PD184352 (CI-1040)

Catalog No.S1020

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. Phase 2.

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In DMSO USD 140 In stock
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Cited by 48 Publications

Purity & Quality Control

Choose Selective MEK Inhibitors

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. 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 NVKzfYhCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3LaXWlEPTB;MD6wNlI4PiEQvF2= MmXjV2FPT0WU
CHP-212 Mo[3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWnJR|UxRTBwMEK4PFUh|ryP MoXvV2FPT0WU
EoL-1-cell NHq3dIZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIr5eW9KSzVyPUCuNFQyPTJizszN MWjTRW5ITVJ?
DU-4475 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmDYTWM2OD1yLkC3OVk6KM7:TR?= NHLacYdUSU6JRWK=
MMAC-SF MlzDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{TWU2lEPTB;MD6xNFk4PCEQvF2= M4Tw[3NCVkeHUh?=
AGS NFjWZlRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmfsTWM2OD1yLkGxO|E{KM7:TR?= MlHxV2FPT0WU
M14 MlTES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFjwcGhKSzVyPUCuNVU1PjhizszN NWTYeVdtW0GQR1XS
CP50-MEL-B MmHzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWfJR|UxRTBwMUeyOVQh|ryP NUPFe2IzW0GQR1XS
C32 MnfQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4jyUWlEPTB;MD6xPVA4OiEQvF2= MXzTRW5ITVJ?
KMOE-2 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYPJR|UxRTBwMUm3PVUh|ryP M1HYbHNCVkeHUh?=
A101D NWrXdIpRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlrGTWM2OD1yLkKxOEDPxE1? NEO3TphUSU6JRWK=
KM12 NXX4dWlxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVy0OGk5UUN3ME2wMlI1ODV5IN88US=> MWfTRW5ITVJ?
HSC-4 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYrJR|UxRTBwMkSzPVUh|ryP NGHWfnVUSU6JRWK=
NOMO-1 MlfjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2T3VmlEPTB;MD6yOVc1OiEQvF2= MlHOV2FPT0WU
MZ7-mel MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHPRU3ZKSzVyPUCuNlY{PCEQvF2= NFG4TZNUSU6JRWK=
ACN NUXPWGRoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2Lqb2lEPTB;MD6yOlc{PyEQvF2= NHvBdINUSU6JRWK=
MEL-HO Moe3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnW0TWM2OD1yLkK3OlUzKM7:TR?= NUfu[W9jW0GQR1XS
BHT-101 M1nMU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGDYV3FKSzVyPUCuNlg3ODZizszN NIrmbWlUSU6JRWK=
SK-MEL-28 MoG5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3XaPGlEPTB;MD6zNFQxQSEQvF2= NECyUnVUSU6JRWK=
KG-1 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV3JR|UxRTBwM{C2Olgh|ryP NIq4dZZUSU6JRWK=
COLO-679 Mkn4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1;I[mlEPTB;MD6zNlczKM7:TR?= MnTrV2FPT0WU
SK-MEL-24 M3LuT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHPYVnFKSzVyPUCuN|I5OTNizszN M2O3TnNCVkeHUh?=
G-361 MkftS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWewWmFCUUN3ME2wMlM3Pzl3IN88US=> M4XTV3NCVkeHUh?=
KY821 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoTvTWM2OD1yLkO3PVEh|ryP Mn;PV2FPT0WU
KASUMI-1 MnHUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnXPTWM2OD1yLkO5PUDPxE1? MVjTRW5ITVJ?
HL-60 NYLmd|Y4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1jvV2lEPTB;MD60NVExPyEQvF2= MUPTRW5ITVJ?
K5 NWfKR2xLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MW\JR|UxRTBwNEOxNVch|ryP MmfnV2FPT0WU
KU812 NWDuS|FYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXLXPI1OUUN3ME2wMlQ2Ojl7IN88US=> NHrxVnFUSU6JRWK=
SH-4 NFTaPVlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mm\UTWM2OD1yLkS2NlU3KM7:TR?= MUDTRW5ITVJ?
HTC-C3 NYDHTVFNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn;TTWM2OD1yLkS2OVMyKM7:TR?= MlWwV2FPT0WU
CP66-MEL NVTnVYhPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYPJR|UxRTBwNEi4NFkh|ryP M1jtfnNCVkeHUh?=
WM-115 MojvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWLJR|UxRTBwNEmyOVch|ryP NGG1[llUSU6JRWK=
