Ceritinib (LDK378)

For research use only. Not for use in humans.

目录号：S7083

CAS No. 1032900-25-6

Ceritinib (LDK378)是一种有效的ALK抑制剂，在无细胞试验中IC50为0.2 nM。Ceritinib (LDK378)还可抑制IGF-1R、InsR、STK22D和FLT3对应的IC50值分别为8 nM、7 nM、23 nM和60 nM。Phase 3。

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价格

库存

购买数量

5mg	RMB 1182.86	现货
50mg	RMB 3868.47	现货
200mg	RMB 10720.71	现货
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客户使用Selleck生产的Ceritinib (LDK378)发表文献70篇：

Cell, 2021, 184(10):2649-2664.e18

PubMed: 33848463 ( click the link to review the publication )

Nature, 2019, 10.1038/s41586-019-1472-0

PubMed: 31391581 ( click the link to review the publication )

Cancer Cell, 2019, 36(2):179-193

PubMed: 31378681 ( click the link to review the publication )

Cell, 2019, 36(2):179-193

PubMed: 28162770 ( click the link to review the publication )

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

PubMed: 26301689 ( click the link to review the publication )

Cancer Cell, 2015, 27(3):397-408

PubMed: 25759024 ( click the link to review the publication )

Nat Med, 2014, 20(9):1027-34

PubMed: 25173427 ( click the link to review the publication )

Cereb Cortex, 2021, bhab058

PubMed: 33791755 ( click the link to review the publication )

ESMO Open, 2021, 6(4):100172

PubMed: 34242968 ( click the link to review the publication )

Sci Rep, 2021, 11(1):9011

PubMed: 33907223 ( click the link to review the publication )

Jpn J Clin Oncol, 2021, hyab048

PubMed: 33829270 ( click the link to review the publication )

Oncol Lett, 2021, 21(5):418

PubMed: 33841579 ( click the link to review the publication )

EMBO Mol Med, 2020, e11099

PubMed: 32558295 ( click the link to review the publication )

Clin Cancer Res, 2020, 8

PubMed: 32269053 ( click the link to review the publication )

Genome Med, 2020, 18;12(1):17

PubMed: 32070411 ( click the link to review the publication )

Cell Rep, 2020, 31(12):107800

PubMed: 32579927 ( click the link to review the publication )

Oncogene, 2020, 39(1):151-163

PubMed: 31462708 ( click the link to review the publication )

Cancers (Basel), 2020, 24;12(4) pii: E1054

PubMed: 32344689 ( click the link to review the publication )

Cancers (Basel), 2020, 26;12(4)

PubMed: 32224911 ( click the link to review the publication )

Cancer Discov, 2020, 1 pii: CD-19-1030

PubMed: 32238360 ( click the link to review the publication )

Int J Mol Sci, 2020, 21(9)E3214

PubMed: 32370101 ( click the link to review the publication )

Sci Rep, 2020, 10(1):218

PubMed: 31937834 ( click the link to review the publication )

Acta Pharmacol Sin, 2020, 10.1038/s41401-020-00513-3

PubMed: 32918045 ( click the link to review the publication )

Oncol Rep, 2020, 44(6):2581-2594

PubMed: 33125153 ( click the link to review the publication )
Hum Cell, 2020, 10.1007/s13577-020-00420-z

PubMed: 32870449 ( click the link to review the publication )

Cancer Cell, 2020, 38(1):44-59.e9

PubMed: 32663469 ( click the link to review the publication )

J Thorac Oncol, 2020, 15(5):752-765

PubMed: 31972351 ( click the link to review the publication )

Nat Commun, 2019, 10(1):4343

PubMed: 31554817 ( click the link to review the publication )

EMBO Mol Med, 2019, 10.15252/emmm.201910581

PubMed: 31633304 ( click the link to review the publication )

Cell Syst, 2019, 8(2):97-108

PubMed: 30797775 ( click the link to review the publication )

Oncogene, 2019, 101038/s41388-019-1136-4

PubMed: 31804622 ( click the link to review the publication )

Cancers (Basel), 2019, 11(1)E104

PubMed: 30658414 ( click the link to review the publication )

Int J Mol Sci, 2019, 20(17)

PubMed: 31480400 ( click the link to review the publication )

Sci Rep, 2019,

PubMed: 31882684 ( click the link to review the publication )

Biochem J, 2019, 10.1042/BCJ20190106

PubMed: 31341009 ( click the link to review the publication )

Invest New Drugs, 2019, 10.1007/s10637-019-00795-3

PubMed: 31124056 ( click the link to review the publication )

Invest New Drugs, 2019, 10.1007/s10637-019-00802-7

PubMed: 31177400 ( click the link to review the publication )

Cancer Immunol Res, 2019,

PubMed: 31540894 ( click the link to review the publication )

Blood, 2018, 131(14):1576-1586

PubMed: 29437595 ( click the link to review the publication )

Clin Cancer Res, 2018, 24(17):4162-4174

PubMed: 29776956 ( click the link to review the publication )

Clin Cancer Res, 2018, 24(23):6066-6077

PubMed: 30061362 ( click the link to review the publication )

Cancer Res, 2018, 78(24):6866-6880

PubMed: 30322862 ( click the link to review the publication )

Cell Death Differ, 2018, 25(12):2053-2070

PubMed: 29515255 ( click the link to review the publication )

Sci Signal, 2018, 11(557)

PubMed: 30459283 ( click the link to review the publication )

Cell Physiol Biochem, 2018, 46(6):2487-2499

PubMed: 29742496 ( click the link to review the publication )

Mol Cancer Ther, 2018, 17(11-:2271-2284

PubMed: 30135214 ( click the link to review the publication )

Mol Cancer Ther, 2018, 17(1):222-231

PubMed: 29054983 ( click the link to review the publication )

Mol Cancer Ther, 2018, 17(1):73-83

PubMed: 29133622 ( click the link to review the publication )
Mol Pharm, 2018, 15(5):1892-1900

PubMed: 29595984 ( click the link to review the publication )

Cancer Discov, 2018, 8(6):714-729

PubMed: 29650534 ( click the link to review the publication )

Cancer Chemother Pharmacol, 2018, 82(2):251-263

PubMed: 29855693 ( click the link to review the publication )

Onco Targets Ther, 2018, 11:8201-8209

PubMed: 30568455 ( click the link to review the publication )

Oncotarget, 2018, 9(43-:27242-27255

PubMed: 29930762 ( click the link to review the publication )

Sci Transl Med, 2017, 14;9(394):eaah6144

PubMed: 28615362 ( click the link to review the publication )

Cell Rep, 2017, 21(11):3298-3309

PubMed: 29241554 ( click the link to review the publication )

J Pathol, 2017, 243(3):307-319

PubMed: 28741662 ( click the link to review the publication )

Arch Toxicol, 2017, 91(8):2921-2938

PubMed: 28032146 ( click the link to review the publication )

Cancer Sci, 2017,

PubMed: 27783866 ( click the link to review the publication )

Anticancer Drugs, 2017, 28(10):1118-1125

PubMed: 29045271 ( click the link to review the publication )

Oncotarget, 2017, 8(35):58771-58780

PubMed: 28938595 ( click the link to review the publication )

J Pathol, 2016, 238(4):543-9

PubMed: 26606880 ( click the link to review the publication )

Oncoimmunology, 2016, 5(3):e1094598

PubMed: 27141355 ( click the link to review the publication )

Cell Physiol Biochem, 2016, 40(5):1129-1140

PubMed: 27960155 ( click the link to review the publication )

Mol Oncol, 2016, 10(4):601-9

PubMed: 26639656 ( click the link to review the publication )

Cancer Discov, 2016, 6(10):1118-1133

PubMed: 27432227 ( click the link to review the publication )

Sci Rep, 2016, 6:33710

PubMed: 27641368 ( click the link to review the publication )

Sci Rep, 2016, 10.1038/srep24817

PubMed: 27102549 ( click the link to review the publication )

Cell Res, 2015, 10.1038/cr.2015.16

PubMed: 25656847 ( click the link to review the publication )

Oncotarget, 2015, 6(42):44643-59

PubMed: 26556876 ( click the link to review the publication )

Biochem Biophys Res Commun, 2014, 454(4):566-571

PubMed: 25450694 ( click the link to review the publication )

产品安全说明书

ALK抑制剂选择性比较

生物活性

产品描述

特性

不与c-Met交叉反应，对体内葡萄糖稳态比TAE684效果好，有效作用于 Crizotinib复发的肿瘤。

靶点

ALK ^[1] (Cell-free assay)	Insulin Receptor ^[1] (Cell-free assay)	IGF-1R ^[1] (Cell-free assay)	STK22D ^[1] (Cell-free assay)	FLT3 ^[1] (Cell-free assay)
0.2 nM	7 nM	8 nM	23 nM	60 nM

体外研究

LDK378作用于Ba/F3-NPM-ALK和Karpas290细胞，具有显著的抗增殖活性，IC50分别为26.0 nM 和 22.8 nM,作用于Ba/F3-Tel-InsR 和Ba/F3-WT细胞，IC50分别为319.5 nM 和 2477 nM。^[1]

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	Formulation	Activity Description	PMID
Parental(+IL3)	NVez[WJST3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=		MWq3NkBp	MnrBSG1UVw>?	M3yybWlEPTB;MUW4OkDDuSBzN{Ogcm0>	NV\WdlAyRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW3OFkxOzRpPkK1O\|Q6ODN2PD;hQi=>
WT 70	M2HQPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7		M3;4OVczKGh?	M2HRO2ROW09?	Mn64TWM2OD1{MTFCtUA5KG6P	MWK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTd2OUCzOEc,OjV5NEmwN\|Q9N2F-
G1128S 1022	NYrrZos2T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=		M4HBWFczKGh?	M{L6fmROW09?	MlG5TWM2OD1zMEKgxtEhOzhibl2=	M1TESVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3N{S5NFM1Lz5{NUe0PVA{PDxxYU6=
C1156F 1293	NEfReoJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=		MmjhO\|IhcA>?	MnzDSG1UVw>?	MnHWTWM2OD1{MUegxtEhOTF3IH7N	MVS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTd2OUCzOEc,OjV5NEmwN\|Q9N2F-
I1171N 519	NGC5XIFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=		NGHJPWI4OiCq	NVKwfllLTE2VTx?=	NHzSVo9KSzVyPUG4O{DDuSB6NzDuUS=>	MVe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTd2OUCzOEc,OjV5NEmwN\|Q9N2F-
I1171T 445	MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?		MWm3NkBp	MYTEUXNQ	M{fGS2lEPTB;OEKgxtEhOTJibl2=	NYnaUVNHRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW3OFkxOzRpPkK1O\|Q6ODN2PD;hQi=>
F1174I 184	NXXO[o5PT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=		MkLwO\|IhcA>?	Ml3zSG1UVw>?	NWXEZoc4UUN3ME2xN{DDuSByLkGgcm0>	NIKwVGM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUe0PVA{PCd-MkW3OFkxOzR:L3G+
N1178H 169	MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?		MoP0O\|IhcA>?	NHXVNZJFVVOR	MYHJR\|UxRTR{INMxJFYhdk1?	M1vKfFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3N{S5NFM1Lz5{NUe0PVA{PDxxYU6=
E1210K 748	NX;N[GhLT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=		NVzGeWllPzJiaB?=	MY\EUXNQ	Ml3JTWM2OD1zOEegxtEhQDRibl2=	M{jLV\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3N{S5NFM1Lz5{NUe0PVA{PDxxYU6=
C1156F/D1203N 2809	M4XScGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7		MVi3NkBp	MnyzSG1UVw>?	MUDJR\|UxRTJ3NDFCtUA6QSCwTR?=	NYXm[5NURGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW3OFkxOzRpPkK1O\|Q6ODN2PD;hQi=>
Ba/F3 NA WT	MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?		MV:3NkBp		NGqyTYtKSzVyPUCuNFIxKM7:TR?=	MkC0QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV5Mke0NFAoRjJ3N{K3OFAxRC:jPh?=
Ba/F3 NA C1156Y	M{\temdzd3e2aDDJcohq[mm2aX;uJGF{e2G7		NEi2PWI4OiCq		Ml7ETWM2OD1yLkC3NUDPxE1?	M4TsXFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3N{K3OFAxLz5{NUeyO\|QxODxxYU6=
Ba/F3 NA L1196M	MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?		NFPP[3E4OiCq		NFnjellKSzVyPUCuNFQzKM7:TR?=	NVHDSWJURGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW3Nlc1ODBpPkK1O\|I4PDByPD;hQi=>
Ba/F3 NA L1152R	NGHZfYlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=		Mn3hO\|IhcA>?		M{O0SWlEPTB;MD6yPFgh\|ryP	MWm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTd{N{SwNEc,OjV5Mke0NFA9N2F-
Ba/F3 NA G1202R	NX3o[XFWT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=		M2XkcVczKGh?		NILPbm1KSzVyPUCuNlc4KM7:TR?=	NEfoTlQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUeyO\|QxOCd-MkW3Nlc1ODB:L3G+
Ba/F3 NA G1269A	MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?		MoDGO\|IhcA>?		MV3JR\|UxRTBwMEG5JO69VQ>?	MVW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTd{N{SwNEc,OjV5Mke0NFA9N2F-
Ba/F3 NA S1206Y	MnfTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?		NIDJVo04OiCq		NHmxXYRKSzVyPUCuNFM4KM7:TR?=	NWSzT\|E4RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW3Nlc1ODBpPkK1O\|I4PDByPD;hQi=>
Ba/F3 EA WT	M3\EWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7		NVvacFVNPzJiaB?=		M3rGemlEPTB;MD6wNlEh\|ryP	MV:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTd{N{SwNEc,OjV5Mke0NFA9N2F-
Ba/F3 EA C1156Y	MmPuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?		M1LYe\|czKGh?		NWnidIh{UUN3ME2wMlAzPiEQvF2=	NX;aZoN3RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW3Nlc1ODBpPkK1O\|I4PDByPD;hQi=>
Ba/F3 EA L1196M	MkTpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?		MmLyO\|IhcA>?		M1X4N2lEPTB;MD6wNVkh\|ryP	MonqQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV5Mke0NFAoRjJ3N{K3OFAxRC:jPh?=
Ba/F3 EA L1152R	M1rRcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7		M4fib\|czKGh?		NHG1NWlKSzVyPUCuNFk6KM7:TR?=	M3nSRlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3N{K3OFAxLz5{NUeyO\|QxODxxYU6=
Ba/F3 EA G1202R	MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?		MUm3NkBp		Mo\CTWM2OD1yLkS2O{DPxE1?	NIXQdZo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUeyO\|QxOCd-MkW3Nlc1ODB:L3G+
Ba/F3 EA G1269A	M4P6cmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7		MXq3NkBp		MlXuTWM2OD1yLkCzN{DPxE1?	Mn3wQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV5Mke0NFAoRjJ3N{K3OFAxRC:jPh?=
Ba/F3 EA S1206Y	MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?		Mn\oO\|IhcA>?		MXLJR\|UxRTBwMEO4JO69VQ>?	MlHHQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV5Mke0NFAoRjJ3N{K3OFAxRC:jPh?=
BAF3	M3K2WWFvfGmycn;sbYZmemG2aY\lJIF{e2G7		NUTwNXBCPzJiaILz		NWLKW2d2SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBud3W\|ZTDCRWY{KGOnbHzzJIhiemKxcnnu[{BGVUx2LVHMT{Bi\nSncjC3NkBpenNiYomgV3JDKG:{IFPDT\|gh[XO\|YYmsJGlEPTBiPTCwMlAyODdizszNMi=>	MWO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTJ6OEm0NEc,Ojl{OEi5OFA9N2F-
NCI-H3122	MVHBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>?		NEjjO204OiCqcoO=		NWHER\|RxSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDOR2kuUDNzMkKgZ4VtdHNiYX\0[ZIhPzJiaILzJIJ6KEOnbHzUbZRmei2JbH:gUJVucW6nc3PlcpQhS2WubDDWbYFjcWyrdImgRZN{[XluIFXDOVAhRSByLkCxOUDPxE1w	M{PJdlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4NU[4Nlg6Lz5{NkW2PFI5QTxxYU6=
NCI-H2228	NUTDdJNsT3Kxd4ToJIlvcGmkaYTpc44h[XO\|YYm=		NELLN3o{KGSjeYO=		NHLGZpBIem:5dHigbY5pcWKrdHnvckBw\iCqdX3hckBPS0lvSEKyNlgh[2WubIOgZYZ1\XJiMzDkZZl{KGK7IHz1cYlv\XOlZX7j[U1j[XOnZDDD[YxtXGm2ZYKtS4xwKGG\|c3H5MEBKSzVyIE2gNE4xOTVizszNMi=>	NYXWdWRWRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm2Nlc4OjVpPkK5OlI4PzJ3PD;hQi=>
SU-DHL1	MmHpS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl?		NXPHTWt6OyCmYYnz		NIixc5hIem:5dHigbY5pcWKrdHnvckBw\iCqdX3hckBUXS2GSFyxJINmdGy\|IHHmeIVzKDNiZHH5d{BjgSCudX3pcoV{[2WwY3WtZoF{\WRiQ3XscHRqfGW{LVfsc{Bie3OjeTygTWM2OCB;IECuNFE2KM7:TT6=	NGfxZZE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OU[yO\|czPSd-Mkm2Nlc4OjV:L3G+
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BAF3	MX;DfZRwfG:6aXPpeJkh[XO\|YYm=		NVzGRWhPOiC2bzCzJIRigXN?		NIDJUZREgXSxdH;4bYNqfHliYXfhbY5{fCCvb4Xz[UBDSUZ\|IHPlcIx{KGGodHXyJFIhfG9iMzDkZZl{KGK7IHz1Z4ln\XKjc3WgdoVxd3K2ZYKg[4Vv\SCjc4PhfUwhUUN3MDC9JFIvPDd5IN88UU4>	NWrKNXdyRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO3OFIzPTJpPkKzO\|QzOjV{PD;hQi=>
Ba/F3	M1zlO2Z2dmO2aX;uJIF{e2G7		M4H1N\|czKGi{cx?=		NFXybppKdmirYnn0bY9vKG:oIFXNUFQuSUyNIFyxNVUzWiCvdYThcpQhMHWwa37ve44hd3KrZ3nuLUBmgHC{ZYPz[YQhcW5ibX;1d4UhSmFxRkOgZ4VtdHNiYYPz[ZN{\WRiYYOgZ4VtdCC4aXHibYxqfHliYX\0[ZIhPzJiaILzJIJ6KE2WUzDhd5NigSxiSVO1NEA:KDJwN{S3JO69VS5?	M1rWU\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4NU[4Nlg6Lz5{NkW2PFI5QTxxYU6=
BA/F3	MXPDfZRwfG:6aXPpeJkh[XO\|YYm=		M4TOVFczKGi{cx?=		NIL4eHNEgXSxdH;4bYNqfHliYXfhbY5{fCCvb4Xz[UBDSS:IMzDj[YxteyCjc4Pld5Nm\CCjczDj[YxtKH[rYXLpcIl1gSCjZoTldkA4OiCqcoOgZpkhVVSVIHHzd4F6NCCLQ{WwJF0hPS53MUKg{txONg>?	MWO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjV4OEK4PUc,OjZ3NkiyPFk9N2F-
KARPAS299	MVfBdI9xfG:\|aYOgZZN{[Xl?	NXrhe\|V2PjBibl2=	MUmyOEBpenN?		NETCZ5BKdmS3Y4Tpc44hd2ZiYYDvdJRwe2m\|IHnuJIh2dWGwIFvBVnBCWzJ7OTDj[YxteyCqYYLic5JqdmdiTmDNMWFNUyCjdDC2NEBvVSCjZoTldkAzPCCqcoOgZpkh[WO{aXTpcoUhd3KjbnflM4V1cGmmaYXtJIJzd22rZHWgd5RicW6rbnegZoF{\WRiZnz1c5Jme2OnbnPlJI1q[3Kxc3PvdIlkKG2ndHjv[C=>	Mnf6QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjlzN{S4NFkoRjJ7MUe0PFA6RC:jPh?=
SU-DHL1	NXnEdFY3TnWwY4Tpc44h[XO\|YYm=	MVmyNEB1dyB{MECgcm0>	NEnSTZgyKGi{		MWjJcohq[mm2aX;uJI9nKEGOSzDpckBpfW2jbjDTWU1FUExzIHPlcIx{KGG\|c3Xzd4VlKGG\|IILl[JVkfGmxbjDpckBUXEGWMzDwbI9{eGixconsZZRqd25iYYSgXVcxPSC{ZYPp[JVmKGG2IEKwJJRwKDJyMDDuUUBi\nSncjCxJIhzKGK7IGfld5Rmem5iYnzveEBidmGueYPpdy=>	NV\lNY9pRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkmyPFg6PDBpPkK5Nlg5QTRyPD;hQi=>
SU-DHL1	MoTnSpVv[3Srb36gZZN{[Xl?	NFLCW\|MzOCC2bzCyNFAhdk1?	MYCxJIhz		MmLRTY5pcWKrdHnvckBw\iCDTFugdIhwe3Cqb4L5cIF1cW:wIHH0JHkyOjd6IILld4llfWViaX6gbJVu[W5iU2WtSGhNOSClZXzsd{BifCB{MDD0c{AzODBibl2gZYZ1\XJiMTDodkBjgSCZZYP0[ZJvKGKub4SgZY5idHm\|aYO=	NVLxU\|ZVRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkmyPFg6PDBpPkK5Nlg5QTRyPD;hQi=>
NCI-H3122	M4XOc2Z2dmO2aX;uJIF{e2G7	M4jhb\|IxKHSxIEKwNEBvVQ>?	M37TW\|EhcHJ?		M{X4UWlvcGmkaYTpc44hd2ZiQVzLJIlvKGi3bXHuJG5EUS2KM{GyNkBk\WyuczDhd5Nme3OnZDDhd{Bz\WS3Y4Tpc44hcW5iRWLLJJBpd3OyaH;yfYxifGmxbjDheEBVOjB{Lz;ZNlA1KHKnc3nkeYV{KGG2IEKwJJRwKDJyMDDuUUBi\nSncjCxJIhzKGK7IGfld5Rmem5iYnzveEBidmGueYPpdy=>	MWO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTJ6OEm0NEc,Ojl{OEi5OFA9N2F-
NCI-H3122	NXzUXJJrTnWwY4Tpc44h[XO\|YYm=	NI\3N5UzOCC2bzCyNFAhdk1?	NHPFTW0yKGi{		M{K2dWlvcGmkaYTpc44hd2ZiQVzLJIlvKGi3bXHuJG5EUS2KM{GyNkBk\WyuczDhd5Nme3OnZDDhd{Bz\WS3Y4Tpc44hcW5iQXv0JJBpd3OyaH;yfYxifGmxbjDheEBUPDd\|IILld4llfWViYYSgNlAhfG9iMkCwJI5OKGGodHXyJFEhcHJiYomgW4V{fGW{bjDicI91KGGwYXz5d4l{	NHvRV3k9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUK4PFk1OCd-MkmyPFg6PDB:L3G+
SU-DHL1	M3rkfWZ2dmO2aX;uJIF{e2G7	M{Hse\|IxKHSxIEKwNEBvVQ>?	MkDVNUBpeg>?		M123[mlvcGmkaYTpc44hd2ZiQVzLJIlvKGi3bXHuJHNWNUSKTEGgZ4VtdHNiYYPz[ZN{\WRiYYOgdoVlfWO2aX;uJIlvKEGtdDDwbI9{eGixconsZZRqd25iYYSgV\|Q4OyC{ZYPp[JVmKGG2IEKwJJRwKDJyMDDuUUBi\nSncjCxJIhzKGK7IGfld5Rmem5iYnzveEBidmGueYPpdy=>	NHPqS4E9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUK4PFk1OCd-MkmyPFg6PDB:L3G+
SU-DHL1	NWizZYk6TnWwY4Tpc44h[XO\|YYm=	NXXNTWtOOjBidH:gNlAxKG6P	NXzI[o96OSCqch?=		NXe0SYo{UW6qaXLpeIlwdiCxZjDBUGshcW5iaIXtZY4hW1VvRFjMNUBk\WyuczDhd5Nme3OnZDDhd{Bz\WS3Y4Tpc44hcW5iRWLLJJBpd3OyaH;yfYxifGmxbjDheEBVOjB{Lz;ZNlA1KHKnc3nkeYV{KGG2IEKwJJRwKDJyMDDuUUBi\nSncjCxJIhzKGK7IGfld5Rmem5iYnzveEBidmGueYPpdy=>	MYi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTJ6OEm0NEc,Ojl{OEi5OFA9N2F-
NCI-H3122	Mnn5SpVv[3Srb36gZZN{[Xl?	NGfZdnEzOCC2bzCyNFAhdk1?	M13PWFEhcHJ?		M3n2PGlvcGmkaYTpc44hd2ZiQVzLJJBpd3OyaH;yfYxifGmxbjDheEB[OTJ5ODDy[ZNq\HWnIHnuJIh2dWGwIF7DTU1JOzF{MjDj[YxteyCjdDCyNEB1dyB{MECgcm0h[W[2ZYKgNUBpeiCkeTDX[ZN1\XKwIHLsc5Qh[W6jbInzbZM>	M{\ndlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7Mki4PVQxLz5{OUK4PFk1ODxxYU6=
NCI-H3122	MWTGeY5kfGmxbjDhd5NigQ>?	NW\Leok6OjBidH:gNlAxKG6P	NVz0XpR5OSCqch?=		M{T0WGlvcGmkaYTpc44hd2ZiQVzLJIlvKGi3bXHuJG5EUS2KM{GyNkBk\WyuczDhd5Nme3OnZDDhd{Bz\WS3Y4Tpc44hcW5iU2TBWFMheGixc4Doc5J6dGG2aX;uJIF1KFl5MEWgdoV{cWS3ZTDheEAzOCC2bzCyNFAhdk1iYX\0[ZIhOSCqcjDifUBY\XO2ZYLuJIJtd3RiYX7hcJl{cXN?	M1nnPVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7Mki4PVQxLz5{OUK4PFk1ODxxYU6=
SU-DHL1	MnXsSpVv[3Srb36gZZN{[Xl?	MXyzNEBvVQ>?	MojsNVYhcHK\|		NWLoc2JKUW6qaXLpeIlwdiCxZjDBUGsh[XW2b4Doc5NxcG:{eXzheIlwdiCjdDDZNVUxPyC{ZYPp[JVmKGmwIHj1cYFvKFOXLVTIUFEh[2WubIOgZZQhOzBibl2gZYZ1\XJiMU[gbJJ{KGK7IGfld5Rmem5iYnzveEBidmGueYPpdy=>	NHHZeHM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OU[yO\|czPSd-Mkm2Nlc4OjV:L3G+
SU-DHL1	MXPGeY5kfGmxbjDhd5NigQ>?	M3jrd\|MxKG6P	Ml7FNVYhcHK\|		M3j4OmlvcGmkaYTpc44hd2ZiQVzLJIlvKGi3bXHuJHNWNUSKTEGgZ4VtdHNiYYPz[ZN{\WRiYYOgdoVlfWO2aX;uJIlvKFOWQWSzJJBpd3OyaH;yfYxifGmxbjDheEB[PzB3IILld4llfWViYYSgN\|Ahdk1iYX\0[ZIhOTZiaILzJIJ6KFenc4Tldo4h[myxdDDhcoFtgXOrcx?=	NUTzXo5RRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm2Nlc4OjVpPkK5OlI4PzJ3PD;hQi=>
NCI-H3122	NGCzU29HfW6ldHnvckBie3OjeR?=	MXS1NEB1dyB{NUCgcm0>	M2DzNlE3KGi{cx?=		M13v[Wlv\HWldHnvckBw\iCDTFug[IVoemGmYYTpc44hcW5iaIXtZY4hVkOLLVizNVIzKGOnbHzzJIF{e2W\|c3XkJIF{KGSnY4LlZZNmKGmwIFHMT{BxcG:\|cHjvdplt[XSrb36gZZQhYTF4MESgZZQhPTBidH:gNlUxKG6PIHHmeIVzKDF4IHjyd{BjgSCrbX31co9jdG:2IH3leIhw\A>?	MY[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTZ4MEm4OEc,Ojl4NkC5PFQ9N2F-
SH-SY5Y	NV71cXYxSW62aYDyc4xq\mW{YYTpeoUh[XO\|YYm=		M2\WSlczKGi{cx?=		MlfERY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6\|dDDoeY1idiCVSD3TXVV[KGOnbHzzJIFnfGW{IEeyJIhzeyCkeTDD[YxtXGm2ZYKtS4xwKGy3bXnu[ZNk\W62IHPlcIwhfmmjYnnsbZR6KGG\|c3H5	M3LQb\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7Nk[wPVg1Lz5{OU[2NFk5PDxxYU6=
CHLA20	MWDBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>?		MnroO\|IhcHK\|		M3HmXGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iQ1jMRVIxKGOnbHzzJIFnfGW{IEeyJIhzeyCkeTDD[YxtXGm2ZYKtS4xwKGy3bXnu[ZNk\W62IHPlcIwhfmmjYnnsbZR6KGG\|c3H5	MXm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTZ4MEm4OEc,Ojl4NkC5PFQ9N2F-
SH-SY5Y	NV\XeIpmSW62aYDyc4xq\mW{YYTpeoUh[XO\|YYm=		MmrCO\|IhcHK\|		MXvBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFOKLWPZOXkh[2WubIOgZYZ1\XJiN{KgbJJ{KGmwIIDy[ZNmdmOnIH;mJGFDS0JzIHnubIljcXSxcjD0ZZJqeXWrZHHyJIJ6KEOnbHzUbZRmei2JbH:gcJVucW6nc3PlcpQh[2WubDD2bYFjcWyrdImgZZN{[Xl?	NE\ZPG49[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OU[2NFk5PCd-Mkm2OlA6QDR:L3G+
KARPAS299	MkL5SpVv[3Srb36gZZN{[Xl?	M4jrcVUxKHSxIEK1NEBvVQ>?	Ml30NVYhcHK\|		MkHQTY5lfWO2aX;uJI9nKEGOSzDk[Ydz[WSjdHnvckBqdiCqdX3hckBMSVKSQWOyPVkh[2WubIOgZZN{\XO\|ZXSgZZMh\GWlcnXhd4UhcW5iQVzLJJBpd3OyaH;yfYxifGmxbjDheEB[OTZyNDDheEA2OCC2bzCyOVAhdk1iYX\0[ZIhOTZiaILzJIJ6KGmvbYXuc4Jtd3RibXX0bI9l	MVG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTZ4MEm4OEc,Ojl4NkC5PFQ9N2F-
CHLA20	NUP4XmI5SW62aYDyc4xq\mW{YYTpeoUh[XO\|YYm=		M2jPd\|czKGi{cx?=		NV3HcJFWSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDDTGxCOjBiY3XscJMh[W[2ZYKgO\|IhcHK\|IHnuJJBz\XOnbnPlJI9nKEGEQ1KxJIlvcGmkaYTvdkB1[XKrcYXp[IFzKGK7IFPlcIxVcXSncj3HcI8hdHWvaX7ld4NmdnRiY3XscEB3cWGkaXzpeJkh[XO\|YYm=	NIXxe2o9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OU[2NFk5PCd-Mkm2OlA6QDR:L3G+
NCI-H3122	NIf5XVBCdnSrcILvcIln\XKjdHn2[UBie3OjeR?=		M3THOVczKGi{cx?=		M{DreWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTlPJMWg{OTJ{IHPlcIx{KGGodHXyJFczKGi{czDifUBE\WyuVHn0[ZIuT2yxIHz1cYlv\XOlZX70JINmdGxidnnhZoltcXS7IHHzd4F6	NVfkd4dPRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm2OlA6QDRpPkK5OlYxQTh2PD;hQi=>
KARPAS299	MUjBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>?		MXK3NkBpenN?		NGXT[5lCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFvBVnBCWzJ7OTDj[YxteyCjZoTldkA4OiCqcoOgZpkhS2WubGTpeIVzNUeubzDseY1qdmW\|Y3XueEBk\WyuII\pZYJqdGm2eTDhd5NigQ>?	M3LSZ\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7Nk[wPVg1Lz5{OU[2NFk5PDxxYU6=
SU-DHL1	MoC2RY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl?		M1LrWlczKGi{cx?=		M1Thb2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iU2WtSGhNOSClZXzsd{Bi\nSncjC3NkBpenNiYomgR4VtdFSrdHXyMWdtdyCudX3pcoV{[2WwdDDj[YxtKH[rYXLpcIl1gSCjc4PhfS=>	MoDhQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl4NkC5PFQoRjJ7Nk[wPVg1RC:jPh?=
KARPAS299	NHPlfGtCeG:ydH;zbZMh[XO\|YYm=	MlnkOVAhdk1?	MofXNlQhcHK\|		NHn0PYhKdmS3Y4Tpc44hd2ZiYYDvdJRwe2m\|IHnuJIh2dWGwIFvBVnBCWzJ7OTDj[YxteyCjc4Pld5Nm\CCjczD1coNt\WG{IHPlcIwhe2i{aX7rZYdmKGG2IEWwJI5OKGGodHXyJFI1KGi{czDifUBJd2WlaIP0JFM{OjV6IIP0ZYlvcW6pIHLhd4VlKGmwdnXyeIVlKG[udX;y[ZNk\W6lZTDtbYNzd3Olb4D5	M1jJTFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyMkKzNVIxLz5\|MEKyN\|EzODxxYU6=
KARPAS299	NIG5U5lCeG:ydH;zbZMh[XO\|YYm=	M1nrNVUxKG6P	MkXINlQhcHK\|		MUjJcoR2[3Srb36gc4Yh[XCxcITvd4l{KGmwIHj1cYFvKEuDUmDBV\|I6QSClZXzsd{Bie3Onc4Pl[EBieyCuYYTlJIFxd3C2b4TpZ{Bk\WyuczDheEA2OCCwTTDh[pRmeiB{NDDodpMh[nliQV:vSWIh\G:3YnzlJJN1[WmwaX7nJIJie2WmIHnueoVzfGWmIH\seY9z\XOlZX7j[UBucWO{b4Pjc5B6	M2jWRlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyMkKzNVIxLz5\|MEKyN\|EzODxxYU6=
KARPAS299	M2TCZWFxd3C2b4Ppd{Bie3OjeR?=	NWHWZ4drPTBibl2=	NH[5TlYzPCCqcoO=		NVTlcY9oUW6mdXP0bY9vKG:oIHHwc5B1d3OrczDpckBpfW2jbjDLRXJRSVN{OUmgZ4VtdHNiYYPz[ZN{\WRiYYOg[pJi\22nboTheIlwdiCjdDC1NEBvVSCjZoTldkAzPCCqcoOgZpkhUG:nY3jzeEA{OzJ3ODDzeIFqdmmwZzDiZZNm\CCrbo\ldpRm\CCobIXvdoV{[2WwY3WgcYlkem:\|Y3;wfS=>	M1LzelxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyMkKzNVIxLz5\|MEKyN\|EzODxxYU6=

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Assay

Methods	Test Index	PMID
Western blot	p-ALK / ALK / p-AKT / AKT / p-ERK / ERK; PubMed: 28425916 eLife Inhibition of ALK autophosphorylation and downstream signaling by ceritinib, crizotinib and PF06463922 in NB-1 cells. Cells were harvested after treatment for 4 hr with the indicated compounds at different concentrations. Whole cell lysates were analyzed by Western blotting to detect the levels of ALK, AKT and ERK proteins and their phosphorylation. pROS1 / ROS1 / pSTAT3 / STAT3 ; PubMed: 25351743 Clin Cancer Res Inhibition of phospho-ROS1 by various ALK inhibitors in Ba/F3 models. CD74-ROS1 expressing Ba/F3 cells were exposed to increasing concentrations of crizotinib, ceritinib, AP26113, or ASP3026 for 3 h. Cell lysates were immunoblotted to detect the indicated proteins.	28425916 25351743
Growth inhibition assay	Cell viability; PubMed: 29067644 Target Oncol The effects of ceritinib treatment on cell viability in ARMS and ERMS cell lines. Cells were treated with 0-5 μM ceritinib for 72 h (Rh30, RD), 120 h (Rh41), or 144 h (Rh18, Aska) and cell viability was assessed. The y-axis represents relative cell viability compared to non-treated cells (control). Effects on cell viability were determined in triplicate. Values are presented as mean ± SD. Dotted line represents the IC50-value. The human synovial sarcoma cell line Aska with constitutive ALK phosphorylation was used as a positive control.	29067644

体内研究

LDK378 用于降低形成反应代谢的可能性，在肝微粒体几乎检测不到谷胱甘肽（GSH）加合物的水平（<1％）。LDK378具有相对良好的代谢稳定性，中度抑制CYP3A4（Midazolam底物）和抑制hERG。LDK378处理动物，与肝脏血流量相比，具有低的血浆清除率（小鼠，大鼠，狗和猴），处理小鼠，大鼠，狗和猴的口服生物利用度都在55％以上。LDK378 处理Karpas299 和H2228 大鼠移植瘤模型，抑制肿瘤生长，诱导肿瘤衰退，这种作用具有剂量依赖性，体重没有降低。LDK378处理小鼠，剂量高达100 mg/kg，对胰岛素水平或血浆葡萄糖的利用无影响。^[1]

激酶实验：^[1]	- 合并激酶分析: 所有激酶使用杆状病毒表达技术表达为组氨酸或GST标签的融合蛋白，除了在大肠杆菌中产生的未标记的ERK2。在LabChip迁移实验中测量激酶活性。实验在30°C下进行60分钟。在有或无LDK378存在时，通过线性进展曲线，获得LDK378对酶活性的作用效果。
细胞实验：^[1]	- 合并 Cell lines: Ba/F3-NPM-ALK, Ba/F3-Tel-InsR, Ba/F3-WT, Karpas299 细胞 Concentrations: ~100 μM Incubation Time: 2-3 天 Method: 表达荧光素酶的细胞与连续稀释的LDK378 或 DMSO 温育2-3天。荧光素酶的表达用来衡量细胞增殖/存活，使用Bright-Glo萤光素酶检测系统来评估。使用 XLFit软件获得 IC50值。 (Only for Reference)
动物实验：^[1]	- 合并 Animal Models: 携带 Karpas299/H2228肿瘤的 RNU裸鼠 Dosages: ~50 mg/kg Administration: 口服饲喂 (Only for Reference)

参考文献

[1] Marsilje TH, et al. J Med Chem. 2013, Jun 6.

溶解度 (25°C)

体外	DMSO	20 mg/mL warmed (35.83 mM)
	Ethanol	3 mg/mL (5.37 mM)
	Water	Insoluble

* 溶解度检测是由Selleck技术部门检测的，可能会和文献中提供的溶解度有所差异，这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。

化学数据 Download Ceritinib (LDK378) SDF

分子量	558.14
化学式	C₂₈H₃₆ClN₅O₃S
CAS号	1032900-25-6
储存条件	3年-20°C 粉状 2年-80°C 溶于溶剂
别名	N/A

动物体内配方计算器 (澄清溶液)

第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）

给药剂量

mg/kg

动物平均体重

每只动物给药体积

动物数量

只

第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系Selleck为您提供正确的澄清溶液配方）

% DMSO+ % + % Tween 80+ % ddH₂O

计算重置

计算结果:

工作液浓度： mg/ml；

DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系Selleck）；

体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL ddH₂O，混匀澄清。

注意：1. 首先保证母液是澄清的；
2. 一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。

计算器

摩尔浓度计算器

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为:

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)

摩尔浓度计算公式

质量

浓度

体积

分子量
=

×

×

*在配置溶液时，请务必参考Selleck产品标签上、MSDS / COA（可在Selleck的产品页面获得）批次特异的分子量使用本工具。

稀释计算器

用本工具协助配置特定浓度的溶液，使用的计算公式为：

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入输出 )

C1

V1

C2

V2
×

=

×

在配置溶液时，请务必参考Selleck产品标签上、MSDS / COA（可在Selleck的产品页面获得）批次特异的分子量使用本工具。.

连续稀释计算器方程

连续稀释
初始浓度:
稀释倍数:

计算结果

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):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):

分子量计算器

通过输入化合物的化学式来计算其分子量：

注：化学分子式大小写敏感。C10H16N2O2 c10h16n2o2

摩尔浓度计算器

质量	浓度	体积	分子量
=	×	×
计算

临床试验信息 (data from https://clinicaltrials.gov, updated on 2021-05-17)

NCT Number	Recruitment	interventions	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT02450903	Completed	Drug: LDK378	Non-Small-Cell Lung Cancer	Novartis Pharmaceuticals\|Novartis	August 21 2015	Phase 2
NCT02040870	Completed	Drug: LDK378	Non-Small Cell Lung Cancer	Novartis Pharmaceuticals\|Novartis	March 7 2014	Phase 1\|Phase 2
NCT01950481	Completed	Drug: LDK378	Normal Hepatic Function\|Impaired Hepatic Function	Novartis Pharmaceuticals\|Novartis	January 2014	Phase 1
NCT01772797	Completed	Drug: LDK378\|Drug: AUY922	Anaplastic Lymphoma Kinase (ALK)\|Non-small Cell Lung Cancer	Novartis Pharmaceuticals\|Novartis	June 2013	Phase 1
NCT01685060	Completed	Drug: LDK378	Non-Small Cell Lung Cancer	Novartis Pharmaceuticals\|Novartis	November 26 2012	Phase 2
NCT01634763	Completed	Drug: LDK378	Tumors Characterized by Genetic Alterations in Anaplastic Lymphoma Kinase (ALK)	Novartis Pharmaceuticals\|Novartis	June 2012	Phase 1

技术支持

在订购、运输、储存和使用我们的产品的任何阶段，您遇到的任何问题，均可以通过拨打我们的热线电话400-668-6834，或者技术支持邮箱tech@selleck.cn，直接联系到我们。我们会在24小时内尽快联系您。

操作手册

如果有其他问题，请给我们留言。

常见问题及建议解决方法

问题 1：
how to reconstitute the inhibitor for oral administration to mice?
回答：
You can resuspend LDK378 in 30% PEG400/0.5% Tween 80/5% propylene glycol and use the suspension for oral gavage feeding.

ALK Signaling Pathway Map

ALK Inhibitors with Unique Features

非特异性的ALK抑制剂

GSK1838705A : IGF-1R, IC50=2.0 nM; IR, IC50=1.6 nM, ALK, IC50=0.5 nM.
FDA批准的ALK抑制剂

Crizotinib (PF-02341066) : Approved by FDA for non-small cell lung carcinoma (NSCLC).
最新的ALK抑制剂

ASP3026 ^New : Novel and selective inhibitor for ALK with IC50 of 3.5 nM.
经典的ALK抑制剂

TAE684 (NVP-TAE684) : Potent and selective ALK inhibitor with IC50 of 3 nM, 100-fold more sensitive for ALK than InsR.

研究领域

产品类型

定制您的化合物库

Ceritinib (LDK378)

客户使用Selleck生产的Ceritinib (LDK378)发表文献70篇：

产品安全说明书

ALK抑制剂选择性比较

生物活性

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

参考文献

溶解度 (25°C)

化学数据 Download Ceritinib (LDK378) SDF

动物体内配方计算器 (澄清溶液)

计算器

摩尔浓度计算器

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)

摩尔浓度计算公式

稀释计算器

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

连续稀释计算器方程

连续稀释

计算结果

分子量计算器

总分子量：g/mol

摩尔浓度计算器

临床试验信息 (data from https://clinicaltrials.gov, updated on 2021-05-17)

技术支持

常见问题及建议解决方法

ALK Signaling Pathway Map

ALK Inhibitors with Unique Features

相关ALK产品