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Ceritinib (LDK378)

Name: Ceritinib (LDK378)
Brand: Selleck Chemicals
SKU: S7083
Rating: 5 (82 reviews)

Catalog No.S7083

For research use only.

Ceritinib (LDK378) is potent inhibitor against ALK with IC50 of 0.2 nM in cell-free assays. Ceritinib (LDK378) also inhibits IGF-1R, InsR, STK22D and FLT3 with IC50 of 8 nM, 7 nM, 23 nM and 60 nM, respectively. Phase 3.

CAS No. 1032900-25-6

Selleck's Ceritinib (LDK378) has been cited by 82 publications

Purity & Quality Control

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ALK Signaling Pathway Map

Biological Activity

Description

Features

Does not cross react with c-Met, and has an improved in vivo glucose homeostasis profile relative to TAE684. May be active in Crizotinib-relapsed tumors.

Targets

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

In vitro

LDK378 shows great anti-proliferative activity in Ba/F3-NPM-ALK and Karpas290 cells with IC50 of 26.0 nM and 22.8 nM, compared with IC50 of 319.5 nM and 2477 nM in Ba/F3-Tel-InsR and Ba/F3-WT cells. ^[1]

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	Formulation	Activity Description	PMID

Parental(+IL3)	MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?		NHPRVJU4OiCq	Mlu5SG1UVw>?	M4noTWlEPTB;MUW4OkDDuSBzN{Ogcm0>	MlTLQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV5NEmwN\|QoRjJ3N{S5NFM1RC:jPh?=
WT 70	NGKyN2hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=		MUi3NkBp	NH\POnZFVVOR	NVrabnJSUUN3ME2yNUDDuSB6IH7N	Mnz6QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV5NEmwN\|QoRjJ3N{S5NFM1RC:jPh?=
G1128S 1022	NWPXd5hkT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=		NGnaUIE4OiCq	NVPL[ndRTE2VTx?=	MmXoTWM2OD1zMEKgxtEhOzhibl2=	MXG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTd2OUCzOEc,OjV5NEmwN\|Q9N2F-
C1156F 1293	NFTnSVBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=		NH3iVHg4OiCq	NH;DUYRFVVOR	NInCSpZKSzVyPUKxO{DDuSBzMUWgcm0>	NGnidIg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUe0PVA{PCd-MkW3OFkxOzR:L3G+
I1171N 519	MnK2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?		M1L4b\|czKGh?	NFrJV2ZFVVOR	NXy3e4Y4UUN3ME2xPFchyrFiOEegcm0>	MUC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTd2OUCzOEc,OjV5NEmwN\|Q9N2F-
I1171T 445	NVfiZXJ2T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=		MVy3NkBp	M1TRS2ROW09?	NWfNS2dyUUN3ME24NkDDuSBzMjDuUS=>	M33sXlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3N{S5NFM1Lz5{NUe0PVA{PDxxYU6=
F1174I 184	NW\3[YkxT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=		NV3YOYRbPzJiaB?=	MXjEUXNQ	MWfJR\|UxRTF\|INMxJFAvOSCwTR?=	Ml3jQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV5NEmwN\|QoRjJ3N{S5NFM1RC:jPh?=
N1178H 169	MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?		Mli1O\|IhcA>?	MWfEUXNQ	MoLCTWM2OD12MjFCtUA3KG6P	M1;4c\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3N{S5NFM1Lz5{NUe0PVA{PDxxYU6=
E1210K 748	MmLpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?		MXi3NkBp	MXvEUXNQ	MnXaTWM2OD1zOEegxtEhQDRibl2=	MnTaQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV5NEmwN\|QoRjJ3N{S5NFM1RC:jPh?=
C1156F/D1203N 2809	Mn3XS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?		Ml3SO\|IhcA>?	M4jTe2ROW09?	MWTJR\|UxRTJ3NDFCtUA6QSCwTR?=	MUW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTd2OUCzOEc,OjV5NEmwN\|Q9N2F-
Ba/F3 NA WT	NYrLOIt1T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=		M1zpPVczKGh?		MoLkTWM2OD1yLkCyNEDPxE1?	MXm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTd{N{SwNEc,OjV5Mke0NFA9N2F-
Ba/F3 NA C1156Y	NEPkNYFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=		MnuzO\|IhcA>?		M4fFUmlEPTB;MD6wO\|Eh\|ryP	M1XscFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3N{K3OFAxLz5{NUeyO\|QxODxxYU6=
Ba/F3 NA L1196M	NIHzbI1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?=		MmXqO\|IhcA>?		MlfUTWM2OD1yLkC0NkDPxE1?	M4S0dFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3N{K3OFAxLz5{NUeyO\|QxODxxYU6=
Ba/F3 NA L1152R	M4fvNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7		NIK0UmE4OiCq		NGe5S2xKSzVyPUCuNlg5KM7:TR?=	NFjIb2I9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUeyO\|QxOCd-MkW3Nlc1ODB:L3G+
Ba/F3 NA G1202R	NGX3c\|VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=		NYPqVGxSPzJiaB?=		NGnZW\|BKSzVyPUCuNlc4KM7:TR?=	NXnYdZIzRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW3Nlc1ODBpPkK1O\|I4PDByPD;hQi=>
Ba/F3 NA G1269A	MkO2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?		NFXYV444OiCq		MWLJR\|UxRTBwMEG5JO69VQ>?	MXe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTd{N{SwNEc,OjV5Mke0NFA9N2F-
Ba/F3 NA S1206Y	Mn\CS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?		MlLjO\|IhcA>?		NVzFdFBUUUN3ME2wMlA{PyEQvF2=	MXy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTd{N{SwNEc,OjV5Mke0NFA9N2F-
Ba/F3 EA WT	MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?		Mlu4O\|IhcA>?		MofTTWM2OD1yLkCyNUDPxE1?	NW[zdJd[RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW3Nlc1ODBpPkK1O\|I4PDByPD;hQi=>
Ba/F3 EA C1156Y	NVjjSG1KT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=		NI\BNVI4OiCq		NFTabW9KSzVyPUCuNFI3KM7:TR?=	M{\ocFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3N{K3OFAxLz5{NUeyO\|QxODxxYU6=
Ba/F3 EA L1196M	NFfIU2FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=		NGTyV5Q4OiCq		NV;6Rml[UUN3ME2wMlAyQSEQvF2=	M{T6VVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3N{K3OFAxLz5{NUeyO\|QxODxxYU6=
Ba/F3 EA L1152R	M3f1Xmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7		NVTo[GdlPzJiaB?=		NIPRcodKSzVyPUCuNFk6KM7:TR?=	NYHBWFhpRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW3Nlc1ODBpPkK1O\|I4PDByPD;hQi=>
Ba/F3 EA G1202R	NWiwc4lET3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=		NUXSNWFQPzJiaB?=		NIPTPJZKSzVyPUCuOFY4KM7:TR?=	M1HZ[VxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3N{K3OFAxLz5{NUeyO\|QxODxxYU6=
Ba/F3 EA G1269A	NX;kU2d1T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=		MWK3NkBp		MXTJR\|UxRTBwMEOzJO69VQ>?	NIfEdms9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUeyO\|QxOCd-MkW3Nlc1ODB:L3G+
Ba/F3 EA S1206Y	M1z3S2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7		MYe3NkBp		MV\JR\|UxRTBwMEO4JO69VQ>?	NWjmXZNvRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW3Nlc1ODBpPkK1O\|I4PDByPD;hQi=>
BAF3	MWDBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>?		NU\EWW02PzJiaILz		NFX1S\|NCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JI1wfXOnIFLBSlMh[2WubIOgbIFz[m:{aX7nJGVOVDRvQVzLJIFnfGW{IEeyJIhzeyCkeTDTVmIhd3JiQ1PLPEBie3OjeTygTWM2OCB;IECuNFExPyEQvF2u	MWq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTJ6OEm0NEc,Ojl{OEi5OFA9N2F-
NCI-H3122	MYLBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>?		MX[3NkBpenN?		NEH0SYRCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF7DTU1JOzF{MjDj[YxteyCjZoTldkA4OiCqcoOgZpkhS2WubGTpeIVzNUeubzDMeY1qdmW\|Y3XueEBE\WyuIG\pZYJqdGm2eTDBd5NigSxiRVO1NEA:KDBwMEG1JO69VS5?	M1L6NVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4NU[4Nlg6Lz5{NkW2PFI5QTxxYU6=
NCI-H2228	MY\Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>?		NWjiTXZOOyCmYYnz		M4T5R2dzd3e2aDDpcohq[mm2aX;uJI9nKGi3bXHuJG5EUS2KMkKyPEBk\WyuczDh[pRmeiB\|IHThfZMh[nlibIXtbY5me2OnbnPlMYJie2WmIFPlcIxVcXSncj3HcI8h[XO\|YYmsJGlEPTBiPTCwMlAyPSEQvF2u	M3HNNVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NkK3O\|I2Lz5{OU[yO\|czPTxxYU6=
SU-DHL1	NF7LR2dIem:5dHigbY5pcWKrdHnvckBie3OjeR?=		MoPwN{Bl[Xm\|		NYrBWo11T3Kxd4ToJIlvcGmkaYTpc44hd2ZiaIXtZY4hW1VvRFjMNUBk\WyuczDh[pRmeiB\|IHThfZMh[nlibIXtbY5me2OnbnPlMYJie2WmIFPlcIxVcXSncj3HcI8h[XO\|YYmsJGlEPTBiPTCwMlAyPSEQvF2u	MVO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTZ{N{eyOUc,Ojl4Mke3NlU9N2F-
DFCI114	MVvBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>?		NVvnVmdYPzJiaILz		NUDHdXVCSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDESmNKOTF2IHPlcIx{KGW6cILld5NqdmdiRV3MOE1CVEtiR{GyOllCKG23dHHueEBi\nSncjC3NkBpenNiYomgR4VtdFSrdHXyMWdtdyCOdX3pcoV{[2WwdDDD[YxtKF[rYXLpcIl1gSCDc4PhfUwhTUN3MDC9JFAvODF6IN88UU4>	M{Pp[FxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4NU[4Nlg6Lz5{NkW2PFI5QTxxYU6=
HCC78	M2PjOWN6fG:2b4jpZ4l1gSCjc4PhfS=>		M1ToZVczKGi{cx?=		NUjQPWVDS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hUEOFN{igZ4VtdHNiaHHyZo9zcW6pIGPMR\|M1STJvUl;TNUBie3Onc4Pl[EBieyC{ZXT1Z5Rqd25iaX6gZ4VtdCCycn;sbYZmemG2aX;uJIFnfGW{IEeyJIhzeyCkeTDNWHQh[XO\|YYmsJGlEPTBiPTCwMlAyQCEQvF2u	MYi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzR5NEmyOUc,Ojd2N{S5NlU9N2F-
KARPAS299	NHnJ[4ZEgXSxdH;4bYNqfHliYYPzZZk>		MWqyJJRwKDNiZHH5dy=>		Mn7hR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gT2FTWEGVMkm5JINmdGy\|IHHmeIVzKDJidH:gN{Bl[Xm\|IHL5JIx2[2moZYLhd4UhemWyb4L0[ZIh\2WwZTDhd5NigSxiSVO1NEA:KDBwMEKyPEDPxE1w	MX68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzd2MkK1Nkc,OjN5NEKyOVI9N2F-
KARPAS299	M1vsS2N6fG:2b4jpZ4l1gSCjc4PhfS=>				NXLoNHdqS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hU0GUUFHTNlk6KGOnbHzzJIV5eHKnc4PpcochVlCPLVHMT{BnfXOrb36g[4Vv\SCjc4Pld5Nm\CCjczDndo94fGhiaX7obYJqfGmxbjygTWM2OCB;IECuNFIzQCEQvF2u	M3XhbVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ\|OEO3O\|k4Lz5{M{izO\|c6PzxxYU6=
NCI-H3122	MVrGeY5kfGmxbjDhd5NigQ>?		NVf0PWNNPzJiaILz		NX3ycZFWUW6qaXLpeIlwdiCxZjDFUWw1KG[3c3XkJGFNUyCrbjDoeY1idiCQQ1mtTFMyOjJiY3XscJMh[XO\|ZYPz[YQh[XNiY3XscEBoem:5dHigbY5pcWKrdHnvckBu\WG\|dYLl[EBi\nSncjC3NkBpenNiYomgV3JDKGG\|c3H5MEBESzVyIE2gNE4xOjVizszNMi=>	M2nrOlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5OUG1NVY6Lz5{N{mxOVE3QTxxYU6=
BAF3	NV;pfYNoTnWwY4Tpc44h[XO\|YYm=		NWrhUmxOOiC2bzCzJIRigXN?		NFP6c\|RKdmirYnn0bY9vKG:oIF7QUU1nfXOnZDDBUGshMHWwa37ve44hd3KrZ3nuLUBmgHC{ZYPz[YQhcW5ibX;1d4UhSkGIMzDj[YxteyCjZoTldkAzKHSxIEOg[IF6eyCkeTDseYNq\mW{YYPlJJJmeG:{dHXyJIdmdmViYYPzZZktKEmFNUCgQUAxNjB{NjFOwG0v	NFTxbVU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{e0NlI2Oid-MkO3OFIzPTJ:L3G+
BA/F3	NGXJRVBEgXSxdH;4bYNqfHliYYPzZZk>				MYDDfZRwfG:6aXPpeJkh[WejaX7zeEBud3W\|ZTDCRU9HOyClZXzsd{BmgHC{ZYPzbY5oKE6STT3BUGsh\nW\|aX;uJIdmdmViYYPz[ZN{\WRiYYOg[5Jwf3SqIHnubIljcXSrb36sJGlEPTBiPTCwMlAzPiEQvF2u	NGeye2w9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{izO\|c6Pyd-MkO4N\|c4QTd:L3G+
KARPAS299	MVvBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>?		MXS3NkBpenN?		NELsc4FCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFvBVnBCWzJ7OTDj[YxteyCqYYLic5JqdmdiTmDNMWFNUyCjZoTldkA4OiCqcoOgZpkhVVSWIHHzd4F6NCCLQ{WwJF0hOC5yMk[g{txONg>?	NIHKS4E9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUG3OFgxQSd-MkmxO\|Q5ODl:L3G+
NCI-H2228	MVjBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>?		MX63NkBpenN?		MXHBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE6FST3INlIzQCClZXzsd{Bp[XKkb4LpcochTU2OND3BUGsh[W[2ZYKgO\|IhcHK\|IHL5JG1VXCCjc4PhfUwhUUN3MDC9JFAvODJ4IN88UU4>	NUnTbXg{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{CyNlMyOjBpPkOwNlI{OTJyPD;hQi=>
KARPAS299	MUjDfZRwfG:6aXPpeJkh[XO\|YYm=		M33ORVczKGi{cx?=		M1LmWWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGtCWlCDU{K5PUBk\WyuczDoZZJjd3KrbnegUnBONUGOSzDhd5Nme3OnZDDhd{Bz\WS3Y4Tpc44hcW5iY3XscEBxem:uaX\ldoF1cW:wIHHmeIVzKDd{IHjyd{BjgSCPVGSgZZN{[XluIFnDOVAhRSByLkCyO{DPxE1w	NHH1Xo89[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{S3OFkzPSd-Mke0O\|Q6OjV:L3G+
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SU-DHL1	NUTZRYpRTnWwY4Tpc44h[XO\|YYm=	NF:3VnozOCC2bzCyNFAhdk1?	MX:xJIhz		MVfJcohq[mm2aX;uJI9nKEGOSzDpckBpfW2jbjDTWU1FUExzIHPlcIx{KGG\|c3Xzd4VlKGG\|IILl[JVkfGmxbjDpckBGWkticHjvd5Bpd3K7bHH0bY9vKGG2IGSyNFIwN1l{MESgdoV{cWS3ZYOgZZQhOjBidH:gNlAxKG6PIHHmeIVzKDFiaIKgZpkhX2W\|dHXyckBjdG:2IHHuZYx6e2m\|	M4HFRVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7Mki4PVQxLz5{OUK4PFk1ODxxYU6=
NCI-H3122	MmPlSpVv[3Srb36gZZN{[Xl?	MmfnNlAhfG9iMkCwJI5O	M1nvfVEhcHJ?		NXvNXnRTUW6qaXLpeIlwdiCxZjDBUGsheGixc4Doc5J6dGG2aX;uJIF1KFlzMke4JJJme2mmdXWgbY4hcHWvYX6gUmNKNUh\|MUKyJINmdGy\|IHH0JFIxKHSxIEKwNEBvVSCjZoTldkAyKGi{IHL5JHdme3Sncn6gZoxwfCCjbnHsfZNqew>?	NIfT[VU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUK4PFk1OCd-MkmyPFg6PDB:L3G+
NCI-H3122	M1W1SGZ2dmO2aX;uJIF{e2G7	M17qXlIxKHSxIEKwNEBvVQ>?	MYCxJIhz		Ml[zTY5pcWKrdHnvckBw\iCDTFugbY4hcHWvYX6gUmNKNUh\|MUKyJINmdGy\|IHHzd4V{e2WmIHHzJJJm\HWldHnvckBqdiCVVFHUN{BxcG:\|cHjvdplt[XSrb36gZZQhYTdyNTDy[ZNq\HWnIHH0JFIxKHSxIEKwNEBvVSCjZoTldkAyKGi{IHL5JHdme3Sncn6gZoxwfCCjbnHsfZNqew>?	M4PGZ\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7Mki4PVQxLz5{OUK4PFk1ODxxYU6=
SU-DHL1	NG\ENG9HfW6ldHnvckBie3OjeR?=	MnviN\|Ahdk1?	MoXHNVYhcHK\|		NF\XOmdKdmirYnn0bY9vKG:oIFHMT{BifXSxcHjvd5Bpd3K7bHH0bY9vKGG2IGmxOVA4KHKnc3nkeYUhcW5iaIXtZY4hW1VvRFjMNUBk\WyuczDheEA{OCCwTTDh[pRmeiBzNjDodpMh[nliV3XzeIVzdiCkbH;0JIFv[Wy7c3nz	NUPhPGxoRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm2Nlc4OjVpPkK5OlI4PzJ3PD;hQi=>
SU-DHL1	NYG3U5hlTnWwY4Tpc44h[XO\|YYm=	NFrzflA{OCCwTR?=	MV6xOkBpenN?		Mlj6TY5pcWKrdHnvckBw\iCDTFugbY4hcHWvYX6gV3UuTEiOMTDj[YxteyCjc4Pld5Nm\CCjczDy[YR2[3Srb36gbY4hW1SDVEOgdIhwe3Cqb4L5cIF1cW:wIHH0JHk4ODVicnXzbYR2\SCjdDCzNEBvVSCjZoTldkAyPiCqcoOgZpkhX2W\|dHXyckBjdG:2IHHuZYx6e2m\|	MXq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTZ{N{eyOUc,Ojl4Mke3NlU9N2F-
NCI-H3122	MmnTSpVv[3Srb36gZZN{[Xl?	M2P4VVUxKHSxIEK1NEBvVQ>?	M4LRbVE3KGi{cx?=		Ml;RTY5lfWO2aX;uJI9nKEGOSzDk[Ydz[WSjdHnvckBqdiCqdX3hckBPS0lvSEOxNlIh[2WubIOgZZN{\XO\|ZXSgZZMh\GWlcnXhd4UhcW5iQVzLJJBpd3OyaH;yfYxifGmxbjDheEB[OTZyNDDheEA2OCC2bzCyOVAhdk1iYX\0[ZIhOTZiaILzJIJ6KGmvbYXuc4Jtd3RibXX0bI9l	M3LKXlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7Nk[wPVg1Lz5{OU[2NFk5PDxxYU6=
SH-SY5Y	MlL3RY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl?		NUSwV4RbPzJiaILz		MV\BcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFOKLWPZOXkh[2WubIOgZYZ1\XJiN{KgbJJ{KGK7IFPlcIxVcXSncj3HcI8hdHWvaX7ld4NmdnRiY3XscEB3cWGkaXzpeJkh[XO\|YYm=	M{fMclxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7Nk[wPVg1Lz5{OU[2NFk5PDxxYU6=
CHLA20	NX;ZdJRbSW62aYDyc4xq\mW{YYTpeoUh[XO\|YYm=		MoXXO\|IhcHK\|		NVn1emFPSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDDTGxCOjBiY3XscJMh[W[2ZYKgO\|IhcHK\|IHL5JGNmdGyWaYTldk1IdG9ibIXtbY5me2OnboSgZ4VtdCC4aXHibYxqfHliYYPzZZk>	MoPMQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl4NkC5PFQoRjJ7Nk[wPVg1RC:jPh?=
SH-SY5Y	NFfhSVdCdnSrcILvcIln\XKjdHn2[UBie3OjeR?=		NEDTZpo4OiCqcoO=		M1;NfGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iU1itV3k2YSClZXzsd{Bi\nSncjC3NkBpenNiaX6gdJJme2WwY3Wgc4YhSUKFQkGgbY5pcWKrdH;yJJRiemmzdXnkZZIh[nliQ3XscHRqfGW{LVfsc{BtfW2rbnXzZ4VvfCClZXzsJJZq[WKrbHn0fUBie3OjeR?=	M2PxelxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7Nk[wPVg1Lz5{OU[2NFk5PDxxYU6=
KARPAS299	NV:3bFNPTnWwY4Tpc44h[XO\|YYm=	MlLKOVAhfG9iMkWwJI5O	MUSxOkBpenN?		M2f0WGlv\HWldHnvckBw\iCDTFug[IVoemGmYYTpc44hcW5iaIXtZY4hU0GUUFHTNlk6KGOnbHzzJIF{e2W\|c3XkJIF{KGSnY4LlZZNmKGmwIFHMT{BxcG:\|cHjvdplt[XSrb36gZZQhYTF4MESgZZQhPTBidH:gNlUxKG6PIHHmeIVzKDF4IHjyd{BjgSCrbX31co9jdG:2IH3leIhw\A>?	MkHzQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl4NkC5PFQoRjJ7Nk[wPVg1RC:jPh?=
CHLA20	NYnj[ldySW62aYDyc4xq\mW{YYTpeoUh[XO\|YYm=		M{ezd\|czKGi{cx?=		NHnuN3lCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFPIUGEzOCClZXzsd{Bi\nSncjC3NkBpenNiaX6gdJJme2WwY3Wgc4YhSUKFQkGgbY5pcWKrdH;yJJRiemmzdXnkZZIh[nliQ3XscHRqfGW{LVfsc{BtfW2rbnXzZ4VvfCClZXzsJJZq[WKrbHn0fUBie3OjeR?=	NVroZmZKRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm2OlA6QDRpPkK5OlYxQTh2PD;hQi=>
NCI-H3122	MWLBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>?		MUi3NkBpenN?		M2XHU2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTlPJMWg{OTJ{IHPlcIx{KGGodHXyJFczKGi{czDifUBE\WyuVHn0[ZIuT2yxIHz1cYlv\XOlZX70JINmdGxidnnhZoltcXS7IHHzd4F6	MYe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTZ4MEm4OEc,Ojl4NkC5PFQ9N2F-
KARPAS299	Mn62RY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl?		Mkn0O\|IhcHK\|		MkD6RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6\|dDDoeY1idiCNQWLQRXMzQTliY3XscJMh[W[2ZYKgO\|IhcHK\|IHL5JGNmdGyWaYTldk1IdG9ibIXtbY5me2OnboSgZ4VtdCC4aXHibYxqfHliYYPzZZk>	M3vTW\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7Nk[wPVg1Lz5{OU[2NFk5PDxxYU6=
SU-DHL1	M4Ljc2FvfGmycn;sbYZmemG2aY\lJIF{e2G7		NEXTN2E4OiCqcoO=		NEmyfJVCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIGPVMWRJVDFiY3XscJMh[W[2ZYKgO\|IhcHK\|IHL5JGNmdGyWaYTldk1IdG9ibIXtbY5me2OnboSgZ4VtdCC4aXHibYxqfHliYYPzZZk>	NVvOPW46RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm2OlA6QDRpPkK5OlYxQTh2PD;hQi=>
KARPAS299	NW\zXo11SXCxcITvd4l{KGG\|c3H5	NIPkWY02OCCwTR?=	NGToNmYzPCCqcoO=		MYHJcoR2[3Srb36gc4Yh[XCxcITvd4l{KGmwIHj1cYFvKEuDUmDBV\|I6QSClZXzsd{Bie3Onc4Pl[EBieyC3bnPs[YFzKGOnbHygd4hzcW6tYXflJIF1KDVyIH7NJIFnfGW{IEK0JIhzeyCkeTDIc4VkcHO2IEOzNlU5KHO2YXnubY5oKGKjc3XkJIlvfmW{dHXkJIZtfW:{ZYPj[Y5k\SCvaXPyc5Nkd3C7	M3\GR\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyMkKzNVIxLz5\|MEKyN\|EzODxxYU6=
KARPAS299	MlSxRZBweHSxc3nzJIF{e2G7	NGq0V5Q2OCCwTR?=	NHjjVGYzPCCqcoO=		MlTyTY5lfWO2aX;uJI9nKGGyb4D0c5NqeyCrbjDoeY1idiCNQWLQRXMzQTliY3XscJMh[XO\|ZYPz[YQh[XNibHH0[UBieG:ydH;0bYMh[2WubIOgZZQhPTBibl2gZYZ1\XJiMkSgbJJ{KGK7IFHPM2VDKGSxdXLs[UB{fGGrbnnu[{Bj[XOnZDDpcpZmenSnZDDmcJVwemW\|Y3XuZ4UhdWmlcn;zZ49xgQ>?	NEfDe\|k9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9\|MEKyN\|EzOCd-M{CyNlMyOjB:L3G+
KARPAS299	MWjBdI9xfG:\|aYOgZZN{[Xl?	Ml3VOVAhdk1?	NWDuSZYyOjRiaILz		NEG3SZBKdmS3Y4Tpc44hd2ZiYYDvdJRwe2m\|IHnuJIh2dWGwIFvBVnBCWzJ7OTDj[YxteyCjc4Pld5Nm\CCjczDmdoFodWWwdHH0bY9vKGG2IEWwJI5OKGGodHXyJFI1KGi{czDifUBJd2WlaIP0JFM{OjV6IIP0ZYlvcW6pIHLhd4VlKGmwdnXyeIVlKG[udX;y[ZNk\W6lZTDtbYNzd3Olb4D5	NXm3OotvRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{CyNlMyOjBpPkOwNlI{OTJyPD;hQi=>

Click to View More Cell Line Experimental Data

Assay

Methods	Test Index	PMID

Western blot	p-ALK / ALK / p-AKT / AKT / p-ERK / ERK ; pROS1 / ROS1 / pSTAT3 / STAT3	28425916 25351743
Growth inhibition assay	Cell viability	29067644

In vivo

LDK378 is designed to reduce the possibility of forming reactive metabolites and shows undetectable levels of glutathione (GSH) adducts (<1%) in liver microsomes. LDK378 has relatively good metabolic stability, with moderate CYP3A4 (Midazolam substrate) inhibition and hERG inhibition. LDK378 exhibits low plasma clearance in animals (mouse, rat, dog and monkey) compared to liver blood flow, with the oral bioavailability of above 55% in mouse, rat, dog and monkey. LDK378 induces a dose-dependent growth inhibition and tumor regression in the Karpas299 and H2228 rat xenograft models, with no body-weight loss. LDK378 shows no impact on insulin levels or plasma glucose utilization in the mouse upon chronic dosing up to 100 mg/kg. ^[1]

Protocol (from reference)

Kinase Assay:^[1]	Enzymatic kinase profiling description: All kinases are expressed as either Histidine- or GST-tagged fusion proteins using the baculovirus expression technology except for the untagged ERK2 which is produced in E. coli. The kinase activity is measured in the LabChip mobility shift assay. The assay is performed at 30°C for 60 min. The effect of LDK378 on the enzymatic activity is obtained from the linear progress curves in the absence and presence of LDK378 and routinely determines from one reading (end point measurement)
Cell Research:^[1]	Cell lines: Ba/F3-NPM-ALK, Ba/F3-Tel-InsR, Ba/F3-WT, Karpas299 cells Concentrations: ~100 μM Incubation Time: 2-3 days Method: Luciferase-expressing cells are incubated with serial dilutions of LDK378 or DMSO for 2-3 days. Luciferase expression is used as a measure of cell proliferation/survival and is evaluated with the Bright-Glo Luciferase Assay System. IC50 values are generated by using XLFit software. (Only for Reference)
Animal Research:^[1]	Animal Models: RNU nude rats bearing the Karpas299/H2228 tumors Dosages: ~50 mg/kg Administration: Oral gavage (Only for Reference)

References

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

Solubility (25°C)

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

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

Chemical Information

Molecular Weight	558.14
Formula	C₂₈H₃₆ClN₅O₃S
CAS No.	1032900-25-6
Storage	3 years	-20°C	powder
Storage	2 years	-80°C	in solvent
Smiles	CC1=CC(=C(C=C1C2CCNCC2)OC(C)C)NC3=NC=C(C(=N3)NC4=CC=CC=C4S(=O)(=O)C(C)C)Cl

Download Ceritinib (LDK378) SDF

In vivo Formulation Calculator (Clear solution)

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

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

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

%DMSO+ %

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.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, 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.

Molarity Calculator

Dilution Calculator Molecular Weight Calculator

Clinical Trial Information

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

(data from https://clinicaltrials.gov, updated on 2022-01-17)

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.

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Frequently Asked Questions

Question 1:
how to reconstitute the inhibitor for oral administration to mice?

Answer:
You can resuspend LDK378 in 30% PEG400/0.5% Tween 80/5% propylene glycol and use the suspension for oral gavage feeding.

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