpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3L3VWlEPTB;MkCuPFA3PyEQvF2= Mn;4V2FPT0WU
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Becker NF[yZ5BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MofMTWM2OD1{MT6xNVE5KM7:TR?= NFS4UHhUSU6JRWK=
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TE-1 M3frSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2C5S2lEPTB;MkWuNFQ6QSEQvF2= MVnTRW5ITVJ?
EW-3 M17ZSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn64TWM2OD1{NT6xNVMh|ryP Ml\pV2FPT0WU
PANC-08-13 M3HxWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHHs[npKSzVyPUK1MlgyODNizszN Ml3CV2FPT0WU
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BT-20 NWDaSJZwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHvsTVhKSzVyPUK2MlQ2PDNizszN MV\TRW5ITVJ?
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TE-11 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmW1TWM2OD1{Nj65PFk2KM7:TR?= NYS1WnZGW0GQR1XS
ESS-1 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUnJR|UxRTJ5LkOyNVYh|ryP NEfGWIpUSU6JRWK=
JVM-3 MlnoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWfJR|UxRTJ5Lk[0O|Uh|ryP MV\TRW5ITVJ?
C3A MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHX1WVFKSzVyPUK3Mlg1QTZizszN NXm1WmVHW0GQR1XS
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KLE MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mlv3TWM2OD1{OD6xNFU5KM7:TR?= MYXTRW5ITVJ?
ES1 M4PUdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnjYTWM2OD1{OD6xPFM5KM7:TR?= MVHTRW5ITVJ?
CAL-120 MnntS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWXJR|UxRTJ6LkO5PVkh|ryP MYfTRW5ITVJ?
NCI-N87 Mlu4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVzJR|UxRTJ6LkWxNFUh|ryP MlzoV2FPT0WU
RPMI-8226 M1HmPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnTTTWM2OD1{OT6xPFQ{KM7:TR?= Mo\XV2FPT0WU
COR-L88 M2m1fGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoK2TWM2OD1{OT6yOFE6KM7:TR?= NIPuTVNUSU6JRWK=
UACC-893 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUDJR|UxRTJ7LkOxN|ch|ryP MWjTRW5ITVJ?
C8166 NFjyepJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mo\pTWM2OD1{OT65PVk3KM7:TR?= MVfTRW5ITVJ?
J82 MojNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWDWT29HUUN3ME2zNE45OTR5IN88US=> MV7TRW5ITVJ?
PFSK-1 MlS2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2\xSGlEPTB;M{GuNFY2QSEQvF2= NVrxSXkxW0GQR1XS
COLO-684 NWeyNmpXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmPsTWM2OD1|MT60N|c1KM7:TR?= NX3mZ2d2W0GQR1XS
CAL-72 NYLpWXNsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVLJR|UxRTNzLkW3Nlkh|ryP MmfuV2FPT0WU
SNB75 NULrZoNqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVHJR|UxRTNzLki5O{DPxE1? NVzzfmdGW0GQR1XS
MDA-MB-415 NHfhTFRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH;GTndKSzVyPUOxMlk4PjJizszN NFHVfFhUSU6JRWK=
SiHa NXPBOFJ[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml3vTWM2OD1|Mj60O|EyKM7:TR?= M3f4TnNCVkeHUh?=
NCI-H1648 M{fadmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1vTXmlEPTB;M{KuPVM1PSEQvF2= MoLMV2FPT0WU
EFO-21 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVn5UJZCUUN3ME2zN{4xODVizszN M3XUOXNCVkeHUh?=
HCC38 NVTHNnh1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEjh[lJKSzVyPUOzMlM5PDFizszN MYrTRW5ITVJ?
IA-LM NEG4PYFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnHnTWM2OD1|Mz63PFg6KM7:TR?= MVfTRW5ITVJ?
CTV-1 M1vqW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEmxbnFKSzVyPUOzMlk4QDZizszN NF:1SHJUSU6JRWK=
NCI-H446 NYnqe4FVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGnFbFZKSzVyPUO0MlI3QDlizszN NE\JWGxUSU6JRWK=
IST-SL1 MkT1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH;VWmFKSzVyPUO0Mlc1ODhizszN MmXyV2FPT0WU
EW-22 NWfzZlFTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV\ZSY1pUUN3ME2zOE44PzV7IN88US=> NWq1XGRzW0GQR1XS
JEG-3 NV;nZpM5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NW\qU4tNUUN3ME2zOk4yPzZ4IN88US=> NHi1eZlUSU6JRWK=
LU-65 MkPvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVPJR|UxRTN4LkK5PFUh|ryP M2HvUHNCVkeHUh?=
NCI-H596 NW\3NHBbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHTMRo5KSzVyPUO2Mlk2QTFizszN MXnTRW5ITVJ?
KNS-81-FD MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWDJR|UxRTN5LkG0OUDPxE1? M3;NR3NCVkeHUh?=
NCI-H1793 NIDzenRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MW\JR|UxRTN5LkewPFYh|ryP NF;OZnFUSU6JRWK=
NCI-H460 MoHKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYPJR|UxRTN6LkC4O|Mh|ryP MVrTRW5ITVJ?
MPP-89 M37xXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2X2TWlEPTB;M{muOVg5PiEQvF2= MnS0V2FPT0WU
D-542MG NFrpUXRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV;JR|UxRTN7Lki0N|Yh|ryP NHHBV5hUSU6JRWK=
JAR NUW0XGZ3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUHicYZkUUN3ME20NE41PzB3IN88US=> NGXtbllUSU6JRWK=
NCI-H209 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mli3TWM2OD12MD62O|ch|ryP MYDTRW5ITVJ?
G-402 M2j3Zmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVjJR|UxRTRzLkO5PVMh|ryP NVrkW4dSW0GQR1XS
IST-MES1 NFfodmVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXPJR|UxRTR{LkG5N|Uh|ryP NVHseWF1W0GQR1XS
Daoy NEPMeFNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWrJR|UxRTR{LkW0O|Eh|ryP NXHkcmlsW0GQR1XS
EW-11 NXTrbW82T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYDJR|UxRTR|LkGyNVEh|ryP M2fFW3NCVkeHUh?=
Saos-2 M1PyRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYHJR|UxRTR|LkG1N|ch|ryP NY\5dHZPW0GQR1XS
no-10 NHjuUFlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXLJR|UxRTR|LkG3NFIh|ryP MnTXV2FPT0WU
HCC1395 MkjKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnfWTWM2OD12Mz60OlQ1KM7:TR?= NXHBR2dTW0GQR1XS
HCE-4 MkT6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1LEcGlEPTB;NEOuO|Y3PCEQvF2= MWfTRW5ITVJ?
EW-1 M4PkUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnPyTWM2OD12Mz64NFQ6KM7:TR?= Ml6yV2FPT0WU
OCUB-M NGnkc4tIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml\ETWM2OD12ND6zOlM5KM7:TR?= NH3DZpRUSU6JRWK=
IGR-1 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFu0WmRKSzVyPUS0MlQyOTVizszN NEj1cnVUSU6JRWK=
NCI-H1838 NILkPWRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF71[XNKSzVyPUS0MlQ{PDlizszN M1O4b3NCVkeHUh?=
NCI-H2405 NXLVUZVtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mm\YTWM2OD12ND61N|Qh|ryP NUfBZYJpW0GQR1XS
GB-1 NWPxOVdjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{\xdmlEPTB;NESuO|Q3OyEQvF2= MlmzV2FPT0WU
MG-63 NVjWeWtbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mm\UTWM2OD12Nj6wOlk3KM7:TR?= MUfTRW5ITVJ?
KP-N-YN NH\Nbm9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEnPVHZKSzVyPUS2MlQ3PzlizszN M4Owd3NCVkeHUh?=
no-11 MkHJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmTBTWM2OD12Nz6wNlQ1KM7:TR?= NWe1ZnB[W0GQR1XS
SW948 NFHRUoVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV\JR|UxRTR5LkOzO|ch|ryP NVHPfFg6W0GQR1XS
CAMA-1 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXLUc4piUUN3ME20O{4{PDN6IN88US=> NF\vO3JUSU6JRWK=
HCC1187 NV\sU2VXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWnJR|UxRTR5LkWxJO69VQ>? NYXvOpM4W0GQR1XS
D-392MG NFnScW9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnS3TWM2OD12Nz62OVE3KM7:TR?= MnXnV2FPT0WU
647-V MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoHOTWM2OD12OT6zOFE1KM7:TR?= MnvWV2FPT0WU