A2780 NWfpc|l5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkfzTWM2OD1yLkS5PFI{KM7:TR?= M3LaWXNCVkeHUh?=
P12-ICHIKAWA NXjYcYR3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF\OWGRKSzVyPUCuOlEzOjFizszN M4Hne3NCVkeHUh?=
HMV-II NX;FSYdjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWLxfoVnUUN3ME2wMlY1PDZ3IN88US=> M1LFeHNCVkeHUh?=
HT-144 Mo[wS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGW1bFlKSzVyPUCuOlQ3PTdizszN MojDV2FPT0WU
LB2518-MEL MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV3JR|UxRTBwN{G2N|Ih|ryP M3\JOXNCVkeHUh?=
NCI-SNU-1 NFHveGZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1z6O2lEPTB;MD63OVQ{OyEQvF2= MX\TRW5ITVJ?
C2BBe1 NW\xUJQyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVzJR|UxRTBwOEGwNlMh|ryP M{\YTnNCVkeHUh?=
PSN1 NFLUPVVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXXqSG0zUUN3ME2wMlk3OTl4IN88US=> NYTQcYU4W0GQR1XS
UACC-257 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXvJR|UxRTBwOU[0O|Mh|ryP MUfTRW5ITVJ?
RVH-421 NUTHVJAzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF;CPJRKSzVyPUCuPVcyQCEQvF2= NXLVSWhWW0GQR1XS
GP5d MlS2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV\JR|UxRTBwOUizNFgh|ryP NF65XldUSU6JRWK=
TYK-nu M2joW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnzYTWM2OD1zLkCzNVczKM7:TR?= M3z0S3NCVkeHUh?=
SK-N-AS NGG3PZNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXrJR|UxRTFwMEe5OFch|ryP MYnTRW5ITVJ?
SW620 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVnPO5UzUUN3ME2xMlE{PTN2IN88US=> MYPTRW5ITVJ?
HuP-T4 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX33eo5HUUN3ME2xMlE5OzV7IN88US=> MnO1V2FPT0WU
A549 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MW\JR|UxRTFwMUm1O|Yh|ryP NFnyS4ZUSU6JRWK=
Mewo NXnKOWd2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYm3RmlQUUN3ME2xMlIxOjd4IN88US=> M3vFPXNCVkeHUh?=
ONS-76 NXHSS5k4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3niZWlEPTB;MT6yNlA1QSEQvF2= NUDIcmRyW0GQR1XS
SK-MEL-1 M3PJbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXfy[JZpUUN3ME2xMlI{PDF7IN88US=> Ml7YV2FPT0WU
RCM-1 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MofGTWM2OD1zLkK0NFQ4KM7:TR?= M2na[nNCVkeHUh?=
H-EMC-SS M2rjVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWDJR|UxRTFwMkm2NFgh|ryP NVi1OoNXW0GQR1XS
NCI-H2291 NUW5flZvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmLhTWM2OD1zLkOyOVM3KM7:TR?= Mn;GV2FPT0WU
SW1463 NGLpXZlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXjJR|UxRTFwM{O3NlEh|ryP NXHBNHpPW0GQR1XS
LS-411N M1zmN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEHLfFVKSzVyPUGuOFA2OTdizszN M3Lhe3NCVkeHUh?=
BV-173 NX7KVnZTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{fIRmlEPTB;MT60OFAyPSEQvF2= MXvTRW5ITVJ?
LS-513 MmnTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4[wb2lEPTB;MT60OVE6OiEQvF2= NEfBeohUSU6JRWK=
LoVo MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn24TWM2OD1zLkS2N|k6KM7:TR?= NGDxW5FUSU6JRWK=
HO-1-N-1 MoT2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NInTfI9KSzVyPUGuOVE3OzRizszN M3zD[3NCVkeHUh?=
ML-2 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYnJR|UxRTFwNUK4Olgh|ryP NWXMOIRxW0GQR1XS
NCI-H1437 NWrtXW5XT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXPJR|UxRTFwNUWyO|Uh|ryP MmLyV2FPT0WU
SW1116 NEnKNZhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVfvd2hlUUN3ME2xMlU3Ozl6IN88US=> M1i5OnNCVkeHUh?=
A4-Fuk NYPMW5JvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnHKTWM2OD1zLkW3NFQ2KM7:TR?= MkXnV2FPT0WU
HD-MY-Z MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUDJR|UxRTFwNUezO|Yh|ryP MnLPV2FPT0WU
SK-MEL-2 NYToPHJZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlfNTWM2OD1zLkW3OFU6KM7:TR?= MXjTRW5ITVJ?
RT-112 MlHlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFmxdHpKSzVyPUGuOVg6PTJizszN M2\vXnNCVkeHUh?=
COLO-829 Mn:4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkPqTWM2OD1zLk[yNlMzKM7:TR?= NFL2d5hUSU6JRWK=
OVCAR-5 NWnQXIk4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVLJR|UxRTFwN{e2PFch|ryP NF74dWtUSU6JRWK=
NB69 NVrpVYZJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkHxTWM2OD1zLke4OFY6KM7:TR?= NUHSOXJLW0GQR1XS
NCI-H292 MlPNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4nONGlEPTB;MT64OlY6QSEQvF2= MWTTRW5ITVJ?
LOXIMVI MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHjxcnZKSzVyPUGuPFk1OjdizszN MkPWV2FPT0WU
BPH-1 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXvnVnBnUUN3ME2xMlg6PTlzIN88US=> NXe0R5lPW0GQR1XS
A375 MoriS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHLZTlNKSzVyPUGuPFk4OTRizszN M3fRVHNCVkeHUh?=
LCLC-97TM1 MoDUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXnJR|UxRTFwOUKyOVYh|ryP MX7TRW5ITVJ?
RXF393 NFHVe3JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MULJR|UxRTFwOUe4PFch|ryP NVv1NFFEW0GQR1XS
HCC70 NWr4cnRyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVLnWZlrUUN3ME2yMlAzPDJ4IN88US=> MYDTRW5ITVJ?
EM-2 M4W4c2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXnacmszUUN3ME2yMlA4OTl6IN88US=> M17Q[HNCVkeHUh?=
MZ2-MEL MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoTnTWM2OD1{LkGxNVI4KM7:TR?= NHzo[3lUSU6JRWK=
HN M37yOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUHJR|UxRTJwMU[yO|gh|ryP NYDN[W5uW0GQR1XS
A2058 NYjOXGZjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn\VTWM2OD1{LkG5Nlc6KM7:TR?= M1;FUnNCVkeHUh?=
NB7 MkSzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4TI[2lEPTB;Mj6zOFA5PiEQvF2= MkjrV2FPT0WU
DOK M{LNcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWH5b|JDUUN3ME2yMlM2Pzd|IN88US=> NWDH[oVyW0GQR1XS
CAL-27 NXTBNpZCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXPJR|UxRTJwM{myN|Yh|ryP MYnTRW5ITVJ?
BB65-RCC M2rTSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVfNTnViUUN3ME2yMlQxPjd2IN88US=> MWfTRW5ITVJ?
RD MnLCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M375ZWlEPTB;Mj60OFczOyEQvF2= MWHTRW5ITVJ?
KNS-62 NWfUe21NT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYrJR|UxRTJwNUGxOlQh|ryP NX[2S5lnW0GQR1XS
EW-13 Ml\0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NED2emhKSzVyPUKuOVY{OzlizszN MlPuV2FPT0WU
DB MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoTKTWM2OD1{LkW4O|g5KM7:TR?= MUXTRW5ITVJ?
HCC2218 NGTw[5lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF71[ZdKSzVyPUKuOlQ4PzhizszN MYfTRW5ITVJ?
L-363 NYO0R25TT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV:zd3FPUUN3ME2yMlc1OzdizszN MoXsV2FPT0WU
CHL-1 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnPQTWM2OD1{LkiwO|g2KM7:TR?= MXnTRW5ITVJ?
BFTC-905 NUSxfINJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn;oTWM2OD1{LkiyOVMh|ryP NELpfZFUSU6JRWK=
HCE-T MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3\hd2lEPTB;Mj64N|I3PCEQvF2= Mo\0V2FPT0WU
COLO-792 M1\nTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYfUfXM{UUN3ME2yMlg1ODJ5IN88US=> NWf2XoZsW0GQR1XS
LB2241-RCC NFKzU2JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUXJR|UxRTJwOEW4PVMh|ryP MlX3V2FPT0WU
CAL-39 MonkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIXZdFhKSzVyPUKuPFk6QTlizszN M{XYOXNCVkeHUh?=
T-24 MmT4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mnf2TWM2OD1{LkmxNVEzKM7:TR?= M1TCc3NCVkeHUh?=
NCI-H727 Mmq3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1nxNWlEPTB;Mj65NVc6PiEQvF2= MULTRW5ITVJ?
Ca9-22 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn3BTWM2OD1{Lkm3NlU2KM7:TR?= MYnTRW5ITVJ?
MIA-PaCa-2 NEX3bVJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWTJR|UxRTNwMEC3PFEh|ryP M4\5SnNCVkeHUh?=
HT-1080 NFiwXnpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1nRb2lEPTB;Mz6wNVk6PyEQvF2= MYPTRW5ITVJ?
D-423MG Ml;yS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2Ltd2lEPTB;Mz6wO|c2OyEQvF2= MVXTRW5ITVJ?
LAMA-84 NVvHdlZNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3TMPWlEPTB;Mz6xN|U5KM7:TR?= MkT0V2FPT0WU
SW780 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoHZTWM2OD1|LkG0NlI6KM7:TR?= NEPwfopUSU6JRWK=
KU-19-19 NIm3NXFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV;4Tm9mUUN3ME2zMlE4ODN2IN88US=> MUHTRW5ITVJ?
COLO-741 Mme3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mlz0TWM2OD1|LkG4Olc{KM7:TR?= MljNV2FPT0WU
HSC-3 Ml73S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXPJR|UxRTNwMkOxOVEh|ryP NUXBXnVHW0GQR1XS
SN12C NIH3PFdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2PBOGlEPTB;Mz6yOFcxOSEQvF2= Mlq2V2FPT0WU
786-0 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV2ySmluUUN3ME2zMlI4OjR|IN88US=> NHnkWoRUSU6JRWK=
GAK M2\BZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYDJR|UxRTNwM{K1OlEh|ryP NFXoUHBUSU6JRWK=
PANC-03-27 M3vZ[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV24cYE3UUN3ME2zMlM2ODR3IN88US=> M4q2dHNCVkeHUh?=
CTB-1 M1Lsb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkPZTWM2OD1|LkS3NFQ4KM7:TR?= NYjXNW9sW0GQR1XS
A427 MnnLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVzieZlUUUN3ME2zMlU6PTV4IN88US=> NIO0OYFUSU6JRWK=
EGI-1 M17ET2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVvJR|UxRTNwNkC1PFMh|ryP NXfJSpBQW0GQR1XS
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SF539 NYntO5pnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1LEPWlEPTB;MkCuOVE4OiEQvF2= MkCzV2FPT0WU
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PC-3 NVXZO4hbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1;HT2lEPTB;MkSuNFUzPiEQvF2= M1vaNHNCVkeHUh?=
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PANC-08-13 M3TY[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkfmTWM2OD1{NT64NVA{KM7:TR?= MW\TRW5ITVJ?
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TGBC24TKB M2XLPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFe2SG5KSzVyPUK2Mlc{OzFizszN MnrOV2FPT0WU
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C3A NHr3W2JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHLIfIVKSzVyPUK3Mlg1QTZizszN NVrSfoR[W0GQR1XS
MDA-MB-157 M4j1TGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV;JR|UxRTJ5Lki3OVMh|ryP NYXwWHF2W0GQR1XS
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NCI-N87 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUXJR|UxRTJ6LkWxNFUh|ryP NH\Q[YZUSU6JRWK=
RPMI-8226 NUjRW4luT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWHZ[pd5UUN3ME2yPU4yQDR|IN88US=> MorZV2FPT0WU
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UACC-893 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVvJR|UxRTJ7LkOxN|ch|ryP NYfhOGp6W0GQR1XS
C8166 NGPoVFJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2C4d2lEPTB;MkmuPVk6PiEQvF2= MUjTRW5ITVJ?
J82 NVL2VY5FT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV\LRm0zUUN3ME2zNE45OTR5IN88US=> NUXTWnZDW0GQR1XS
PFSK-1 MlSyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWXpXmxmUUN3ME2zNU4xPjV7IN88US=> MlvwV2FPT0WU
COLO-684 NV7HOGQ4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3;rR2lEPTB;M{GuOFM4PCEQvF2= MYrTRW5ITVJ?
CAL-72 NHj4TIpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkTLTWM2OD1|MT61O|I6KM7:TR?= Mn\HV2FPT0WU
SNB75 MlPvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFfu[ZlKSzVyPUOxMlg6PyEQvF2= NGjQd5ZUSU6JRWK=
MDA-MB-415 M3n1bGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkjoTWM2OD1|MT65O|YzKM7:TR?= NYXnU4pnW0GQR1XS
SiHa MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVvJR|UxRTN{LkS3NVEh|ryP NEK2SXdUSU6JRWK=
NCI-H1648 M1iwdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVfj[YF6UUN3ME2zNk46OzR3IN88US=> MXTTRW5ITVJ?
EFO-21 NFPqTZdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGPJTGFKSzVyPUOzMlAxPSEQvF2= M1vyS3NCVkeHUh?=
HCC38 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NG\jVHZKSzVyPUOzMlM5PDFizszN MYjTRW5ITVJ?
IA-LM NVP6UYU1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVnJR|UxRTN|Lke4PFkh|ryP M1;TeHNCVkeHUh?=
CTV-1 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnLqTWM2OD1|Mz65O|g3KM7:TR?= M3n4TXNCVkeHUh?=
NCI-H446 M1:5eGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1TYbWlEPTB;M{SuNlY5QSEQvF2= NY\m[oRKW0GQR1XS
IST-SL1 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlPUTWM2OD1|ND63OFA5KM7:TR?= MYnTRW5ITVJ?
EW-22 Mm\tS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUfYR|NiUUN3ME2zOE44PzV7IN88US=> M1\KfHNCVkeHUh?=
JEG-3 M{iwfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmDmTWM2OD1|Nj6xO|Y3KM7:TR?= M4LMc3NCVkeHUh?=
LU-65 M1Lpbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkHLTWM2OD1|Nj6yPVg2KM7:TR?= MnvFV2FPT0WU
NCI-H596 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUfJR|UxRTN4Lkm1PVEh|ryP NYW1cnpwW0GQR1XS
KNS-81-FD MoX1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NW\p[pM5UUN3ME2zO{4yPDVizszN NHuyXFlUSU6JRWK=
NCI-H1793 NXHDU4VUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlvMTWM2OD1|Nz63NFg3KM7:TR?= MV7TRW5ITVJ?
NCI-H460 M3\tSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGDLVVhKSzVyPUO4MlA5PzNizszN NFj4VIJUSU6JRWK=
MPP-89 M3zZbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlXBTWM2OD1|OT61PFg3KM7:TR?= M1f2b3NCVkeHUh?=
D-542MG NYHZUXFbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3zHVWlEPTB;M{muPFQ{PiEQvF2= NF\s[45USU6JRWK=
JAR NH7FXoxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mkf5TWM2OD12MD60O|A2KM7:TR?= MkDZV2FPT0WU
NCI-H209 MljFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3rSWGlEPTB;NECuOlc4KM7:TR?= NY\PVYJtW0GQR1XS
G-402 M1Ticmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnPqTWM2OD12MT6zPVk{KM7:TR?= NH\4PWFUSU6JRWK=
IST-MES1 MnrlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWHWUplIUUN3ME20Nk4yQTN3IN88US=> NEi2d2lUSU6JRWK=
Daoy NWP5O3hjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX3JR|UxRTR{LkW0O|Eh|ryP MWHTRW5ITVJ?
EW-11 MoTLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml3YTWM2OD12Mz6xNlEyKM7:TR?= MWLTRW5ITVJ?
Saos-2 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWjJR|UxRTR|LkG1N|ch|ryP NHPVN4FUSU6JRWK=
no-10 M3LKWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmryTWM2OD12Mz6xO|AzKM7:TR?= MoPPV2FPT0WU
HCC1395 M2n4[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1\vT2lEPTB;NEOuOFY1PCEQvF2= MkP2V2FPT0WU
HCE-4 NIi2U2FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHLufHFKSzVyPUSzMlc3PjRizszN MX;TRW5ITVJ?
EW-1 NFnPWXlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVi2eXpOUUN3ME20N{45ODR7IN88US=> M3;5bXNCVkeHUh?=
OCUB-M NH7sNm5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYntSGlNUUN3ME20OE4{PjN6IN88US=> MX;TRW5ITVJ?
IGR-1 MlPXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYO0Sos5UUN3ME20OE41OTF3IN88US=> NVqzT4x7W0GQR1XS
NCI-H1838 NYfGZ21nT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFzoUJhKSzVyPUS0MlQ{PDlizszN Ml\uV2FPT0WU
NCI-H2405 NWTNcJBkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2XrUGlEPTB;NESuOVM1KM7:TR?= MY\TRW5ITVJ?
GB-1 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXHJR|UxRTR2Lke0OlMh|ryP NV3tNWhwW0GQR1XS
MG-63 M1nuO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIHHc2lKSzVyPUS2MlA3QTZizszN NILMdXlUSU6JRWK=
KP-N-YN NIXUNJpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnXBTWM2OD12Nj60Olc6KM7:TR?= NIPj[2VUSU6JRWK=
no-11 NWrXTW9NT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXXJR|UxRTR5LkCyOFQh|ryP NEfLSYZUSU6JRWK=
SW948 M4Dodmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4TCWGlEPTB;NEeuN|M4PyEQvF2= MkO3V2FPT0WU
CAMA-1 NXj0UWhRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1WybGlEPTB;NEeuN|Q{QCEQvF2= MoXPV2FPT0WU
HCC1187 NF;rd5hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1jq[2lEPTB;NEeuOVEh|ryP NEPESnZUSU6JRWK=
D-392MG M2\3SGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXTJR|UxRTR5Lk[1NVYh|ryP MoDkV2FPT0WU
647-V NXP5eGtFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUDJR|UxRTR7LkO0NVQh|ryP M1fVcHNCVkeHUh?=

... Click to View More Cell Line Experimental Data

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]

+ Expand

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]

+ Expand
  • 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]

+ Expand
  • Animal Models: PTC cells in athymic mice
  • Formulation: Cremophor EL–95% ethanol (50:50) and dilutes with water
  • Dosages: 150 mg/kg
  • Administration: Orally twice daily
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 96 mg/mL (200.55 mM)
Ethanol 14 mg/mL (29.24 mM)
Water Insoluble
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

Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

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    C2
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* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
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    C8=C7/X C8: LOG(C8):
Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

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Molarity Calculator

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT00033384 Completed Breast Cancer|Colorectal Cancer|Lung Cancer|Pancreatic Cancer University of Alabama at Birmingham|National Cancer Institute (NCI) February 2002 Phase 2
NCT00033384 Completed Breast Cancer|Colorectal Cancer|Lung Cancer|Pancreatic Cancer University of Alabama at Birmingham|National Cancer Institute (NCI) February 2002 Phase 2
NCT00034827 Completed Colorectal Neoplasms|Breast Neoplasms|Carcinoma Non-Small-Cell Lung|Pancreatic Neoplasms Pfizer January 2002 Phase 2
NCT00034827 Completed Colorectal Neoplasms|Breast Neoplasms|Carcinoma Non-Small-Cell Lung|Pancreatic Neoplasms Pfizer January 2002 Phase 2

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