Ceritinib (LDK378)

For research use only. Not for use in humans.

目录号:S7083

Ceritinib (LDK378) Chemical Structure

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-1RInsRSTK22DFLT3对应的IC50值分别为8 nM、7 nM、23 nM和60 nM。Phase 3。

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RMB 10720.71 现货
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客户使用Selleck生产的Ceritinib (LDK378)发表文献76篇:

产品安全说明书

ALK抑制剂选择性比较

生物活性

产品描述 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-1RInsRSTK22DFLT3对应的IC50值分别为8 nM、7 nM、23 nM和60 nM。Phase 3。
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) NWi1dndbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXK3NkBp NH\xb3ZFVVOR M2\pRmlEPTB;MUW4OkDDuSBzN{Ogcm0> M4DQVFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3N{S5NFM1Lz5{NUe0PVA{PDxxYU6=
WT 70 NILodZJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUXGbGRiPzJiaB?= MUjEUXNQ M3\icWlEPTB;MkGgxtEhQCCwTR?= MoTQQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV5NEmwN|QoRjJ3N{S5NFM1RC:jPh?=
G1128S 1022 NFrwZ2tIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M13qcFczKGh? NYTkWZdDTE2VTx?= M4CydGlEPTB;MUCyJOKyKDN6IH7N NIPmV4U9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUe0PVA{PCd-MkW3OFkxOzR:L3G+
C1156F 1293 M2\xc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkHUO|IhcA>? NEnrTFlFVVOR MmTCTWM2OD1{MUegxtEhOTF3IH7N NIXucYw9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUe0PVA{PCd-MkW3OFkxOzR:L3G+
I1171N 519 NYHjfodRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGD4coE4OiCq NF7QbVZFVVOR MnWwTWM2OD1zOEegxtEhQDdibl2= M2\ZTlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3N{S5NFM1Lz5{NUe0PVA{PDxxYU6=
I1171T 445 NVzvcWI{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1\oRVczKGh? NES2bFdFVVOR MVXJR|UxRTh{INMxJFEzKG6P MkfVQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV5NEmwN|QoRjJ3N{S5NFM1RC:jPh?=
F1174I 184 NUjO[nVOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2nC[VczKGh? MVnEUXNQ M2n1SGlEPTB;MUOgxtEhOC5zIH7N MoDjQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV5NEmwN|QoRjJ3N{S5NFM1RC:jPh?=
N1178H 169 NITme5RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEe4V3A4OiCq MX7EUXNQ MXLJR|UxRTR{INMxJFYhdk1? NGTsSYY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUe0PVA{PCd-MkW3OFkxOzR:L3G+
E1210K 748 NUK3bnAyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{CxV|czKGh? NIf3fZJFVVOR M{jLUmlEPTB;MUi3JOKyKDh2IH7N MWO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTd2OUCzOEc,OjV5NEmwN|Q9N2F-
C1156F/D1203N 2809 M4izc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYLxTFZHPzJiaB?= MXfEUXNQ NWr2S|ZLUUN3ME2yOVQhyrFiOUmgcm0> M1u1OVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3N{S5NFM1Lz5{NUe0PVA{PDxxYU6=
Ba/F3 NA WT M1v6Omdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4j6eVczKGh? NYTTT2VtUUN3ME2wMlAzOCEQvF2= MoLpQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV5Mke0NFAoRjJ3N{K3OFAxRC:jPh?=
Ba/F3 NA C1156Y MkXFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn\LO|IhcA>? M3;jNmlEPTB;MD6wO|Eh|ryP NH\ZSXY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUeyO|QxOCd-MkW3Nlc1ODB:L3G+
Ba/F3 NA L1196M Mk\XS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoHsO|IhcA>? MVrJR|UxRTBwMESyJO69VQ>? NWLTbHZTRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW3Nlc1ODBpPkK1O|I4PDByPD;hQi=>
Ba/F3 NA L1152R M3e3OWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1TvOVczKGh? NEPVU4pKSzVyPUCuNlg5KM7:TR?= NWWwTYNpRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW3Nlc1ODBpPkK1O|I4PDByPD;hQi=>
Ba/F3 NA G1202R MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml\zO|IhcA>? MmnLTWM2OD1yLkK3O{DPxE1? MXW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTd{N{SwNEc,OjV5Mke0NFA9N2F-
Ba/F3 NA G1269A MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Moi0O|IhcA>? MVzJR|UxRTBwMEG5JO69VQ>? MUO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTd{N{SwNEc,OjV5Mke0NFA9N2F-
Ba/F3 NA S1206Y Mo\LS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4Phc|czKGh? NUjtS5VYUUN3ME2wMlA{PyEQvF2= M1HsblxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3N{K3OFAxLz5{NUeyO|QxODxxYU6=
Ba/F3 EA WT MlXuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV\FS|JKPzJiaB?= MVHJR|UxRTBwMEKxJO69VQ>? MlvVQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV5Mke0NFAoRjJ3N{K3OFAxRC:jPh?=
Ba/F3 EA C1156Y MmO2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mli4O|IhcA>? M33Uc2lEPTB;MD6wNlYh|ryP NGT2PHg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUeyO|QxOCd-MkW3Nlc1ODB:L3G+
Ba/F3 EA L1196M NVHwRmR3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2Ll[|czKGh? Mn34TWM2OD1yLkCxPUDPxE1? M4XFN|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3N{K3OFAxLz5{NUeyO|QxODxxYU6=
Ba/F3 EA L1152R Mn7FS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUO3NkBp MnzrTWM2OD1yLkC5PUDPxE1? NEXJZmI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUeyO|QxOCd-MkW3Nlc1ODB:L3G+
Ba/F3 EA G1202R Mo\JS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NInKTmg4OiCq NEDte5NKSzVyPUCuOFY4KM7:TR?= NUfOO|V4RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW3Nlc1ODBpPkK1O|I4PDByPD;hQi=>
Ba/F3 EA G1269A NY\IOo8xT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFjhVZA4OiCq M37TNGlEPTB;MD6wN|Mh|ryP MlXxQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV5Mke0NFAoRjJ3N{K3OFAxRC:jPh?=
Ba/F3 EA S1206Y M2HvPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYjVPHU4PzJiaB?= NFz0OplKSzVyPUCuNFM5KM7:TR?= NVK3eotzRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW3Nlc1ODBpPkK1O|I4PDByPD;hQi=>
BAF3 M3TkZWFvfGmycn;sbYZmemG2aY\lJIF{e2G7 NYTRdI1mPzJiaILz MYfBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IH3veZNmKEKDRkOgZ4VtdHNiaHHyZo9zcW6pIFXNUFQuSUyNIHHmeIVzKDd{IHjyd{BjgSCVUlKgc5IhS0ONODDhd5NigSxiSVO1NEA:KDBwMEGwO{DPxE1w M2jRbVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7Mki4PVQxLz5{OUK4PFk1ODxxYU6=
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NCI-H2228 MYDHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MoLYN{Bl[Xm| MUDHdo94fGhiaX7obYJqfGmxbjDv[kBpfW2jbjDOR2kuUDJ{MkigZ4VtdHNiYX\0[ZIhOyCmYYnzJIJ6KGy3bXnu[ZNk\W6lZT3iZZNm\CCFZXzsWIl1\XJvR3zvJIF{e2G7LDDJR|UxKD1iMD6wNVUh|ryPLh?= MnT4QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl4Mke3NlUoRjJ7NkK3O|I2RC:jPh?=
SU-DHL1 MlT2S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MVOzJIRigXN? M2q4R2dzd3e2aDDpcohq[mm2aX;uJI9nKGi3bXHuJHNWNUSKTEGgZ4VtdHNiYX\0[ZIhOyCmYYnzJIJ6KGy3bXnu[ZNk\W6lZT3iZZNm\CCFZXzsWIl1\XJvR3zvJIF{e2G7LDDJR|UxKD1iMD6wNVUh|ryPLh?= M2jXXVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NkK3O|I2Lz5{OU[yO|czPTxxYU6=
DFCI114 M{jHTGFvfGmycn;sbYZmemG2aY\lJIF{e2G7 MXq3NkBpenN? NFrafYdCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFTGR2kyOTRiY3XscJMh\XiycnXzd4lv\yCHTVy0MWFNUyCJMUK2PWEhdXW2YX70JIFnfGW{IEeyJIhzeyCkeTDD[YxtXGm2ZYKtS4xwKEy3bXnu[ZNk\W62IFPlcIwhXmmjYnnsbZR6KEG|c3H5MEBGSzVyIE2gNE4xOThizszNMi=> MUe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjV4OEK4PUc,OjZ3NkiyPFk9N2F-
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KARPAS299 MkDxR5l1d3SxeHnjbZR6KGG|c3H5 M{LFZVIhfG9iMzDkZZl{ M4eybmN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGtCWlCDU{K5PUBk\WyuczDh[pRmeiB{IITvJFMh\GG7czDifUBtfWOrZnXyZZNmKHKncH;yeIVzKGenbnWgZZN{[XluIFnDOVAhRSByLkCyNlgh|ryPLh?= NUTRZVU6RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO3OFIzPTJpPkKzO|QzOjV{PD;hQi=>
KARPAS299 Ml\IR5l1d3SxeHnjbZR6KGG|c3H5 MknQR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gT2FTWEGVMkm5JINmdGy|IHX4dJJme3OrbnegUnBONUGOSzDmeZNqd25iZ3Xu[UBie3Onc4Pl[EBieyCpcn;3eIghcW6qaXLpeIlwdixiSVO1NEA:KDBwMEKyPEDPxE1w NYHmNHliRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO4N|c4QTdpPkKzPFM4Pzl5PD;hQi=>
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NCI-H3122 NHKwXXhHfW6ldHnvckBie3OjeR?= MkSwNlAhfG9iMkCwJI5O NW\JeZI2OSCqch?= NUXTU4d6UW6qaXLpeIlwdiCxZjDBUGsheGixc4Doc5J6dGG2aX;uJIF1KFlzMke4JJJme2mmdXWgbY4hcHWvYX6gUmNKNUh|MUKyJINmdGy|IHH0JFIxKHSxIEKwNEBvVSCjZoTldkAyKGi{IHL5JHdme3Sncn6gZoxwfCCjbnHsfZNqew>? NUfqS5ByRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkmyPFg6PDBpPkK5Nlg5QTRyPD;hQi=>
NCI-H3122 MUjGeY5kfGmxbjDhd5NigQ>? NGPtNnozOCC2bzCyNFAhdk1? MWixJIhz NXy4VopJUW6qaXLpeIlwdiCxZjDBUGshcW5iaIXtZY4hVkOLLVizNVIzKGOnbHzzJIF{e2W|c3XkJIF{KHKnZIXjeIlwdiCrbjDTWGFVOyCyaH;zdIhwenmuYYTpc44h[XRiWUewOUBz\XOrZIXlJIF1KDJyIITvJFIxOCCwTTDh[pRmeiBzIHjyJIJ6KFenc4Tldo4h[myxdDDhcoFtgXOrcx?= M{fOXVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7Mki4PVQxLz5{OUK4PFk1ODxxYU6=
SU-DHL1 NH;6W4JHfW6ldHnvckBie3OjeR?= MUSzNEBvVQ>? NW\3OoNkOTZiaILz NGG1WGZKdmirYnn0bY9vKG:oIFHMT{BifXSxcHjvd5Bpd3K7bHH0bY9vKGG2IGmxOVA4KHKnc3nkeYUhcW5iaIXtZY4hW1VvRFjMNUBk\WyuczDheEA{OCCwTTDh[pRmeiBzNjDodpMh[nliV3XzeIVzdiCkbH;0JIFv[Wy7c3nz NI\iXZc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OU[yO|czPSd-Mkm2Nlc4OjV:L3G+
SU-DHL1 MkPWSpVv[3Srb36gZZN{[Xl? NVnW[XpkOzBibl2= MnnSNVYhcHK| MkXsTY5pcWKrdHnvckBw\iCDTFugbY4hcHWvYX6gV3UuTEiOMTDj[YxteyCjc4Pld5Nm\CCjczDy[YR2[3Srb36gbY4hW1SDVEOgdIhwe3Cqb4L5cIF1cW:wIHH0JHk4ODVicnXzbYR2\SCjdDCzNEBvVSCjZoTldkAyPiCqcoOgZpkhX2W|dHXyckBjdG:2IHHuZYx6e2m| NGD4dms9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OU[yO|czPSd-Mkm2Nlc4OjV:L3G+
NCI-H3122 NX\QR|FGTnWwY4Tpc44h[XO|YYm= NGHy[|A2OCC2bzCyOVAhdk1? NYiyXHo6OTZiaILz NGDQNoVKdmS3Y4Tpc44hd2ZiQVzLJIRm\3KjZHH0bY9vKGmwIHj1cYFvKE6FST3IN|EzOiClZXzsd{Bie3Onc4Pl[EBieyCmZXPy[YF{\SCrbjDBUGsheGixc4Doc5J6dGG2aX;uJIF1KFlzNkC0JIF1KDVyIITvJFI2OCCwTTDh[pRmeiBzNjDodpMh[nliaX3teY5w[myxdDDt[ZRpd2R? M3;USFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7Nk[wPVg1Lz5{OU[2NFk5PDxxYU6=
SH-SY5Y MUTBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? M2\sVlczKGi{cx?= NXnsdVg2SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDTTE1UYTW\IHPlcIx{KGGodHXyJFczKGi{czDifUBE\WyuVHn0[ZIuT2yxIHz1cYlv\XOlZX70JINmdGxidnnhZoltcXS7IHHzd4F6 MYK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTZ4MEm4OEc,Ojl4NkC5PFQ9N2F-
CHLA20 NX7JNoVvSW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= NGTISXM4OiCqcoO= NYn2eIE4SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDDTGxCOjBiY3XscJMh[W[2ZYKgO|IhcHK|IHL5JGNmdGyWaYTldk1IdG9ibIXtbY5me2OnboSgZ4VtdCC4aXHibYxqfHliYYPzZZk> M1fQT|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7Nk[wPVg1Lz5{OU[2NFk5PDxxYU6=
SH-SY5Y M3rWZ2FvfGmycn;sbYZmemG2aY\lJIF{e2G7 M33IN|czKGi{cx?= MXrBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFOKLWPZOXkh[2WubIOgZYZ1\XJiN{KgbJJ{KGmwIIDy[ZNmdmOnIH;mJGFDS0JzIHnubIljcXSxcjD0ZZJqeXWrZHHyJIJ6KEOnbHzUbZRmei2JbH:gcJVucW6nc3PlcpQh[2WubDD2bYFjcWyrdImgZZN{[Xl? NXL6c202RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm2OlA6QDRpPkK5OlYxQTh2PD;hQi=>
KARPAS299 MY\GeY5kfGmxbjDhd5NigQ>? NXHXXmcxPTBidH:gNlUxKG6P NVvTNHZIOTZiaILz NWfmemc{UW6mdXP0bY9vKG:oIFHMT{Bl\We{YXTheIlwdiCrbjDoeY1idiCNQWLQRXMzQTliY3XscJMh[XO|ZYPz[YQh[XNiZHXjdoVie2ViaX6gRWxMKHCqb4PwbI9zgWyjdHnvckBifCC\MU[wOEBifCB3MDD0c{AzPTBibl2gZYZ1\XJiMU[gbJJ{KGK7IHntcZVvd2Kub4SgcYV1cG:m MkDvQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl4NkC5PFQoRjJ7Nk[wPVg1RC:jPh?=
CHLA20 M1[zRmFvfGmycn;sbYZmemG2aY\lJIF{e2G7 NEjWOmk4OiCqcoO= NIDjNoxCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFPIUGEzOCClZXzsd{Bi\nSncjC3NkBpenNiaX6gdJJme2WwY3Wgc4YhSUKFQkGgbY5pcWKrdH;yJJRiemmzdXnkZZIh[nliQ3XscHRqfGW{LVfsc{BtfW2rbnXzZ4VvfCClZXzsJJZq[WKrbHn0fUBie3OjeR?= MWq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTZ4MEm4OEc,Ojl4NkC5PFQ9N2F-
NCI-H3122 MorHRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? MVy3NkBpenN? M{XlfWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTlPJMWg{OTJ{IHPlcIx{KGGodHXyJFczKGi{czDifUBE\WyuVHn0[ZIuT2yxIHz1cYlv\XOlZX70JINmdGxidnnhZoltcXS7IHHzd4F6 MWS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTZ4MEm4OEc,Ojl4NkC5PFQ9N2F-
KARPAS299 M1r0VWFvfGmycn;sbYZmemG2aY\lJIF{e2G7 NGLXU5o4OiCqcoO= Mk\kRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCNQWLQRXMzQTliY3XscJMh[W[2ZYKgO|IhcHK|IHL5JGNmdGyWaYTldk1IdG9ibIXtbY5me2OnboSgZ4VtdCC4aXHibYxqfHliYYPzZZk> NIPWNGE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OU[2NFk5PCd-Mkm2OlA6QDR:L3G+