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
p-ERK1/2 / ERK1/2 ; 

PubMed: 21762482     


Effect of PD184352 on phosphorylation of ERK1/2 in sympathetic neurons. Immunoblots were performed with whole cell extracts from sympathetic neurons maintained in the presence of NGF and left untreated or treated with PD184352 at 0.1, 1, 2 or 10 μM for 16 hours. Antibodies to detect total ERK1/2 and phospho-ERK1/2 were used. 

p-ERK5 / ERK5 ; 

PubMed: 21762482     


Effect of PD184352 on phosphorylation of ERK5 in sympathetic neurons.

21762482
Growth inhibition assay
Cell viability; 

PubMed: 29989268     


Relative viability of DU145CR cells treated with PD184352 was significantly less than that of DU145 cells in WST assay. 

29989268
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]

Protocol

Kinase Assay:

[2]

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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:

[1]

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  • 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.


    (Only for Reference)
Animal Research:

[3]

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  • Animal Models: PTC cells in athymic mice
  • Dosages: 150 mg/kg
  • Administration: Orally twice daily
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 96 mg/mL (200.55 mM)
Water Insoluble
Ethanol '14 mg/mL
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
30% PEG400+0.5% Tween80+5% propylene glycol, pH 9
For best results, use promptly after mixing.
10 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 478.67
Formula

C17H14ClF2IN2O2

CAS No. 212631-79-3
Storage powder
in solvent
Synonyms N/A
Smiles C1CC1CONC(=O)C2=C(C(=C(C=C2)F)F)NC3=C(C=C(C=C3)I)Cl

In vivo Formulation Calculator (Clear solution)

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Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Mass Concentration Volume Molecular Weight

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.

Handling Instructions

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID