Selumetinib (AZD6244)

Name: Selumetinib (AZD6244)
Brand: Selleck Chemicals
SKU: S1008
Rating: 5 (557 reviews)

For research use only.

Catalog No.S1008 Synonyms: ARRY-142886

557 publications

Selumetinib (AZD6244) Chemical Structure

CAS No. 606143-52-6

Selumetinib (AZD6244, ARRY-142886) 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.

Selleck's Selumetinib (AZD6244) has been cited by 557 publications

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Nature, 2016, 10.1038/nature19347

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Nat Med, 2015, 21(9):1038-47

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Cell Signal, 2021, S0898-6568(21)00123-6

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Gastroenterology, 2019, 157(3):823-837

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Stem Cell Reports, 2019,

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Cancers (Basel), 2019, 11(11)

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PLoS Pathog, 2019,

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Cells, 2019, 8(12)

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Molecules, 2019, 24(3)

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Oncotarget, 2019, 10(14):1440-1457

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Sci Transl Med, 2018, 10(450)

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Nat Commun, 2018, 9(1):579

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PLoS Biol, 2018,

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Genome Med, 2018, 10(1):90

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

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Clin Cancer Res, 2013, 19(9):2584-91

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Clin Cancer Res, 2013, 19(1):118-27

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Proc Natl Acad Sci USA, 2013, 10.1038/onc.2013.389

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Cancer Res, 2013, 73(23):7101-10

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

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Mol Syst Biol, 2013,

PubMed: 23752269 ( click the link to review the publication )

Cell Rep, 2013, 4(6):1090-9

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Oncogene, 2013, 33(33):4236-41

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Sci Signal, 2013, 6(271):ra25

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Sci Signal, 2013, 5(206):ra3

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Sci Signal, 2013,

PubMed: 23532334 ( click the link to review the publication )

Pigment Cell Melanoma Res, 2013, 26(4):518-26

PubMed: 23582185 ( click the link to review the publication )

Pigment Cell Melanoma Res, 2013, 26(4):509-17

PubMed: 23490205 ( click the link to review the publication )

J Neurosci, 2013, 33(10):4280-94

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Exp Mol Med, 2013, 45:e64

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Cancer Discov, 2013, 3(4):444-57

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Mol Cancer Ther, 2013, 12(6):1131-9

PubMed: 23515613 ( click the link to review the publication )

J Mol Cell Cardiol, 2013, 59:139-47

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Carcinogenesis, 2013, 34(3):638-46

PubMed: 23172668 ( click the link to review the publication )

Cancer Sci, 2013, 104(7):896-903

PubMed: 23578175 ( click the link to review the publication )

Skelet Muscle, 2013, 3(1):17

PubMed: 23815988 ( click the link to review the publication )

Mol Cell Biol, 2013, 33(20):4051-67

PubMed: 23959801 ( click the link to review the publication )

Exp Cell Res, 2013, 319(12):1732-43

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Cell Cycle, 2013, 12(13):2073-83

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Oncol Rep, 2013, 29(2):812-8

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PLoS One, 2013, 8(10):e77243

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PLoS One, 2013, 8(7):e68817

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J Surg Res, 2013, 184(2):898-906

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Oncotarget, 2013, 4(9):1496-506

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University of Southampton, 2013, University of Southampton

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Nature, 2013, 504(7478):138-42

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Cancer Res, 2013, 73(15):4840-51

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J Thorac Oncol, 2012, 7(2):272-80

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Cell Death Differ, 2012, 19(12):2029-39

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Oncogene, 2012, 31(27):3277-86

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Cancer Lett, 2012, 316(1):77-84

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Sci Signal, 2012, 5(224):rs4

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Cardiovasc Res, 2012, 93(2):311-9

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Carcinogenesis, 2012, 33(5):956-61

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Purity & Quality Control

Choose Selective MEK Inhibitors

Biological Activity

Description

Features

First MEK inhibitor being tested in Phase II clinical trials.

Targets

MEK1 ^[1] (Cell-free assay)	MEK1 ^[13] (Cell-free assay)	MEK2 ^[13] (Cell-free assay)
14 nM	99 nM(Kd)	530 nM(Kd)

In vitro

AZD6244 is not competitive with ATP and inactivates the ERK1/2 phosphorylation with IC50 concentrations below 40 nM. AZD6244 also inhibits the growth of primary HCC cells through inhibition of ERK1/2 and p90^RSK phosphorylation, accompanied with elevation of the cleavage of caspase-3 and caspase-7, and cleaved poly(ADP)ribose polymerase. AZD6244 has little effects on the p38, c-Jun-NH₂-kinase, phosphatidylinositol 3-kinase, and MEK5/ERK5 pathways. ^[1] AZD6244 is sensitive to Raf mutations in breast cancer cell lines and Ras mutations in NSCLC cell lines. ^[2]

Cell Data

Cell Lines	Assay Type	Incubation Time	Activity Description	PMID
CHP-212	M{DUbGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7		MnPVTY5pcWKrdHnvckBw\iCqdX3hckBEUFBvMkGyJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUCgQUAxNjByM{G1N{DPxE1w	NILNNVg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyPjF2N{CxM{c,W0GQR1XSQE9iRg>?
H9	NWLSSHlFT3Kxd4ToJIlvcGmkaYTpc44h[XO\|YYm=		MWTJcohq[mm2aX;uJI9nKGi3bXHuJGg6KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVAhRSByLkCyNlg5KM7:TT6=	NXLBUnZORGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTZzNEewNU8oRlODTlfFVlww[T5?
HL-60	MkPsS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl?		MkfrTY5pcWKrdHnvckBw\iCqdX3hckBJVC14MDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG\|c3H5MEBKSzVyIE2gNE4xOjR3OTFOwG0v	MV68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxOlE1PzBzLze+V2FPT0WUPD;hQi=>
NOMO-1	MV;Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>?		M1r3cWlvcGmkaYTpc44hd2ZiaIXtZY4hVk:PTz2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUCgQUAxNjB\|MUm3JO69VS5?	M2j1eFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFE3OTR5MEGvK\|5USU6JRWK8M4E,
DU-4475	NXnKRo1jT3Kxd4ToJIlvcGmkaYTpc44h[XO\|YYm=		NHq2enNKdmirYnn0bY9vKG:oIHj1cYFvKESXLUS0O\|Uh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NEA:KDBwMEOzOlch\|ryPLh?=	NIjIeZc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyPjF2N{CxM{c,W0GQR1XSQE9iRg>?
M14	NVv1VGtHT3Kxd4ToJIlvcGmkaYTpc44h[XO\|YYm=		MV;Jcohq[mm2aX;uJI9nKGi3bXHuJG0yPCClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR\|UxKD1iMD6wN\|Y5QSEQvF2u	MnjrQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVYyPDdyMT:nQnNCVkeHUkyvZV4>
HT-144	NHHvbFlIem:5dHigbY5pcWKrdHnvckBie3OjeR?=		M4LPdWlvcGmkaYTpc44hd2ZiaIXtZY4hUFRvMUS0JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUCgQUAxNjB6OUC1JO69VS5?	NIHidVY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyPjF2N{CxM{c,W0GQR1XSQE9iRg>?
SK-N-AS	MXnHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>?		NGnCNIhKdmirYnn0bY9vKG:oIHj1cYFvKFONLV6tRXMh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NEA:KDBwMEmyPFMh\|ryPLh?=	M4O2WVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFE3OTR5MEGvK\|5USU6JRWK8M4E,
LB2518-MEL	NHnWfXNIem:5dHigbY5pcWKrdHnvckBie3OjeR?=		M3;VVGlvcGmkaYTpc44hd2ZiaIXtZY4hVEJ{NUG4MW1GVCClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR\|UxKD1iMD6wPVM5OiEQvF2u	NHjXVW09[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyPjF2N{CxM{c,W0GQR1XSQE9iRg>?
C32	MorhS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl?		MlHzTY5pcWKrdHnvckBw\iCqdX3hckBEOzJiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OCB;IECuNFk5OjNizszNMi=>	MV28ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxOlE1PzBzLze+V2FPT0WUPD;hQi=>
BHT-101	NVflfJRzT3Kxd4ToJIlvcGmkaYTpc44h[XO\|YYm=		MWnJcohq[mm2aX;uJI9nKGi3bXHuJGJJXC1zMEGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3MDC9JFAvOTB4OUOg{txONg>?	NInmO5o9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyPjF2N{CxM{c,W0GQR1XSQE9iRg>?
KY821	NX\ENXJrT3Kxd4ToJIlvcGmkaYTpc44h[XO\|YYm=		MVLJcohq[mm2aX;uJI9nKGi3bXHuJGt[QDJzIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO\|YYmsJGlEPTBiPTCwMlExPzF6IN88UU4>	MojwQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVYyPDdyMT:nQnNCVkeHUkyvZV4>
CP50-MEL-B	MW\Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>?		MVHJcohq[mm2aX;uJI9nKGi3bXHuJGNRPTBvTVXMMWIh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NEA:KDBwMUK3PVQh\|ryPLh?=	NYnFeWY2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTZzNEewNU8oRlODTlfFVlww[T5?
MEL-HO	NYC0b4RPT3Kxd4ToJIlvcGmkaYTpc44h[XO\|YYm=		M2HacmlvcGmkaYTpc44hd2ZiaIXtZY4hVUWOLVjPJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUCgQUAxNjF\|OEi0JO69VS5?	MUG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxOlE1PzBzLze+V2FPT0WUPD;hQi=>
EoL-1-cell	MYjHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>?		NG\BVmVKdmirYnn0bY9vKG:oIHj1cYFvKEWxTD2xMYNmdGxiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OCB;IECuNVQ1PzZizszNMi=>	NGPVXIw9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyPjF2N{CxM{c,W0GQR1XSQE9iRg>?
DOK	Mk\wS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl?		Mn;0TY5pcWKrdHnvckBw\iCqdX3hckBFV0tiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OCB;IECuNVQ4ODhizszNMi=>	MYC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxOlE1PzBzLze+V2FPT0WUPD;hQi=>
SH-4	NHnpO2JIem:5dHigbY5pcWKrdHnvckBie3OjeR?=		NXr0VFJOUW6qaXLpeIlwdiCxZjDoeY1idiCVSD20JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUCgQUAxNjF4NkS4JO69VS5?	MWG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxOlE1PzBzLze+V2FPT0WUPD;hQi=>
BPH-1	M3rO[mdzd3e2aDDpcohq[mm2aX;uJIF{e2G7		MnvkTY5pcWKrdHnvckBw\iCqdX3hckBDWEhvMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG\|c3H5MEBKSzVyIE2gNE4yQDJ\|MTFOwG0v	MoDKQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVYyPDdyMT:nQnNCVkeHUkyvZV4>
HuP-T4	NHn3UYNIem:5dHigbY5pcWKrdHnvckBie3OjeR?=		MnexTY5pcWKrdHnvckBw\iCqdX3hckBJfVBvVESgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3MDC9JFAvOTl3M{Kg{txONg>?	MVK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxOlE1PzBzLze+V2FPT0WUPD;hQi=>
KU812	MXLHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>?		MXzJcohq[mm2aX;uJI9nKGi3bXHuJGtWQDF{IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO\|YYmsJGlEPTBiPTCwMlIyOTZ6IN88UU4>	NUjCW3JoRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTZzNEewNU8oRlODTlfFVlww[T5?
A549	Ml6wS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl?		Ml;vTY5pcWKrdHnvckBw\iCqdX3hckBCPTR7IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO\|YYmsJGlEPTBiPTCwMlIyPDF\|IN88UU4>	Mn;XQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVYyPDdyMT:nQnNCVkeHUkyvZV4>
HTC-C3	NYW0fmRpT3Kxd4ToJIlvcGmkaYTpc44h[XO\|YYm=		M3zYSWlvcGmkaYTpc44hd2ZiaIXtZY4hUFSFLVOzJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUCgQUAxNjJzNE[xJO69VS5?	M2TMNlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFE3OTR5MEGvK\|5USU6JRWK8M4E,
A101D	Ml3US5Jwf3SqIHnubIljcXSrb36gZZN{[Xl?		NWDTfpRtUW6qaXLpeIlwdiCxZjDoeY1idiCDMUCxSEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwJF0hOC5{NECzN{DPxE1w	MoHVQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVYyPDdyMT:nQnNCVkeHUkyvZV4>
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GCT	MWrHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>?		NEL0[pBKdmirYnn0bY9vKG:oIHj1cYFvKEeFVDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG\|c3H5MEBKSzVyIE2gOE4yODR2MjFOwG0v	MVO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxOlE1PzBzLze+V2FPT0WUPD;hQi=>
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PANC-03-27	NHnE[m5Iem:5dHigbY5pcWKrdHnvckBie3OjeR?=		MYDJcohq[mm2aX;uJI9nKGi3bXHuJHBCVkNvMEOtNlch[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NEA:KDRwNUO5Nlkh\|ryPLh?=	MnLkQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVYyPDdyMT:nQnNCVkeHUkyvZV4>
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EPLC-272H	Ml;jS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl?		M4LONmlvcGmkaYTpc44hd2ZiaIXtZY4hTVCOQz2yO\|JJKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVAhRSB2LkixOlk5KM7:TT6=	MUG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxOlE1PzBzLze+V2FPT0WUPD;hQi=>
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NCI-H526	M2S3PWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7		MWTJcohq[mm2aX;uJI9nKGi3bXHuJG5EUS2KNUK2JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUCgQUA{PC5yN{[g{txONg>?	M1XObFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFE3OTR5MEGvK\|5USU6JRWK8M4E,
RPMI-2650	NGP4UolIem:5dHigbY5pcWKrdHnvckBie3OjeR?=		M3[0NmlvcGmkaYTpc44hd2ZiaIXtZY4hWlCPST2yOlUxKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVAhRSB\|ND60N\|M1KM7:TT6=	MnzyQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVYyPDdyMT:nQnNCVkeHUkyvZV4>
KYSE-70	M1m1Xmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7		M3LucWlvcGmkaYTpc44hd2ZiaIXtZY4hU1mVRT23NEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwJF0hOzRwOESyOkDPxE1w	NXrSXFhSRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTZzNEewNU8oRlODTlfFVlww[T5?
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OVCAR-4	Ml60S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl?		NVO2bGs6UW6qaXLpeIlwdiCxZjDoeY1idiCRVlPBVk01KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVAhRSB\|Nz6yNVc3KM7:TT6=	Mn\uQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVYyPDdyMT:nQnNCVkeHUkyvZV4>
OVCAR-8	NX7Ie4dNT3Kxd4ToJIlvcGmkaYTpc44h[XO\|YYm=		NV\vWXVrUW6qaXLpeIlwdiCxZjDoeY1idiCRVlPBVk05KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVAhRSB\|Nz65PFI{KM7:TT6=	M3Lhc\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFE3OTR5MEGvK\|5USU6JRWK8M4E,
NCI-H1355	M2T6fGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7		MkDpTY5pcWKrdHnvckBw\iCqdX3hckBPS0lvSEGzOVUh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NEA:KDN6LkGwOVEh\|ryPLh?=	MXO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxOlE1PzBzLze+V2FPT0WUPD;hQi=>
COLO-680N	M4DGSWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7		MlHpTY5pcWKrdHnvckBw\iCqdX3hckBEV0yRLU[4NG4h[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NEA:KDN6LkK0Nlkh\|ryPLh?=	NGPCN4I9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyPjF2N{CxM{c,W0GQR1XSQE9iRg>?
NCI-H2122	NWXlSHRQT3Kxd4ToJIlvcGmkaYTpc44h[XO\|YYm=		M1fvfGlvcGmkaYTpc44hd2ZiaIXtZY4hVkOLLViyNVIzKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVAhRSB\|OT6zN\|Y{KM7:TT6=	NI\HTY89[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyPjF2N{CxM{c,W0GQR1XSQE9iRg>?
Saos-2	NUjYUZFMT3Kxd4ToJIlvcGmkaYTpc44h[XO\|YYm=		MYjJcohq[mm2aX;uJI9nKGi3bXHuJHNid3NvMjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG\|c3H5MEBKSzVyIE2gN\|kvPzB3MzFOwG0v	MlT0QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVYyPDdyMT:nQnNCVkeHUkyvZV4>
HCC2157	MXrHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>?		MV\Jcohq[mm2aX;uJI9nKGi3bXHuJGhESzJzNUegZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3MDC9JFQxNjd5M{Sg{txONg>?	NXfzVppzRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTZzNEewNU8oRlODTlfFVlww[T5?
VMRC-RCZ	NVfIcldbT3Kxd4ToJIlvcGmkaYTpc44h[XO\|YYm=		NE[zV4tKdmirYnn0bY9vKG:oIHj1cYFvKF[PUlOtVmNbKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVAhRSB2MT6yPVYzKM7:TT6=	NITVcXI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyPjF2N{CxM{c,W0GQR1XSQE9iRg>?
ETK-1	NYjkfHlqT3Kxd4ToJIlvcGmkaYTpc44h[XO\|YYm=		MXTJcohq[mm2aX;uJI9nKGi3bXHuJGVVUy1zIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO\|YYmsJGlEPTBiPTC0NU42PzVzIN88UU4>	M2fUeVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFE3OTR5MEGvK\|5USU6JRWK8M4E,
RCC10RGB	M4PoTWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7		NWLiSZdkUW6qaXLpeIlwdiCxZjDoeY1idiCUQ1OxNHJISiClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR\|UxKD1iNEKuNFE5KM7:TT6=	MnzKQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVYyPDdyMT:nQnNCVkeHUkyvZV4>
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A431	NFrnOmZIem:5dHigbY5pcWKrdHnvckBie3OjeR?=		MXPJcohq[mm2aX;uJI9nKGi3bXHuJGE1OzFiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OCB;IES1MlE5OzFizszNMi=>	NX;p[HY{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTZzNEewNU8oRlODTlfFVlww[T5?
HDLM-2	NFTUR2NIem:5dHigbY5pcWKrdHnvckBie3OjeR?=		MmHDTY5pcWKrdHnvckBw\iCqdX3hckBJTEyPLUKgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3MDC9JFQ2NjJ4MUeg{txONg>?	Mn[1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVYyPDdyMT:nQnNCVkeHUkyvZV4>
CHP-134	M1q0SWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7		MnTvTY5pcWKrdHnvckBw\iCqdX3hckBEUFBvMUO0JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUCgQUA1Pi5zN{e5JO69VS5?	MlnxQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVYyPDdyMT:nQnNCVkeHUkyvZV4>
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NCI-H1650	NHXicXNIem:5dHigbY5pcWKrdHnvckBie3OjeR?=		M33XT2lvcGmkaYTpc44hd2ZiaIXtZY4hVkOLLVixOlUxKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVAhRSB2Nj61NVA1KM7:TT6=	MnTnQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVYyPDdyMT:nQnNCVkeHUkyvZV4>
MHH-PREB-1	Mk\ZS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl?		NFLGfYhKdmirYnn0bY9vKG:oIHj1cYFvKE2KSD3QVmVDNTFiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OCB;IES2MlUzPjZizszNMi=>	NFrhSoI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyPjF2N{CxM{c,W0GQR1XSQE9iRg>?
SJRH30	NGDyfG5Iem:5dHigbY5pcWKrdHnvckBie3OjeR?=		MoOxTY5pcWKrdHnvckBw\iCqdX3hckBUUlKKM{CgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3MDC9JFQ3Njd5N{Wg{txONg>?	NGG0VGQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyPjF2N{CxM{c,W0GQR1XSQE9iRg>?
SF295	M4XndGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7		NX7YbpVjUW6qaXLpeIlwdiCxZjDoeY1idiCVRkK5OUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwJF0hPDhwNUG5JO69VS5?	NX7jPHlbRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTZzNEewNU8oRlODTlfFVlww[T5?
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A375	NVnTNJgyWHKxbHnm[ZJifGmxbjDhd5NigQ>?	MVO3NkBp	MkC2RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6\|dDDoeY1idiCDM{e1JINmdGy\|IHX4dJJme3OrbnegRnJCTiCYNkCwSUBufXSjboSgZYZ1\XJiN{KgbJJ{KGK7IFPlcIwhfGm2ZYKt[4xwKGG\|c3H5MEBKSzVyPUOxJI5ONg>?	MXS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzR5NEO4PEc,OjN2N{SzPFg9N2F-
A549	NVOzbHFSSW62aYDyc4xq\mW{YYTpeoUh[XO\|YYm=		NYfjU2I1SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDBOVQ6KGOnbHzzMEBKSzVyIE2gNU44PSEQvF2u	M1TScVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ\|NEe0N\|g5Lz5{M{S3OFM5QDxxYU6=
LoVo	M1vUWWFvfGmycn;sbYZmemG2aY\lJIF{e2G7		NG\XOYpCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFzvWo8h[2WubIOsJGlEPTBiPTCyMlg{KM7:TT6=	M1y0dVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ\|NEe0N\|g5Lz5{M{S3OFM5QDxxYU6=
HCT116	MVnBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>?		NXew[VZCSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDIR3QyOTZiY3XscJMh\XiycnXzd4lv\yCNUlHTJGcyO0RibYX0ZY51NCCLQ{WwJF0hOy5zIN88UU4>	MXy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzR5NEO4PEc,OjN2N{SzPFg9N2F-
HeLa-MaTu	NFLsXpdHfW6ldHnvckBie3OjeR?=		MWXJcohq[mm2aX;uJI9nKE2HS{GgbY4hcHWvYX6gTIVN[S2PYWT1JI1ifGOqZXSgdIFqeiClZXzsd{Bie3Onc4Pl[EBieyC{ZXT1Z5Rqd25iaX6gSXJMKHCqb4PwbI9zgWyjdHnvckwhUUN3MDC9JFAvODF2IN88UU4>	M3LFclxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4NkGxPVIxLz5{Nk[xNVkzODxxYU6=
HepG2	MojHRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl?		NYixUmJ3SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDI[ZBIOiClZXzsd{Bp[XKkb4LpcochVi2UYYOgcZV1[XSrb36sJGlEPTBiPTCwMlA{OiEQvF2u	M4e0OVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4NkGxPVIxLz5{Nk[xNVkzODxxYU6=
COLO205	MULBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>?		NUPaPI5nSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDDU2xQOjB3IHPlcIx{KGijcnLvdolv\yCEUlHGJI12fGG2aX;uMEBKSzVyIE2gNE4xPjlizszNMi=>	M1zxSVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4NkGxPVIxLz5{Nk[xNVkzODxxYU6=
A549	NH\j[3pCdnSrcILvcIln\XKjdHn2[UBie3OjeR?=		MoPYRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6\|dDDoeY1idiCDNUS5JINmdGy\|IHjhdoJwemmwZzDLMXJieyCvdYTheIlwdixiSVO1NEA:KDFwN{Wg{txONg>?	M1znOFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4NkGxPVIxLz5{Nk[xNVkzODxxYU6=
HCT116	NYLoNYpXSW62aYDyc4xq\mW{YYTpeoUh[XO\|YYm=		M2nnOmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSFPUNVE3KGOnbHzzJIhiemKxcnnu[{BMNVKjczDHNVNFKG23dHH0bY9vNCCLQ{WwJF0hOyEQvF2u	NXHCbFY6RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[2NVE6OjBpPkK2OlEyQTJyPD;hQi=>
HeLa-MaTu-ADR	MYPGeY5kfGmxbjDhd5NigQ>?		Ml;3TY5pcWKrdHnvckBw\iCPRVuxJIlvKGi3bXHuJGhmVGFvTXHUeU1CTFJibXH0Z4hm\CCyYXnyJINmdGy\|IHHzd4V{e2WmIHHzJJJm\HWldHnvckBqdiCHUlugdIhwe3Cqb4L5cIF1cW:wLDDJR\|UxKD1iMz63JO69VS5?	MXG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjZzMUmyNEc,OjZ4MUG5NlA9N2F-
SW480	NIfrelZCdnSrcILvcIln\XKjdHn2[UBie3OjeR?=	NV7qU5kyPzJiaILz	M1TLTWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iU2e0PFAh[2WubIOgZYZ1\XJiN{KgbJJ{KGK7IF3UWEBie3OjeTygTWM2OCB;IECuOFIzKM7:TT6=	M1P4UlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5NES4PVE5Lz5{N{S0PFkyQDxxYU6=
SW620	NG\kcYhCdnSrcILvcIln\XKjdHn2[UBie3OjeR?=	NEnzRnM4OiCqcoO=	NVHJOZBqSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDTW\|YzOCClZXzsd{Bp[XKkb4LpcochU1KDUzDHNVJXKG23dHHueEBi\nSncjC3NkBpenNiYomgR4VtdFSrdHXyMWdtdyCjc4PhfUwhUUN3MDC9JFAvODF3IN88UU4>	Mnm3QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjhyM{i5OFAoRjJ6MEO4PVQxRC:jPh?=
AsPC1	MY\BcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>?	MlfIO\|IhcHK\|	NEO4fIVCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFHzVGMyKGOnbHzzJIhiemKxcnnu[{BMWkGVIFexNmQhdXW2YX70JIFnfGW{IEeyJIhzeyCkeTDD[YxtXGm2ZYKtS4xwKGG\|c3H5MEBKSzVyIE2gNE4xPjR{IN88UU4>	M1fTWVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6MEO4PVQxLz5{OECzPFk1ODxxYU6=
BA/F3	NGjtOGdCdnSrcILvcIln\XKjdHn2[UBie3OjeR?=	MnnaO\|IhcHK\|	NYTJflB5SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBud3W\|ZTDCRU9HOyClZXzsd{Bp[XKkb4LpcochU1KDUzDHNVJFKG23dHHueEBi\nSncjC3NkBpenNiYomgR4VtdFSrdHXyMWdtdyCjc4PhfUwhUUN3MDC9JFAvOSEQvF2u	MX[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDB\|OEm0NEc,OjhyM{i5OFA9N2F-
SKCO1	MUjBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>?	MoWwO\|IhcHK\|	M1v5PWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iU1vDU\|Eh[2WubIOgbIFz[m:{aX7nJGtTSVNiR{GyWkBufXSjboSgZYZ1\XJiN{KgbJJ{KGK7IFPlcIxVcXSncj3HcI8h[XO\|YYmsJGlEPTBiPTCwMlEyPyEQvF2u	NXPoN\|R3RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkiwN\|g6PDBpPkK4NFM5QTRyPD;hQi=>
COLO205	NITW[FZCdnSrcILvcIln\XKjdHn2[UBie3OjeR?=	NEnlPIg4OiCqcoO=	NUf3Sog1SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDDU2xQOjB3IHPlcIx{KGijcnLvdolv\yCEUlHGJI12fGGwdD;3bYxlKHS7cHWgT3JCWy:5aXzkJJR6eGViUFnLN2NCKGGodHXyJFczKGi{czDifUBES0t6IHHzd4F6NCCLQ{WwJF0hOC5yNUmg{txONg>?	MYq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTNzN{G0PEc,Ojl\|MUexOFg9N2F-

... Click to View More Cell Line Experimental Data

Assay

Methods	Test Index	PMID
Western blot	p-ERK / ERK / β-catenin / E-cadherin / Vimentin / Fibronection; PubMed: 26384399 Mol Cancer Ther MDA-MB-231 and SUM149 cells were treated with selumetinib for 48 hours, and western blot analysis was performed, with β-actin used as a loading control. pS6(235/236) / pS6(240/244); PubMed: 26137449 Mol Cancer Ther Selumetinib (Sel) in combination with BEZ235 or ZSTK474 inhibits pS6 expression in BRAF-mutant melanoma cell lines that are highly sensitive (NZM3, NZM11, NZM20) or moderately sensitive (NZM6, NZM7, NZM12) to single agent selumetinib. Cells were treated with 500 nM of each compound as indicated for 1 or 24 h. Blots are representative images of two independent determinations. pVEGFR(Y1175) / VEGFR2 / pPDGFRβ(Y751) / pPDGFRβ / pAXL(Y702) / AXL / pMEK / MEK; PubMed: 22500798 Cell Dose-dependent RTK reprogramming in response to AZD6244. Dose-dependent induction of RTK expression and activity in 24h-treated SUM159 cells was determined by western blot. Bak / Bad / Bcl-xl / BimEL / BimL / BimS / PUMA / NOXA ; PubMed: 20885957 PLoS One Human lung cancer cell lines (Calu-6, H2347, and H3122) were treated with 3 µM AZD6244 for 4, 8, 24, 48, and 72 hours. Western blots of Bcl-2 family members after treatment with AZD6244.	26384399 26137449 22500798 20885957
Immunofluorescence	β-catenin; PubMed: 26384399 Mol Cancer Ther MDA-MB-231 and SUM149 cells were treated with selumetinib in a 3D culture for 48 hours. Immunofluorescence staining was done to detect β-catenin-FITC (fluorescein isothiocyanate), and nuclei were stained with DAPI. Images were taken under 60× magnification. FOXO3a; PubMed: 20885957 PLoS One Subcellular localization of FOXO3a in Calu-6 and H522 cells was detected with immunofluorescence staining after AZD6244 treatment.	26384399 20885957
Growth inhibition assay	Cell viability; PubMed: 26384399 Mol Cancer Ther MDA-MB-231 and SUM149 cells were treated with selumetinib for 72 hours, and then cell viability was measured using the WST-1 assay.	26384399

In vivo

AZD6244 significantly inhibits phosphorylation of ERK1/2 in 2-1318, 5-1318, 26-1004 and 4-1318 xenografts and induces apoptosis in primary 2-1318 cells by activating the caspase pathway. ^[1] AZD6244 could inhibit the tumor growth in HT-29 xenograft, which is a colorectal tumor model carrying a B-Raf mutation, at a dose of 100 mg/kg and the tumor growth inhibition of AZD6244 is better than it of Gemcitabine. ^[3] Otherwise AZD6244 could inhibit HCC xenografts tumor growth, which associated with increased apoptosis and down-regulation of cell cycle regulators, including cyclin D1, Cdc-2, CDK2 and 4, cyclin B1, and c-Myc. ^[4]

Protocol

Kinase Assay: ^[1]	- Collapse Assay of MEK Kinase Activity: Anti-MEK1 antibody is used to immunoprecipitate MEK1 molecules. MEK kinase activity is measured as the ability of immuno-isolated MEK1 to activate recombinant ERK1 in a coupled assay using MBP as the end point of the assay. Phosphorylated MBP is resolved on a 14% SDS-PAGE gel and vacuum-dried before exposure to X-ray film.
Cell Research: ^[1]	- Collapse Cell lines: Primary HCC cell lines including 2-1318, 4-1318 and 26-1004 cells Concentrations: ~ 10 μM Incubation Time: 24 or 48 hours Method: Cells are seeded at a density of 2.0 × 10⁴. After 48 hours incubation, the cells are rinsed twice with culture media. Cells are treated with various concentrations of AZD6244 for 24 or 48 hours. Cell viability is determined by the 3-(4,5-dimethylthiazol-2y1)-2,5-diphenyltetrazolium bromide (MTT) assay. Cell proliferation is assayed using a bromodeoxyuridine kit. (Only for Reference)
Animal Research: ^[1]	- Collapse Animal Models: HCC xenografts in mice homozygous for the SCID (severe combined immunodeficiency) mutation Dosages: 50 or 100mg/kg Administration: Administered via p.o. (Only for Reference)

References

- Collapse

Solubility (25°C)

In vitro	DMSO	91 mg/mL warmed (198.82 mM)
	Water	Insoluble
	Ethanol	Insoluble
In vivo	Add solvents to the product individually and in order(Data is from Selleck tests instead of citations): 4% DMSO+30% PEG 300+5% Tween 80+ddH2O For best results, use promptly after mixing.	5mg/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 Selumetinib (AZD6244) SDF

Molecular Weight	457.68
Formula	C₁₇H₁₅BrClFN₄O₃
CAS No.	606143-52-6
Storage	3 years-20°C powder 2 years-80°C in solvent
Synonyms	ARRY-142886
Smiles	CN1C=NC2=C1C=C(C(=C2F)NC3=C(C=C(C=C3)Br)Cl)C(=O)NOCCO

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 (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% 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 μL 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

Molarity Calculator

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

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

*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

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 )

* 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
Concertration (start):
Dilution-folds:

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):
C6=C5/X	C6:	LOG(C6):
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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

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

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

Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2021-05-17)

NCT Number	Recruitment	interventions	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT03433183	Recruiting	Drug: Selumetinib\|Drug: Sirolimus	Malignant Peripheral Nerve Sheath Tumors\|Neurofibromatosis 1	Sarcoma Alliance for Research through Collaboration\|United States Department of Defense\|AstraZeneca	October 2 2019	Phase 2
NCT03326388	Recruiting	Drug: Selumetinib	Neurofibromatosis Type 1\|Plexiform Neurofibroma\|Optic Nerve Glioma	Great Ormond Street Hospital for Children NHS Foundation Trust\|AstraZeneca	September 26 2019	Phase 1\|Phase 2
NCT03705507	Recruiting	Drug: Selumetinib\|Drug: Dexamethasone	Acute Lymphoblastic Leukemia\|Acute Lymphoblastic Leukemia Adult\|Acute Lymphoblastic Leukemia Pediatric\|Acute Lymphoblastic Leukemia in Relapse\|Acute Lymphoblastic Leukemia Recurrent	University of Birmingham\|Cancer Research UK\|AstraZeneca	May 18 2018	Phase 1\|Phase 2
NCT03162627	Recruiting	Drug: Selumetinib\|Drug: Olaparib	Malignant Neoplasm of Breast\|Malignant Neoplasms of Digestive Organs\|Malignant Neoplasms of Female Genital Organs\|Malignant Neoplasms of Male Genital Organs\|Malignant Neoplasms of Thyroid and Other Endocrine Glands	M.D. Anderson Cancer Center\|AstraZeneca	August 4 2017	Phase 1

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

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

Frequently Asked Questions

Question 1:
How about the solubility of S1008? How to prepare for the solution if I need to do the in vivo experiments?
Answer:
S1008 AZD6244 in vehicle 5% DMSO+30% PEG 300+ddH2O will be a suspension for oral administration. If you want a clear solution for injection, you can dissolve it in 4% DMSO+30% PEG 300+5% Tween 80+ddH2O.

MEK Signaling Pathway Map

MEK Inhibitors with Unique Features

Pan MEK Inhibitor

U0126-EtOH : MEK1, IC50=0.07 μM; MEK2, IC50=0.06 μM,
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 (G-868) is a potent and ATP-uncompetitive MEK1 inhibitor with K_i of 0.13 nM. Phase 1.
Trametinib (GSK1120212)

Trametinib (GSK1120212, JTP-74057, Mekinist) 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.
Mirdametinib (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.
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.
PD184352 (CI-1040)

PD184352 (CI-1040) is an ATP non-competitive MEK1/2 inhibitor with IC50 of 17 nM in cell-based assays, 100-fold more selective for MEK1/2 than MEK5. PD184352 (CI-1040) selectively induces apoptosis. Phase 2.

Features:First MEK inhibitor to begin clinical development.
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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Selumetinib (AZD6244)