PD184352 (CI-1040)

Name: PD184352 (CI-1040)
Brand: Selleck Chemicals
SKU: S1020
Rating: 5 (88 reviews)

For research use only.

Catalog No.S1020

88 publications

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.

Selleck's PD184352 (CI-1040) has been cited by 88 publications

Cancer Cell, 2020, 37(1):85-103

PubMed: 31935375 ( click the link to review the publication )

Cancer Discov, 2016, 6(8):838-851

PubMed: 27179038 ( click the link to review the publication )

Cancer Cell, 2016, 12;30(3):499-500

PubMed: 27622337 ( click the link to review the publication )

Cancer Cell, 2016, 10.1016/j.ccell.2016.01.006

PubMed: 26859455 ( click the link to review the publication )

Cancer Discov, 2013, 3(9):1058-71

PubMed: 23744832 ( click the link to review the publication )

Cancer Discov, 2012, 2(10):934-47

PubMed: 22961667 ( click the link to review the publication )

Nat Chem Biol, 2012, 8(11):905-912

PubMed: 23023260 ( click the link to review the publication )

Science, 2011, 331(6019):912-6

PubMed: 21330545 ( click the link to review the publication )

Nat Genet, 2011, 44(2):133-9

PubMed: 22197931 ( click the link to review the publication )

Sci Signal, 2020, 28;13(629)

PubMed: 32345725 ( click the link to review the publication )

Cancers (Basel), 2020, 10;12(6):E1516

PubMed: 32531927 ( click the link to review the publication )

Cancers (Basel), 2020, 27;12(5)pii: E1087

PubMed: 32349331 ( click the link to review the publication )

Food Funct, 2020, 11(3):2714-2724

PubMed: 32163057 ( click the link to review the publication )

Nat Cell Biol, 2019, 21(6):778-790

PubMed: 31160710 ( click the link to review the publication )

Mol Cell, 2019, 74(5):1086-1102.e5

PubMed: 31101498 ( click the link to review the publication )

Cell Rep, 2019, 28(9):2358-2372

PubMed: 31461652 ( click the link to review the publication )

J Exp Clin Cancer Res, 2019, 38(1):322

PubMed: 31331377 ( click the link to review the publication )

Pigment Cell Melanoma Res, 2019, 32(2):280-291

PubMed: 30277012 ( click the link to review the publication )

Cell Death Dis, 2019, 10(12):871

PubMed: 31740667 ( click the link to review the publication )

Sci Rep, 2019, 9(1):13308

PubMed: 31527768 ( click the link to review the publication )

Oncotarget, 2019, 10(56):5755-5767

PubMed: 31645898 ( click the link to review the publication )

EMBO J, 2018, 37(1):19-38

PubMed: 29150432 ( click the link to review the publication )

PLoS Biol, 2018, 16(5):e2003619

PubMed: 29771909 ( click the link to review the publication )

J Cell Biol, 2018, 217(5):1701-1717

PubMed: 29545370 ( click the link to review the publication )
EMBO Rep, 2018, 19(2):320-336

PubMed: 29263201 ( click the link to review the publication )

Elife, 2018, 7

PubMed: 29595474 ( click the link to review the publication )

Elife, 2018, 10.7554/eLife.40167

PubMed: 30561326 ( click the link to review the publication )

Sci Rep, 2018, 8(1):18043

PubMed: 30575780 ( click the link to review the publication )

Nat Chem Biol, 2017, 13(1):38-45

PubMed: 27820799 ( click the link to review the publication )

Cancer Res, 2017, 77(5):1212-1226

PubMed: 28087600 ( click the link to review the publication )

J Hematol Oncol, 2017, 10(1):19

PubMed: 28100259 ( click the link to review the publication )

FASEB J, 2017, 31(5):1903-1915

PubMed: 28174207 ( click the link to review the publication )

Antiviral Res, 2017, 142:178-184

PubMed: 28377100 ( click the link to review the publication )

Biochem Pharmacol, 2017, 136:40-50

PubMed: 28404378 ( click the link to review the publication )

Methods Mol Biol, 2017, 1487:163-174

PubMed: 27924566 ( click the link to review the publication )

J Clin Invest, 2016, 1;126(4):1282-99

PubMed: 26974158 ( click the link to review the publication )

Elife, 2016, 10.7554/eLife.11414

PubMed: 26999821 ( click the link to review the publication )

Cell Mol Immunol, 2016, 13(5):658-68

PubMed: 26189368 ( click the link to review the publication )

Oncogene, 2016, 35(29):3854-3865

PubMed: 26657151 ( click the link to review the publication )

Drug Metab Dispos, 2016, 44(5):665-71

PubMed: 26953171 ( click the link to review the publication )

Oncol Lett, 2016, 11(1):99-104

PubMed: 26870175 ( click the link to review the publication )

Eur Rev Med Pharmacol Sci, 2016, 20(10):1961-8

PubMed: 27249593 ( click the link to review the publication )

Oncogene, 2015, 10.1038/onc.2015.12

PubMed: 25684139 ( click the link to review the publication )

Cell Death Dis, 2015, 6:e1711

PubMed: 25837487 ( click the link to review the publication )

Anim Reprod Sci, 2015, 161:47-57

PubMed: 26307658 ( click the link to review the publication )

J Exp Med, 2015, 212(6):883-92

PubMed: 25987726 ( click the link to review the publication )

Cytometry A, 2015, 10.1002/cyto.a.22628

PubMed: 25598437 ( click the link to review the publication )

eNeuro, 2015, 2(5)

PubMed: 26730399 ( click the link to review the publication )
J Clin Invest, 2014, 124(7):3016-31

PubMed: 24937430 ( click the link to review the publication )

EMBO Mol Med, 2014, 7(1):102-23

PubMed: 25550395 ( click the link to review the publication )

EMBO Mol Med, 2014, 6(6):821-34

PubMed: 24778454 ( click the link to review the publication )

Cancer Lett, 2014, 347(2):212-24

PubMed: 24576622 ( click the link to review the publication )

Cancer Lett, 2014, 348(1-2):38-49

PubMed: 24650799 ( click the link to review the publication )

Cell Death Dis, 2014, 5:e1445

PubMed: 25299770 ( click the link to review the publication )

FASEB J, 2014, 28(10):4551-62

PubMed: 25008089 ( click the link to review the publication )

Mol Cell Proteomics, 2014, 13(6):1429-38

PubMed: 24643969 ( click the link to review the publication )

Biochem J, 2014, 459(3):513-24

PubMed: 24527759 ( click the link to review the publication )

Virology, 2014, 468-470C:490-503

PubMed: 25261871 ( click the link to review the publication )

BMC Cancer, 2014, 14(1):240

PubMed: 24708867 ( click the link to review the publication )

PLoS One, 2014, 9(12):e114389

PubMed: 25486532 ( click the link to review the publication )

Blood, 2013, 121(19):3879-88, S1-8

PubMed: 23460614 ( click the link to review the publication )

J Clin Invest, 2013, 123(11):4786-98

PubMed: 24216509 ( click the link to review the publication )

Clin Cancer Res, 2013, 19(20):5749-57

PubMed: 23948972 ( click the link to review the publication )

Cancer Res, 2013, 73(20):6346-58

PubMed: 23966295 ( click the link to review the publication )

Dis Model Mech, 2013, 6(2):521-9

PubMed: 22996645 ( click the link to review the publication )

PLoS One, 2013, 8(10):e76505

PubMed: 24124570 ( click the link to review the publication )

PLoS One, 2013, 8(9):e73548

PubMed: 24019927 ( click the link to review the publication )

PLoS One, 2013, 8(7):e68378

PubMed: 23874604 ( click the link to review the publication )

J Natl Cancer Inst, 2012, 104(21):1673-9

PubMed: 22997239 ( click the link to review the publication )

Oncogene, 2012, 32(38):4480-9

PubMed: 23108403 ( click the link to review the publication )

Breast Cancer Res, 2012, 14(4):R111

PubMed: 22817771 ( click the link to review the publication )

Neoplasia, 2012, 14(4):283-96

PubMed: 22577344 ( click the link to review the publication )
J Biol Chem, 2012, 288(6):4174-93

PubMed: 23255592 ( click the link to review the publication )

J Biol Chem, 2012, 287(33):27863-75

PubMed: 22685289 ( click the link to review the publication )

Mol Endocrinol, 2012, 26(6):1056-73

PubMed: 22570334 ( click the link to review the publication )

Int J Parasitol, 2012, 40(5):555-67

PubMed: 19887070 ( click the link to review the publication )

J Cell Biochem, 2012, 113(1):360-71

PubMed: 21928324 ( click the link to review the publication )

J Biomol Screen, 2012, 17(6):813-21

PubMed: 22453235 ( click the link to review the publication )

J Exp Med, 2011, 208(9):1889-900

PubMed: 21825016 ( click the link to review the publication )

Proc Natl Acad Sci USA, 2011, 108(39):16392-7

PubMed: 21930937 ( click the link to review the publication )

Cell Death Dis, 2011, 2:e124

PubMed: 21368895 ( click the link to review the publication )

Neoplasia, 2011, 13(2):154-66

PubMed: 21403841 ( click the link to review the publication )

Dis Model Mech, 2011, 4(3):393-9

PubMed: 21263000 ( click the link to review the publication )

Antiviral Res, 2011, 92(2):195-203

PubMed: 21854809 ( click the link to review the publication )

Toxicol Sci, 2011, 123(2):542-9

PubMed: 21742783 ( click the link to review the publication )

Front Physiol, 2011, 2:71

PubMed: 22028692 ( click the link to review the publication )

Sci Signal, 2010, 3(149):ra84

PubMed: 21098728 ( click the link to review the publication )

Methods Mol Biol, 2010, 661:107-22

PubMed: 20811979 ( click the link to review the publication )

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	Activity Description	PMID
H9	NYnBZY5LT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	NYXSVnRsUUN3ME2wMlAzOjd4IN88US=>	NHLsdnJUSU6JRWK=
CHP-212	NEW1XoNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NVzzNVdIUUN3ME2wMlAzQDh3IN88US=>	NFjqfGNUSU6JRWK=
EoL-1-cell	NYPkWXNLT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	M{m1VmlEPTB;MD6wOFE2OiEQvF2=	NYntS4NqW0GQR1XS
DU-4475	M4XqTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	NH3CVnBKSzVyPUCuNFc2QTlizszN	MUHTRW5ITVJ?
MMAC-SF	MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	MXXJR\|UxRTBwMUC5O\|Qh\|ryP	MVnTRW5ITVJ?
AGS	MlPiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	NVzFb\|IzUUN3ME2wMlEyPzF\|IN88US=>	MkS1V2FPT0WU
M14	MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	NFrkTlRKSzVyPUCuNVU1PjhizszN	M4HxNXNCVkeHUh?=
CP50-MEL-B	M4\uUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	MnXjTWM2OD1yLkG3NlU1KM7:TR?=	MWfTRW5ITVJ?
C32	M1TGOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	NGDzPWRKSzVyPUCuNVkxPzJizszN	MlPLV2FPT0WU
KMOE-2	M3HSXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	M1XZVWlEPTB;MD6xPVc6PSEQvF2=	M{DQbnNCVkeHUh?=
A101D	NXLxUYl2T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	MX\JR\|UxRTBwMkG0JO69VQ>?	NFLtNHpUSU6JRWK=
KM12	MmnCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	NVO2S45KUUN3ME2wMlI1ODV5IN88US=>	MXfTRW5ITVJ?
HSC-4	MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	MoO0TWM2OD1yLkK0N\|k2KM7:TR?=	NUnmcHFPW0GQR1XS
NOMO-1	M4X4RWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	MYPJR\|UxRTBwMkW3OFIh\|ryP	MV;TRW5ITVJ?
MZ7-mel	MoHhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	NVrNXIhKUUN3ME2wMlI3OzRizszN	NEnxV4lUSU6JRWK=
ACN	NHLBXHJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	M{HOeGlEPTB;MD6yOlc{PyEQvF2=	MVzTRW5ITVJ?
MEL-HO	MoO4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	MlW5TWM2OD1yLkK3OlUzKM7:TR?=	M1HNd3NCVkeHUh?=
BHT-101	M13TTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	NFzY[\|VKSzVyPUCuNlg3ODZizszN	NGX4b\|FUSU6JRWK=
SK-MEL-28	MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	MofiTWM2OD1yLkOwOFA6KM7:TR?=	MUfTRW5ITVJ?
KG-1	MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	NYThT5pVUUN3ME2wMlMxPjZ6IN88US=>	MUjTRW5ITVJ?
COLO-679	M4\GXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	MXzJR\|UxRTBwM{K3NkDPxE1?	NF\UeHNUSU6JRWK=
SK-MEL-24	NFrHdJdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NEHwR\|ZKSzVyPUCuN\|I5OTNizszN	NIP1NlZUSU6JRWK=
G-361	MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	NVqzUlg3UUN3ME2wMlM3Pzl3IN88US=>	MoHYV2FPT0WU
KY821	NIT2[lJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	MYfJR\|UxRTBwM{e5NUDPxE1?	MkDEV2FPT0WU
KASUMI-1	NHz3VGNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	M1SwfGlEPTB;MD6zPVkh\|ryP	NYXBeZJ{W0GQR1XS
HL-60	NGLlWIhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	M{O5c2lEPTB;MD60NVExPyEQvF2=	MWrTRW5ITVJ?
K5	M334fWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	NV3GR3RvUUN3ME2wMlQ{OTF5IN88US=>	MnuzV2FPT0WU
KU812	MoXaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	M4P5fWlEPTB;MD60OVI6QSEQvF2=	MVjTRW5ITVJ?
SH-4	MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	NVzhdlJDUUN3ME2wMlQ3OjV4IN88US=>	MnGyV2FPT0WU
HTC-C3	MoX1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	MknoTWM2OD1yLkS2OVMyKM7:TR?=	MmHHV2FPT0WU
CP66-MEL	NHjofWNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	MlHXTWM2OD1yLkS4PFA6KM7:TR?=	NUnMUo9CW0GQR1XS
WM-115	MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	MlXiTWM2OD1yLkS5NlU4KM7:TR?=	MXHTRW5ITVJ?
A2780	MoLWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	M2LUXmlEPTB;MD60PVgzOyEQvF2=	MmH5V2FPT0WU
P12-ICHIKAWA	M3Xrcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	M1vvR2lEPTB;MD62NVIzOSEQvF2=	NITtUFJUSU6JRWK=
HMV-II	MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	M4LnSGlEPTB;MD62OFQ3PSEQvF2=	NIS4R3VUSU6JRWK=
HT-144	M3jrXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	MWXJR\|UxRTBwNkS2OVch\|ryP	M{XMZnNCVkeHUh?=
LB2518-MEL	NX\ScHVkT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	NFzmUJlKSzVyPUCuO\|E3OzJizszN	MX;TRW5ITVJ?
NCI-SNU-1	NFnEOXBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	Mn;OTWM2OD1yLke1OFM{KM7:TR?=	M3;ocHNCVkeHUh?=
C2BBe1	MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	M3iwWWlEPTB;MD64NVAzOyEQvF2=	NYDXd5hpW0GQR1XS
PSN1	MlnFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	M{LQdmlEPTB;MD65OlE6PiEQvF2=	NGj1OVZUSU6JRWK=
UACC-257	NITOWGxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	M4HYS2lEPTB;MD65OlQ4OyEQvF2=	NIe0[HRUSU6JRWK=
RVH-421	M2fIWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	MmLTTWM2OD1yLkm3NVgh\|ryP	M33VTHNCVkeHUh?=
GP5d	MoTlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	MkfzTWM2OD1yLkm4N\|A5KM7:TR?=	NH\DS41USU6JRWK=
TYK-nu	M3rycGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	NEnT[GlKSzVyPUGuNFMyPzJizszN	MmPRV2FPT0WU
SK-N-AS	MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	NUDyXm9oUUN3ME2xMlA4QTR5IN88US=>	NUHHdVVnW0GQR1XS
SW620	NGHUXnRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	M13GbmlEPTB;MT6xN\|U{PCEQvF2=	MYLTRW5ITVJ?
HuP-T4	M{ezfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	M{SxOWlEPTB;MT6xPFM2QSEQvF2=	Mn7zV2FPT0WU
A549	NWfjd41UT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	NEXD[HZKSzVyPUGuNVk2PzZizszN	M1LyVXNCVkeHUh?=
Mewo	MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	MVzJR\|UxRTFwMkCyO\|Yh\|ryP	NHjzdGlUSU6JRWK=
ONS-76	MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	NIOwWZBKSzVyPUGuNlIxPDlizszN	NHK3RoJUSU6JRWK=
SK-MEL-1	M1nDPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	NULNWWVmUUN3ME2xMlI{PDF7IN88US=>	NX3FN5JoW0GQR1XS
RCM-1	MkTjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	MUDJR\|UxRTFwMkSwOFch\|ryP	NV\KUoY1W0GQR1XS
H-EMC-SS	NIHzSWdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NGSwSWtKSzVyPUGuNlk3ODhizszN	MXLTRW5ITVJ?
NCI-H2291	NV7UU4hMT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	MkHtTWM2OD1zLkOyOVM3KM7:TR?=	NUKwXpc{W0GQR1XS
SW1463	Ml\iS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	NGTzRVRKSzVyPUGuN\|M4OjFizszN	NH;HSlRUSU6JRWK=
LS-411N	M2Xqcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	MojoTWM2OD1zLkSwOVE4KM7:TR?=	NEm0PGtUSU6JRWK=
BV-173	M2PXUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	Ml;mTWM2OD1zLkS0NFE2KM7:TR?=	NGrabldUSU6JRWK=
LS-513	M{XlTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	MUfJR\|UxRTFwNEWxPVIh\|ryP	MXXTRW5ITVJ?
LoVo	MlLSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	M4fEVmlEPTB;MT60OlM6QSEQvF2=	MX\TRW5ITVJ?
HO-1-N-1	NXHXU4xIT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	NEXRNFJKSzVyPUGuOVE3OzRizszN	M2fpN3NCVkeHUh?=
ML-2	M1\HOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	NHPSRo5KSzVyPUGuOVI5PjhizszN	M3XaRnNCVkeHUh?=
NCI-H1437	M1rZUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	MYTJR\|UxRTFwNUWyO\|Uh\|ryP	NGX0bnNUSU6JRWK=
SW1116	NV7sfYh5T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	NVSzTpBEUUN3ME2xMlU3Ozl6IN88US=>	NUHQc4pxW0GQR1XS
A4-Fuk	MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	NWHlSWx6UUN3ME2xMlU4ODR3IN88US=>	NGrXVWlUSU6JRWK=
HD-MY-Z	NWfQZ5lDT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	NV\FPJk5UUN3ME2xMlU4Ozd4IN88US=>	NX\hRZh[W0GQR1XS
SK-MEL-2	MmDPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	MVfJR\|UxRTFwNUe0OVkh\|ryP	NIPU[pdUSU6JRWK=
RT-112	M3ewZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	MXvJR\|UxRTFwNUi5OVIh\|ryP	MUTTRW5ITVJ?
COLO-829	NVnHNVhET3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	NVTxeY9rUUN3ME2xMlYzOjN{IN88US=>	MkKzV2FPT0WU
OVCAR-5	NF\2PVlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	Ml75TWM2OD1zLke3Olg4KM7:TR?=	M1\mfXNCVkeHUh?=
NB69	M2TncWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	M3fWW2lEPTB;MT63PFQ3QSEQvF2=	NUDxXpl7W0GQR1XS
NCI-H292	NX7zN3lwT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	NGLDPIRKSzVyPUGuPFY3QTlizszN	Ml3QV2FPT0WU
LOXIMVI	NXvZbnNqT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	Mn7LTWM2OD1zLki5OFI4KM7:TR?=	NVPDW4FoW0GQR1XS
BPH-1	MojrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	MUjJR\|UxRTFwOEm1PVEh\|ryP	M3TwVXNCVkeHUh?=
A375	MnLVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	MXTJR\|UxRTFwOEm3NVQh\|ryP	Mnf0V2FPT0WU
LCLC-97TM1	MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	MVXJR\|UxRTFwOUKyOVYh\|ryP	MV\TRW5ITVJ?
RXF393	NHLLRmFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	MVnJR\|UxRTFwOUe4PFch\|ryP	MnrCV2FPT0WU
HCC70	M3PIbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	NFfUfFVKSzVyPUKuNFI1OjZizszN	M4TsTnNCVkeHUh?=
EM-2	MkPDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	MmrrTWM2OD1{LkC3NVk5KM7:TR?=	MorQV2FPT0WU
MZ2-MEL	M4rsN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7	NYLCNoxwUUN3ME2yMlEyOTJ5IN88US=>	MU\TRW5ITVJ?
HN	MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	M2\XZmlEPTB;Mj6xOlI4QCEQvF2=	MnzjV2FPT0WU
A2058	MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	NGLIbJlKSzVyPUKuNVkzPzlizszN	NUXaV3MyW0GQR1XS
NB7	MojCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	MULJR\|UxRTJwM{SwPFYh\|ryP	MUDTRW5ITVJ?
DOK	NH3TcWdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	M1H4WGlEPTB;Mj6zOVc4OyEQvF2=	NV3KbHc5W0GQR1XS
CAL-27	MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	MWXJR\|UxRTJwM{myN\|Yh\|ryP	NIL3XJNUSU6JRWK=
BB65-RCC	MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	MlXOTWM2OD1{LkSwOlc1KM7:TR?=	MWXTRW5ITVJ?
RD	MnzES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	MWrJR\|UxRTJwNES3NlMh\|ryP	MXXTRW5ITVJ?
KNS-62	NVfxe5dtT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	NEPBWVBKSzVyPUKuOVEyPjRizszN	Ml\3V2FPT0WU
EW-13	MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	NIe2XZFKSzVyPUKuOVY{OzlizszN	M1r0fnNCVkeHUh?=
DB	NIntNXJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	MlnqTWM2OD1{LkW4O\|g5KM7:TR?=	NEHSNItUSU6JRWK=
HCC2218	MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	NUDCVGM1UUN3ME2yMlY1Pzd6IN88US=>	MXfTRW5ITVJ?
L-363	MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	M4fyNGlEPTB;Mj63OFM4KM7:TR?=	MULTRW5ITVJ?
CHL-1	MkXiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	Mkn0TWM2OD1{LkiwO\|g2KM7:TR?=	NFrv[XpUSU6JRWK=
BFTC-905	NYTiW4l6T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	MWDJR\|UxRTJwOEK1N{DPxE1?	MYHTRW5ITVJ?
HCE-T	MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	M{TURmlEPTB;Mj64N\|I3PCEQvF2=	NHu3UXVUSU6JRWK=
COLO-792	MkGzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	NEPySWJKSzVyPUKuPFQxOjdizszN	MVzTRW5ITVJ?
LB2241-RCC	NHzRbWlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	MVjJR\|UxRTJwOEW4PVMh\|ryP	Mn7EV2FPT0WU
CAL-39	NYP2cWF3T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	NHXzUnRKSzVyPUKuPFk6QTlizszN	M3jkXnNCVkeHUh?=
T-24	MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	M1vMSWlEPTB;Mj65NVEyOiEQvF2=	MlXmV2FPT0WU
NCI-H727	MnW1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	MXrJR\|UxRTJwOUG3PVYh\|ryP	MU\TRW5ITVJ?
Ca9-22	MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	NGHzWI1KSzVyPUKuPVczPTVizszN	MVjTRW5ITVJ?
MIA-PaCa-2	NWXW[JRrT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	NUjIUI94UUN3ME2zMlAxPzhzIN88US=>	NW[3VVFTW0GQR1XS
HT-1080	M1rxNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	MmDWTWM2OD1\|LkCxPVk4KM7:TR?=	MWPTRW5ITVJ?
D-423MG	NIjoN2ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NFL4d\|hKSzVyPUOuNFc4PTNizszN	NF31TlhUSU6JRWK=
LAMA-84	NHu5Vo9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	MkDyTWM2OD1\|LkGzOVgh\|ryP	M1:yPHNCVkeHUh?=
SW780	MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	MmrjTWM2OD1\|LkG0NlI6KM7:TR?=	NXHsXYVFW0GQR1XS
KU-19-19	NFTGT4JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NEfTOGNKSzVyPUOuNVcxOzRizszN	MmGzV2FPT0WU
COLO-741	MoXpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	NVn5NZZ3UUN3ME2zMlE5Pjd\|IN88US=>	MlzGV2FPT0WU
HSC-3	M1jhcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	MV;JR\|UxRTNwMkOxOVEh\|ryP	M1fHZXNCVkeHUh?=
SN12C	M1XTZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	MW\JR\|UxRTNwMkS3NFEh\|ryP	MmrsV2FPT0WU
786-0	NX\DcIlWT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	M3vEVWlEPTB;Mz6yO\|I1OyEQvF2=	MX7TRW5ITVJ?
GAK	MmDiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	NE\s[5BKSzVyPUOuN\|I2PjFizszN	M4O5XnNCVkeHUh?=
PANC-03-27	MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	MmX6TWM2OD1\|LkO1NFQ2KM7:TR?=	MmTVV2FPT0WU
CTB-1	M2PIOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	M2rzeWlEPTB;Mz60O\|A1PyEQvF2=	NInDVlRUSU6JRWK=
A427	MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	M{\TXWlEPTB;Mz61PVU2PiEQvF2=	MnG3V2FPT0WU
EGI-1	NInjcIxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	MkjOTWM2OD1\|Lk[wOVg{KM7:TR?=	NHHiO2hUSU6JRWK=
U-2-OS	NVTJfnJST3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	M1vkb2lEPTB;Mz62O\|I2PiEQvF2=	M2Ppd3NCVkeHUh?=
NCI-SNU-5	MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	MmfqTWM2OD1\|Lk[3O\|Mh\|ryP	NH7qOJBUSU6JRWK=
SK-LU-1	MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	Ml7UTWM2OD1\|Lk[4O\|k5KM7:TR?=	NETvdGtUSU6JRWK=
697	NWTLfWp{T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	M{\ZWmlEPTB;Mz62PVYxOyEQvF2=	MWfTRW5ITVJ?
HPAF-II	M3zBc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7	NUT1THdYUUN3ME2zMlc2PDlizszN	NU\1cZBOW0GQR1XS
NCI-H2087	NXXqPYQ6T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	MYXJR\|UxRTNwOES2O\|Ih\|ryP	NWTt[3p1W0GQR1XS
SK-MEL-3	M3KzWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	Mn6zTWM2OD1\|Lki1NVU1KM7:TR?=	NFy5SI1USU6JRWK=
CGTH-W-1	NHzOelhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NVnN[YtEUUN3ME2zMlg2PzJ3IN88US=>	NXPBV493W0GQR1XS
8505C	NE\weJNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	MXzJR\|UxRTNwOUCwO\|gh\|ryP	NFrHeWZUSU6JRWK=
GAMG	MnnaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	NVHqTpR7UUN3ME20MlAzOzd5IN88US=>	M3vrT3NCVkeHUh?=
SW626	NYe2WXE2T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	NYC0RXJVUUN3ME20MlA1PDhizszN	MYHTRW5ITVJ?
CAL-62	NEjHUZNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NWPScYJoUUN3ME20MlA4PDNizszN	MkHZV2FPT0WU
MHH-PREB-1	M{LTfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	MmnHTWM2OD12LkGyNVEyKM7:TR?=	NWnmPWpvW0GQR1XS
RPMI-7951	MmG4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	NITweJZKSzVyPUSuNlU2QDlizszN	NWXwXWhPW0GQR1XS
HOP-92	NGXIXYpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	M4rHeWlEPTB;ND6yOVY4KM7:TR?=	MkfuV2FPT0WU
MDA-MB-231	M2fKfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	Mln3TWM2OD12LkK5NlI{KM7:TR?=	NGLkcWVUSU6JRWK=
LAN-6	MmHES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	NY[5d\|E3UUN3ME20MlMyPjN5IN88US=>	NWHi[XhSW0GQR1XS
ALL-PO	NV[yZ\|k{T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	NHjCcVJKSzVyPUSuN\|YyPTZizszN	MluyV2FPT0WU
HH	NUXiTIhQT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	MonYTWM2OD12LkSxOVk4KM7:TR?=	M1z4WHNCVkeHUh?=
IGROV-1	M4ryOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	Mnq4TWM2OD12LkS1NVcyKM7:TR?=	MmHOV2FPT0WU
NCI-H358	MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	NWnrWWpGUUN3ME20MlQ2Ozh3IN88US=>	NXf1OIJNW0GQR1XS
NB5	NImyO5RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NV34clJjUUN3ME20MlYxOzZ7IN88US=>	NWS0b4Y5W0GQR1XS
NCI-H747	NICxfYVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	M4qybWlEPTB;ND62PFgxPyEQvF2=	M1XEV3NCVkeHUh?=
NH-12	Mn\xS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	NGHte2JKSzVyPUSuO\|E3OjVizszN	NXexPVBZW0GQR1XS
LB1047-RCC	M3n3OWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	MVfJR\|UxRTRwN{O4NVUh\|ryP	Mn7FV2FPT0WU
EFO-27	NUfZVHpJT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	NXmxSmR[UUN3ME20Mlc5PjZ5IN88US=>	NGr2cHdUSU6JRWK=
EPLC-272H	M1nk[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	MmfBTWM2OD12Lkm5OlY6KM7:TR?=	MYTTRW5ITVJ?
CAL-54	MlXQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	Mn7hTWM2OD13LkCyOlk2KM7:TR?=	MnLuV2FPT0WU
H4	MnLXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	M3O0[2lEPTB;NT6wOFI2PSEQvF2=	NGfHSphUSU6JRWK=
MOLT-13	NGqzXYFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	M3TGb2lEPTB;NT6wOlc4PiEQvF2=	NFSxUW1USU6JRWK=
CAL-33	NFjUc2lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NXHOO5BCUUN3ME21MlEzOzF5IN88US=>	NVrUVYtZW0GQR1XS
23132-87	NHzFS3BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NHj5UlhKSzVyPUWuNVY5PzJizszN	MWfTRW5ITVJ?
UM-UC-3	MmLMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	MXzJR\|UxRTVwMUiwOFch\|ryP	NXXCT2pzW0GQR1XS
HuH-7	NGnOdoZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	MmnhTWM2OD13LkK3NVQ4KM7:TR?=	MV\TRW5ITVJ?
BCPAP	M3G5N2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7	M1\0cGlEPTB;NT6zNlk3QSEQvF2=	NVj2VZBTW0GQR1XS
AsPC-1	NFzFbIlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	MULJR\|UxRTVwM{[3OlMh\|ryP	M{[2ZnNCVkeHUh?=
NCI-H1155	MofvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	MUjJR\|UxRTVwNECwOVEh\|ryP	MmHVV2FPT0WU
GT3TKB	M1XqeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	M{nk[GlEPTB;NT60OlU6QCEQvF2=	NVXTclFlW0GQR1XS
HCC2998	MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	Mn;0TWM2OD13LkS5NVA6KM7:TR?=	M4rEN3NCVkeHUh?=
NUGC-3	NU\CcmZ6T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	MnXiTWM2OD13LkS5N\|AzKM7:TR?=	NWD2[4s2W0GQR1XS
Hs-578-T	M3fTcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	NXrHXWJDUUN3ME21MlU{Pzl2IN88US=>	NVLROYo4W0GQR1XS
FADU	NGXORlJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	MULJR\|UxRTVwNUW3NlYh\|ryP	MkezV2FPT0WU
NBsusSR	NVS4UlFkT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	NV3GSJhDUUN3ME21MlU4OTV3IN88US=>	NXvsd4NyW0GQR1XS
ME-180	NUnuT4JNT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	NVG5SZRpUUN3ME21MlU5ODl{IN88US=>	NGe5dHVUSU6JRWK=
SW1710	M1zHRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	M4jUNWlEPTB;NT62NVY2PCEQvF2=	NF3ONXhUSU6JRWK=
HuP-T3	MofBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	NF[zcplKSzVyPUWuOlIxOjlizszN	NVrtfFI4W0GQR1XS
HOS	MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	MXzJR\|UxRTVwNkK5NlMh\|ryP	MXjTRW5ITVJ?
PA-1	M2jQNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	MX3JR\|UxRTVwNkSyOlUh\|ryP	MVzTRW5ITVJ?
LU-99A	MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	MYnJR\|UxRTVwNk[0OVEh\|ryP	NWDWe2d[W0GQR1XS
RS4-11	NXPpbnU5T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	NVnQd5FTUUN3ME21MlY3Pzd3IN88US=>	NXvaSXIzW0GQR1XS
TE-8	M{LScGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	MnzETWM2OD13Lk[4OVM4KM7:TR?=	MlvPV2FPT0WU
RERF-LC-MS	NFr1S3hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NFHmPVVKSzVyPUWuOlg5ODNizszN	M1TlOnNCVkeHUh?=
MEL-JUSO	MmDUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	MX3JR\|UxRTVwN{O3PEDPxE1?	NYjxZWlOW0GQR1XS
SK-MES-1	Moi2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	MV3JR\|UxRTVwOEO1Nlgh\|ryP	MX7TRW5ITVJ?
D-263MG	MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	MWnJR\|UxRTVwOEizOVEh\|ryP	NVO5R\|UzW0GQR1XS
NB10	NXfvO4V3T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	M3PnTmlEPTB;NT64PVQ3KM7:TR?=	M2\LPXNCVkeHUh?=
SK-HEP-1	NX36b3hqT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	MVPJR\|UxRTVwOUO0O\|Eh\|ryP	MX\TRW5ITVJ?
HT-29	MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	M4LpeWlEPTB;NT65PFEyQCEQvF2=	M4rGUHNCVkeHUh?=
KYSE-140	M2HP[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7	NV\5R4NnUUN3ME22MlAzOTh{IN88US=>	M332eHNCVkeHUh?=
NCI-H1666	MmHIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	MWrJR\|UxRTZwMEi0OlEh\|ryP	NX7tOnlXW0GQR1XS
NCI-H1304	Ml3jS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	NGXX[WVKSzVyPU[uNVk6PCEQvF2=	MWfTRW5ITVJ?
RPMI-8866	M{fWUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	NV\yZmxVUUN3ME22MlIyOzF\|IN88US=>	NHP4O\|ZUSU6JRWK=
MV-4-11	NF7F[JNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NWjsUJo2UUN3ME22MlI{OTl7IN88US=>	MXTTRW5ITVJ?
A431	Mo\wS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	NFr2b\|NKSzVyPU[uNlQzQTZizszN	M1j3enNCVkeHUh?=
PANC-10-05	M4PiOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	NW\yU4lnUUN3ME22MlI5OzZ\|IN88US=>	M{DoWnNCVkeHUh?=
TK10	NIDZenBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	M1HjRWlEPTB;Nj6zNlYxPCEQvF2=	NXPmTIk3W0GQR1XS
NCI-H1975	Mn\mS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	MoTYTWM2OD14LkS3NlE2KM7:TR?=	NUTuVmp1W0GQR1XS
A172	NXThWWpXT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	NGL6VpZKSzVyPU[uOFkyPzZizszN	MVPTRW5ITVJ?
D-566MG	NGDldWJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NWLMWIY4UUN3ME22MlU1OzB\|IN88US=>	MULTRW5ITVJ?
NCI-H2122	NIfVNYVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	MXnJR\|UxRTZwNkG1Nlgh\|ryP	MnjiV2FPT0WU
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BALL-1	MkTaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	Mn7qTWM2OD1zND60OlY2KM7:TR?=	NXTm[Xp5W0GQR1XS
LS-1034	MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	MnHHTWM2OD1zND62NVUzKM7:TR?=	NHrVS5RUSU6JRWK=
U-118-MG	M3rnd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7	NFHsN\|NKSzVyPUG0MlY{OSEQvF2=	NIfY[IdUSU6JRWK=
NCI-H630	M4DOOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	M3\nRmlEPTB;MUSuOlU3QCEQvF2=	MUDTRW5ITVJ?
OVCAR-8	MnXRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	MnfTTWM2OD1zND63NlAyKM7:TR?=	MkjBV2FPT0WU
NCI-H2347	MkXBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	M2\JfWlEPTB;MUSuPFI{KM7:TR?=	NV\DXVFoW0GQR1XS
BT-549	NX73d45wT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	Ml\QTWM2OD1zND64Nlg1KM7:TR?=	NEXadmpUSU6JRWK=
LB831-BLC	MkDWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	NHraUXpKSzVyPUG0Mlg6OzRizszN	MYPTRW5ITVJ?
NCI-H661	NFT3S4JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NWq1OHVoUUN3ME2xOE46PTlizszN	M{P2[HNCVkeHUh?=
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OVCAR-4	MoDVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	M2TTPWlEPTB;MUWuNVQzPCEQvF2=	MWjTRW5ITVJ?
OE33	NITtWWdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NWHYTVZ4UUN3ME2xOU4yPzFzIN88US=>	MUPTRW5ITVJ?
EC-GI-10	NF3J[W5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	MVfJR\|UxRTF3LkKzOVch\|ryP	NIK2RZFUSU6JRWK=
AM-38	M1jmcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	MYTJR\|UxRTF3LkK3NVch\|ryP	M4\UbXNCVkeHUh?=
NCI-H1563	Mlm5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	MV;JR\|UxRTF3LkO0PUDPxE1?	NXzxcppoW0GQR1XS
SCC-4	Mm\XS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	NHfVNVlKSzVyPUG1MlQyODNizszN	NEPLSWNUSU6JRWK=
Detroit562	MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	NEHtbnpKSzVyPUG1MlQ2PDdizszN	Mn3wV2FPT0WU
PC-14	NEHyPWxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NV64NWZtUUN3ME2xOU41QDZ4IN88US=>	NFnCWXBUSU6JRWK=
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CAL-85-1	M13CO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7	M4XXWmlEPTB;MUiuNVgxQSEQvF2=	MnLSV2FPT0WU
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RO82-W-1	M4HQ[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7	NILWdmtKSzVyPUG4MlgzQDhizszN	MY\TRW5ITVJ?
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NCI-H226	M4P1R2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7	NUPF[JBrUUN3ME2yNE41Ozl7IN88US=>	M3jLOXNCVkeHUh?=
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TE-6	M33rRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	MW\JR\|UxRTJyLkiwOlch\|ryP	NVvtTGM5W0GQR1XS
UMC-11	M2XZO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7	M2PaTWlEPTB;MkCuPVE3PCEQvF2=	M1THc3NCVkeHUh?=
Becker	Ml3hS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	M3nXR2lEPTB;MkGuNVEyQCEQvF2=	Ml;GV2FPT0WU
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ChaGo-K-1	MofMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	MUnJR\|UxRTJzLkO2Nlch\|ryP	NUHiRWJDW0GQR1XS
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NCI-H1755	MkD6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	MkXrTWM2OD1{MT62O\|QyKM7:TR?=	MmPzV2FPT0WU
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NCI-H441	NV;HRWd2T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	NHfFWIZKSzVyPUKyMlU3QDlizszN	MmfjV2FPT0WU
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LC-2-ad	MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	MmPTTWM2OD1{Mz62NVQ4KM7:TR?=	NHvjfXRUSU6JRWK=
VM-CUB-1	MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	NG\4NZFKSzVyPUKzMlc{PDFizszN	M3iycnNCVkeHUh?=
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MDA-MB-157	MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	NWPk[FluUUN3ME2yO{45PzV\|IN88US=>	MVzTRW5ITVJ?
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CAL-120	NYPHVJJ4T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	M2\HdWlEPTB;MkiuN\|k6QSEQvF2=	MV\TRW5ITVJ?
NCI-N87	NH7sTmpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NULFbYtpUUN3ME2yPE42OTB3IN88US=>	M3;DPHNCVkeHUh?=
RPMI-8226	NWL5WmVbT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	NV;5ZZNbUUN3ME2yPU4yQDR\|IN88US=>	NH7Jbm1USU6JRWK=
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CAL-72	NVriUZlrT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	NXT4[FRmUUN3ME2zNU42PzJ7IN88US=>	MXHTRW5ITVJ?
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MDA-MB-415	MnHUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	NWDvVVdyUUN3ME2zNU46PzZ{IN88US=>	NIPJPIFUSU6JRWK=
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NCI-H1648	NYLlVVNzT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	NULWT\|ZCUUN3ME2zNk46OzR3IN88US=>	M1\4THNCVkeHUh?=
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HCC38	NWLiPFdnT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	MVfJR\|UxRTN\|LkO4OFEh\|ryP	M2m1XXNCVkeHUh?=
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CTV-1	NEnG[I1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	MoPLTWM2OD1\|Mz65O\|g3KM7:TR?=	MWTTRW5ITVJ?
NCI-H446	MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	MmLnTWM2OD1\|ND6yOlg6KM7:TR?=	MWnTRW5ITVJ?
IST-SL1	MmLFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	MkPwTWM2OD1\|ND63OFA5KM7:TR?=	MYrTRW5ITVJ?
EW-22	M{fsO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7	NGr5Zo5KSzVyPUO0Mlc4PTlizszN	MXfTRW5ITVJ?
JEG-3	MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	M2LqSmlEPTB;M{[uNVc3PiEQvF2=	MVTTRW5ITVJ?
LU-65	NWHSeXlpT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	M1m1OmlEPTB;M{[uNlk5PSEQvF2=	MoftV2FPT0WU
NCI-H596	NWjL[plsT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	MYjJR\|UxRTN4Lkm1PVEh\|ryP	NFu4UlNUSU6JRWK=
KNS-81-FD	NUWzb2RlT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	MWLJR\|UxRTN5LkG0OUDPxE1?	MVPTRW5ITVJ?
NCI-H1793	NUnB[ndCT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	M1HnemlEPTB;M{euO\|A5PiEQvF2=	NV20SmtmW0GQR1XS
NCI-H460	NHLOXYhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NVKySHpEUUN3ME2zPE4xQDd\|IN88US=>	NGn5NW5USU6JRWK=
MPP-89	MoLNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	M4\vbWlEPTB;M{muOVg5PiEQvF2=	Mn;mV2FPT0WU
D-542MG	MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	NWjGd\|d1UUN3ME2zPU45PDN4IN88US=>	M2X0OHNCVkeHUh?=
JAR	MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	Mn7YTWM2OD12MD60O\|A2KM7:TR?=	NI\VbGtUSU6JRWK=
NCI-H209	NUjH[nV{T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	NXTvdG5FUUN3ME20NE43PzdizszN	MmLTV2FPT0WU
G-402	NIPPcHNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	M1vJcWlEPTB;NEGuN\|k6OyEQvF2=	M4TvR3NCVkeHUh?=
IST-MES1	M4nyRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	MnLSTWM2OD12Mj6xPVM2KM7:TR?=	Mki5V2FPT0WU
Daoy	M4TJZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7	MVnJR\|UxRTR{LkW0O\|Eh\|ryP	NE\aV2xUSU6JRWK=
EW-11	NGK1WFVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	Mn;5TWM2OD12Mz6xNlEyKM7:TR?=	M1TaXHNCVkeHUh?=
Saos-2	MljwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	NVqyeXlbUUN3ME20N{4yPTN5IN88US=>	NYTNXFRFW0GQR1XS
no-10	NEHvVIVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	MVjJR\|UxRTR\|LkG3NFIh\|ryP	NXLrRXgzW0GQR1XS
HCC1395	NHHoZmtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	M3rWZ2lEPTB;NEOuOFY1PCEQvF2=	NV64dGZ{W0GQR1XS
HCE-4	MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	M1nSSWlEPTB;NEOuO\|Y3PCEQvF2=	NWj2RmNtW0GQR1XS
EW-1	M2\jN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7	MlfsTWM2OD12Mz64NFQ6KM7:TR?=	MWnTRW5ITVJ?
OCUB-M	NFLwRZdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	MUnJR\|UxRTR2LkO2N\|gh\|ryP	MoLTV2FPT0WU
IGR-1	NYLRdZl2T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	MnS2TWM2OD12ND60NVE2KM7:TR?=	M37VV3NCVkeHUh?=
NCI-H1838	NFjzcFZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NYrYbVRDUUN3ME20OE41OzR7IN88US=>	MWPTRW5ITVJ?
NCI-H2405	NIOwd29Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	MVzJR\|UxRTR2LkWzOEDPxE1?	NYPsdohCW0GQR1XS
GB-1	NGLpb4xIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	MXfJR\|UxRTR2Lke0OlMh\|ryP	MWTTRW5ITVJ?
MG-63	Mkj6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	NWX5dHpJUUN3ME20Ok4xPjl4IN88US=>	MWXTRW5ITVJ?
KP-N-YN	MnuzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	NF;w[nRKSzVyPUS2MlQ3PzlizszN	Mkn4V2FPT0WU
no-11	M4HXW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7	NYPvbG1oUUN3ME20O{4xOjR2IN88US=>	MWTTRW5ITVJ?
SW948	NFTPbWhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NFTkSItKSzVyPUS3MlM{PzdizszN	M{nKe3NCVkeHUh?=
CAMA-1	NWnkc\|JLT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	NFrMR5BKSzVyPUS3MlM1OzhizszN	M3nWWXNCVkeHUh?=
HCC1187	NV;3eG5YT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	Mn35TWM2OD12Nz61NUDPxE1?	NUnI[296W0GQR1XS
D-392MG	M2PXNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	M2XQbmlEPTB;NEeuOlUyPiEQvF2=	M4S1Z3NCVkeHUh?=
647-V	MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	NH3HN2ZKSzVyPUS5MlM1OTRizszN	MmXWV2FPT0WU

... Click to View More Cell Line Experimental Data

Assay

Methods	Test Index	PMID
Western blot	p-ERK1/2 / ERK1/2 ; PubMed: 21762482 BMC Neurosci 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 BMC Neurosci Effect of PD184352 on phosphorylation of ERK5 in sympathetic neurons.	21762482
Growth inhibition assay	Cell viability; PubMed: 29989268 Cancer Sci 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]	- Collapse 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]	- Collapse 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]	- Collapse Animal Models: PTC cells in athymic mice Dosages: 150 mg/kg Administration: Orally twice daily (Only for Reference)

References

- Collapse

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 Download PD184352 (CI-1040) SDF

Molecular Weight	478.67
Formula	C₁₇H₁₄ClF₂IN₂O₂
CAS No.	212631-79-3
Storage	3 years-20°C powder 2 years-80°C in solvent
Synonyms	N/A
Smiles	FC1=CC=C(C(=O)NOCC2CC2)C(=C1F)NC3=CC=C(I)C=C3Cl

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

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Step 2: Enter the in vivo formulation (Different batches have different solubility ratios, please contact Selleck to provide you with the correct ratio)

% DMSO+ % + % Tween 80+ % ddH₂O

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Calculation results:

Working concentration： mg/ml；

Method for preparing DMSO master liquid: ： mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL， Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation：Take DMSO master liquid, next addμL PEG300， mix and clarify, next addμL Tween 80，mix and clarify, next add μL ddH₂O，mix and clarify.

Note：1.Please make sure the liquid is clear before adding the next solvent.
2.Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.

Bio Calculators

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The Serial Dilution Calculator Equation

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Computed Result

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Molecular Weight Calculator

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

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

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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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MEK Signaling Pathway Map

MEK Inhibitors with Unique Features

Selective MEK Inhibitor

Selumetinib (AZD6244) : MEK1-selective, IC50=14 nM.
Most Potent MEK Inhibitor

PD0325901 : MEK, IC50=0.33 nM,
FDA-approved MEK Inhibitor

Trametinib (GSK1120212) : Approved by FDA for BRAF V600E mutated metastatic melanoma.
Newest MEK Inhibitor

Binimetinib (MEK162, ARRY-162, ARRY-438162) : Potent inhibitor of MEK1/2 with IC50 of 12 nM.

Related MEK Products

Cobimetinib (GDC-0973) ^New

Cobimetinib (GDC-0973, RG7420) is a potent and highly selective MEK1 inhibitor with IC50 of 4.2 nM, showing more than 100-fold selectively for MEK1 over MEK2 and showed no significant inhibition when tested against a panel of more than 100 of serine-threonine and tyrosine kinases. Cobimetinib induces apoptosis. Phase 3.
BI-847325 ^New

BI-847325 is an orally bioavailable, and selective dual MEK/Aurora kinase inhibitor with IC50 of 3 nM, 25 nM, 15 nM, 25 nM, and 4 nM for Xenopus laevis Aurora B, human Aurora A and Aurora C, as well as human MEK1 and MEK2, respectively. Phase 1.
GDC-0623 ^New

GDC-0623 is a potent and ATP-uncompetitive MEK1 inhibitor with K_i of 0.13 nM. Phase 1.
Trametinib (GSK1120212)

Trametinib (GSK1120212) is a highly specific and potent MEK1/2 inhibitor with IC50 of 0.92 nM/1.8 nM in cell-free assays, no inhibition of the kinase activities of c-Raf, B-Raf, ERK1/2. Trametinib activates autophagy and induces apoptosis.

Features:More potent than PD0325901 or AZD6244.
PD0325901(Mirdametinib)

PD0325901 is a selective and non ATP-competitive MEK inhibitor with IC50 of 0.33 nM in cell-free assays, roughly 500-fold more potent than CI-1040 on phosphorylation of ERK1 and ERK2. Phase 2.
Selumetinib (AZD6244)

Selumetinib (AZD6244) is a potent, highly selective MEK inhibitor with IC50 of 14 nM for MEK1 and Kd value of 530 nM for MEK2. It also inhibits ERK1/2 phosphorylation with IC50 of 10 nM, no inhibition to p38α, MKK6, EGFR, ErbB2, ERK2, B-Raf, etc. Selumetinib suppresses cell proliferation, migration and trigger apoptosis. Phase 3.

Features:First MEK inhibitor being tested in Phase II clinical trials.
U0126-EtOH

U0126-EtOH is a highly selective inhibitor of MEK1/2 with IC50 of 0.07 μM/0.06 μM in cell-free assays, 100-fold higher affinity for ΔN3-S218E/S222D MEK than PD98059. U0126 inhibits autophagy and mitophagy with antiviral activity.

Features:A chemically synthesized and highly selective inhibitor of both MEK1 and MEK2.
PD98059

PD98059 is a non-ATP competitive MEK inhibitor with IC50 of 2 μM in a cell-free assay, specifically inhibits MEK-1-mediated activation of MAPK; does not directly inhibit ERK1 or ERK2. PD98059 is a ligand for the aryl hydrocarbon receptor (AHR) and functions as an AHR antagonist.

Features:Does not inhibit c-Raf phosphorylated MEK1.
Binimetinib (MEK162)

Binimetinib (MEK162, ARRY-162, ARRY-438162) is a potent inhibitor of MEK1/2 with IC50 of 12 nM in a cell-free assay. Binimetinib induces G1 cell cycle arrest and apoptosis in human NSCLC cell lines and induces autophagy. Phase 3.
Refametinib (RDEA119)

Refametinib (RDEA119, Bay 86-9766) is a potent, ATP non-competitive and highly selective inhibitor of MEK1 and MEK2 with IC50 of 19 nM and 47 nM, respectively.

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PD184352 (CI-1040)