SU-DHL1 MY\BcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? NIK1WoY4OiCqcoO= M4e0[GFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iU2WtSGhNOSClZXzsd{Bi\nSncjC3NkBpenNiYomgR4VtdFSrdHXyMWdtdyCudX3pcoV{[2WwdDDj[YxtKH[rYXLpcIl1gSCjc4PhfS=> M3XFS|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7Nk[wPVg1Lz5{OU[2NFk5PDxxYU6=
KARPAS299 NF7DVHZCeG:ydH;zbZMh[XO|YYm= NIfMZpU2OCCwTR?= MVyyOEBpenN? MW\JcoR2[3Srb36gc4Yh[XCxcITvd4l{KGmwIHj1cYFvKEuDUmDBV|I6QSClZXzsd{Bie3Onc4Pl[EBieyC3bnPs[YFzKGOnbHygd4hzcW6tYXflJIF1KDVyIH7NJIFnfGW{IEK0JIhzeyCkeTDIc4VkcHO2IEOzNlU5KHO2YXnubY5oKGKjc3XkJIlvfmW{dHXkJIZtfW:{ZYPj[Y5k\SCvaXPyc5Nkd3C7 NXmwflhMRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{CyNlMyOjBpPkOwNlI{OTJyPD;hQi=>
KARPAS299 MlHmRZBweHSxc3nzJIF{e2G7 NX7Mc2htPTBibl2= MVWyOEBpenN? NYr3doh3UW6mdXP0bY9vKG:oIHHwc5B1d3OrczDpckBpfW2jbjDLRXJRSVN{OUmgZ4VtdHNiYYPz[ZN{\WRiYYOgcIF1\SCjcH;weI91cWNiY3XscJMh[XRiNUCgcm0h[W[2ZYKgNlQhcHK|IHL5JGFQN0WEIHTveYJt\SC|dHHpcolv\yCkYYPl[EBqdn[ncoTl[EBndHWxcnXzZ4Vv[2VibXnjdo9{[2:yeR?= Ml7SQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzB{MkOxNlAoRjNyMkKzNVIxRC:jPh?=
KARPAS299 MVrBdI9xfG:|aYOgZZN{[Xl? MmO4OVAhdk1? Ml\WNlQhcHK| NEPs[FNKdmS3Y4Tpc44hd2ZiYYDvdJRwe2m|IHnuJIh2dWGwIFvBVnBCWzJ7OTDj[YxteyCjc4Pld5Nm\CCjczDmdoFodWWwdHH0bY9vKGG2IEWwJI5OKGGodHXyJFI1KGi{czDifUBJd2WlaIP0JFM{OjV6IIP0ZYlvcW6pIHLhd4VlKGmwdnXyeIVlKG[udX;y[ZNk\W6lZTDtbYNzd3Olb4D5 M{fhV|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyMkKzNVIxLz5|MEKyN|EzODxxYU6=

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
p-ALK / ALK / p-AKT / AKT / p-ERK / ERK; 

PubMed: 28425916     


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     


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     


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]

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)

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)

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

分子量 558.14
化学式

C28H36ClN5O3S

CAS号 1032900-25-6
储存条件 粉状
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 g 每只动物给药体积 ul 动物数量
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

计算器

摩尔浓度计算器

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、SDS / 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

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、SDS / 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

  • 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

分子量计算器

通过输入化合物的化学式来计算其分子量:

总分子量:g/mol

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

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。

  • * 必填项

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

相关ALK产品

Tags: 购买Ceritinib (LDK378) | Ceritinib (LDK378)供应商 | 采购Ceritinib (LDK378) | Ceritinib (LDK378)价格 | Ceritinib (LDK378)生产 | 订购Ceritinib (LDK378) | Ceritinib (LDK378)代理商
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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID