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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客户使用Selleck生产的Ceritinib (LDK378)发表文献64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) MmjmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWi3NkBp NUTxN5FZTE2VTx?= MlL0TWM2OD1zNUi2JOKyKDF5MzDuUS=> MW[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTd2OUCzOEc,OjV5NEmwN|Q9N2F-
WT 70 MoPBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2\PdVczKGh? MnjGSG1UVw>? M1rPd2lEPTB;MkGgxtEhQCCwTR?= M1y5S|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3N{S5NFM1Lz5{NUe0PVA{PDxxYU6=
G1128S 1022 Mk\JS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkfMO|IhcA>? MW\EUXNQ M{PTSGlEPTB;MUCyJOKyKDN6IH7N NFzrO5I9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUe0PVA{PCd-MkW3OFkxOzR:L3G+
C1156F 1293 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mom0O|IhcA>? Mk\OSG1UVw>? MoLFTWM2OD1{MUegxtEhOTF3IH7N MYK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTd2OUCzOEc,OjV5NEmwN|Q9N2F-
I1171N 519 M1GzSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUXFbXZtPzJiaB?= MnTpSG1UVw>? NX;XSlI4UUN3ME2xPFchyrFiOEegcm0> MnvzQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV5NEmwN|QoRjJ3N{S5NFM1RC:jPh?=
I1171T 445 NFG5dotIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUnwZ5RHPzJiaB?= NEDOdYpFVVOR NGPFPG9KSzVyPUiyJOKyKDF{IH7N Moi4QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV5NEmwN|QoRjJ3N{S5NFM1RC:jPh?=
F1174I 184 M3ewd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2L4XVczKGh? NWLNeoFKTE2VTx?= NEjWUmJKSzVyPUGzJOKyKDBwMTDuUS=> MXq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTd2OUCzOEc,OjV5NEmwN|Q9N2F-
N1178H 169 M4mwU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYK3NkBp MnfISG1UVw>? MVvJR|UxRTR{INMxJFYhdk1? MXq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTd2OUCzOEc,OjV5NEmwN|Q9N2F-
E1210K 748 NXvsOoZJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVm3NkBp NUC3cZB[TE2VTx?= M4LyPWlEPTB;MUi3JOKyKDh2IH7N MY[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTd2OUCzOEc,OjV5NEmwN|Q9N2F-
C1156F/D1203N 2809 MnXGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2O5XlczKGh? MVXEUXNQ MoTkTWM2OD1{NUSgxtEhQTlibl2= NVfNdGx{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW3OFkxOzRpPkK1O|Q6ODN2PD;hQi=>
Ba/F3 NA WT NIrUO2pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV[3NkBp M3LaRWlEPTB;MD6wNlAh|ryP NXfaWGhzRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW3Nlc1ODBpPkK1O|I4PDByPD;hQi=>
Ba/F3 NA C1156Y MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3PnSVczKGh? MnjOTWM2OD1yLkC3NUDPxE1? MYS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTd{N{SwNEc,OjV5Mke0NFA9N2F-
Ba/F3 NA L1196M NXXT[nZIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGXpeZk4OiCq M4npTmlEPTB;MD6wOFIh|ryP Mo\4QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV5Mke0NFAoRjJ3N{K3OFAxRC:jPh?=
Ba/F3 NA L1152R MorWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXS3NkBp MnHrTWM2OD1yLkK4PEDPxE1? MUW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTd{N{SwNEc,OjV5Mke0NFA9N2F-
Ba/F3 NA G1202R M{XqcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUK3NkBp MofaTWM2OD1yLkK3O{DPxE1? Mo\nQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV5Mke0NFAoRjJ3N{K3OFAxRC:jPh?=
Ba/F3 NA G1269A NUjBfmlST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIjLT204OiCq MWfJR|UxRTBwMEG5JO69VQ>? NWrtPWN3RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW3Nlc1ODBpPkK1O|I4PDByPD;hQi=>
Ba/F3 NA S1206Y M2jCN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGXvVY04OiCq MkHHTWM2OD1yLkCzO{DPxE1? Mm[wQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV5Mke0NFAoRjJ3N{K3OFAxRC:jPh?=
Ba/F3 EA WT MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEf5UYk4OiCq Mk\pTWM2OD1yLkCyNUDPxE1? NHHNeos9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUeyO|QxOCd-MkW3Nlc1ODB:L3G+
Ba/F3 EA C1156Y NFzEbYxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUHSXmppPzJiaB?= M2e0WmlEPTB;MD6wNlYh|ryP MYC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTd{N{SwNEc,OjV5Mke0NFA9N2F-
Ba/F3 EA L1196M NHPjb|VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NELDSZQ4OiCq MXnJR|UxRTBwMEG5JO69VQ>? MXy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTd{N{SwNEc,OjV5Mke0NFA9N2F-
Ba/F3 EA L1152R MlzyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2LLW|czKGh? MYrJR|UxRTBwMEm5JO69VQ>? NFHyWG49[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUeyO|QxOCd-MkW3Nlc1ODB:L3G+
Ba/F3 EA G1202R Ml;2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1fKcVczKGh? NUK5d5FqUUN3ME2wMlQ3PyEQvF2= MkjFQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV5Mke0NFAoRjJ3N{K3OFAxRC:jPh?=
Ba/F3 EA G1269A MkXBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1voW|czKGh? MXPJR|UxRTBwMEOzJO69VQ>? M1X3eVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3N{K3OFAxLz5{NUeyO|QxODxxYU6=
Ba/F3 EA S1206Y NIHWdGFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEPiWXo4OiCq MlzaTWM2OD1yLkCzPEDPxE1? MmLWQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV5Mke0NFAoRjJ3N{K3OFAxRC:jPh?=
BAF3 MXvBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? NXPa[494PzJiaILz MnLXRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDtc5V{\SCEQV[zJINmdGy|IHjhdoJwemmwZzDFUWw1NUGOSzDh[pRmeiB5MjDodpMh[nliU2LCJI9zKEOFS{igZZN{[XluIFnDOVAhRSByLkCxNFch|ryPLh?= MVS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTJ6OEm0NEc,Ojl{OEi5OFA9N2F-
NCI-H3122 MUTBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? MlXBO|IhcHK| MWjBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE6FST3IN|EzOiClZXzsd{Bi\nSncjC3NkBpenNiYomgR4VtdFSrdHXyMWdtdyCOdX3pcoV{[2WwdDDD[YxtKF[rYXLpcIl1gSCDc4PhfUwhTUN3MDC9JFAvODF3IN88UU4> MmjzQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ3NkiyPFkoRjJ4NU[4Nlg6RC:jPh?=
NCI-H2228 Mk\GS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M{ezSVMh\GG7cx?= MmrTS5Jwf3SqIHnubIljcXSrb36gc4YhcHWvYX6gUmNKNUh{MkK4JINmdGy|IHHmeIVzKDNiZHH5d{BjgSCudX3pcoV{[2WwY3WtZoF{\WRiQ3XscHRqfGW{LVfsc{Bie3OjeTygTWM2OCB;IECuNFE2KM7:TT6= M{XTV|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NkK3O|I2Lz5{OU[yO|czPTxxYU6=
SU-DHL1 MVHHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NVTOd41EOyCmYYnz NXTUVWR5T3Kxd4ToJIlvcGmkaYTpc44hd2ZiaIXtZY4hW1VvRFjMNUBk\WyuczDh[pRmeiB|IHThfZMh[nlibIXtbY5me2OnbnPlMYJie2WmIFPlcIxVcXSncj3HcI8h[XO|YYmsJGlEPTBiPTCwMlAyPSEQvF2u M2nlVlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NkK3O|I2Lz5{OU[yO|czPTxxYU6=
DFCI114 NGHFSY5CdnSrcILvcIln\XKjdHn2[UBie3OjeR?= NV;IcWJ5PzJiaILz NIDjOGJCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFTGR2kyOTRiY3XscJMh\XiycnXzd4lv\yCHTVy0MWFNUyCJMUK2PWEhdXW2YX70JIFnfGW{IEeyJIhzeyCkeTDD[YxtXGm2ZYKtS4xwKEy3bXnu[ZNk\W62IFPlcIwhXmmjYnnsbZR6KEG|c3H5MEBGSzVyIE2gNE4xOThizszNMi=> NITzVWU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkW2PFI5QSd-Mk[1OlgzQDl:L3G+
HCC78 M3LkeWN6fG:2b4jpZ4l1gSCjc4PhfS=> M4X2clczKGi{cx?= NHvJTIREgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBJS0N5ODDj[YxteyCqYYLic5JqdmdiU1zDN|RCOi2UT2OxJIF{e2W|c3XkJIF{KHKnZIXjeIlwdiCrbjDj[YxtKHC{b3zp[oVz[XSrb36gZYZ1\XJiN{KgbJJ{KGK7IF3UWEBie3OjeTygTWM2OCB;IECuNFE5KM7:TT6= NVK3eHlvRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMke0O|Q6OjVpPkK3OFc1QTJ3PD;hQi=>
KARPAS299 M37MNmN6fG:2b4jpZ4l1gSCjc4PhfS=> Mnf5NkB1dyB|IHThfZM> M{HCSGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGtCWlCDU{K5PUBk\WyuczDh[pRmeiB{IITvJFMh\GG7czDifUBtfWOrZnXyZZNmKHKncH;yeIVzKGenbnWgZZN{[XluIFnDOVAhRSByLkCyNlgh|ryPLh?= MXG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzd2MkK1Nkc,OjN5NEKyOVI9N2F-
KARPAS299 NFjkfItEgXSxdH;4bYNqfHliYYPzZZk> MVrDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDLRXJRSVN{OUmgZ4VtdHNiZYjwdoV{e2mwZzDOVG0uSUyNIH\1d4lwdiCpZX7lJIF{e2W|c3XkJIF{KGe{b4f0bEBqdmirYnn0bY9vNCCLQ{WwJF0hOC5yMkK4JO69VS5? MYC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzh|N{e5O{c,OjN6M{e3PVc9N2F-
NCI-H3122 NHfsfGZHfW6ldHnvckBie3OjeR?= NVr5S|BOPzJiaILz MV;Jcohq[mm2aX;uJI9nKEWPTESg[pV{\WRiQVzLJIlvKGi3bXHuJG5EUS2KM{GyNkBk\WyuczDhd5Nme3OnZDDhd{Bk\WyuIHfyc5d1cCCrbnjpZol1cW:wIH3lZZN2emWmIHHmeIVzKDd{IHjyd{BjgSCVUlKgZZN{[XluIFPDOVAhRSByLkCyOUDPxE1w MnjCQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjd7MUWxOlkoRjJ5OUG1NVY6RC:jPh?=
BAF3 M1nDVmZ2dmO2aX;uJIF{e2G7 NIjFPGYzKHSxIEOg[IF6ew>? Mlu4TY5pcWKrdHnvckBw\iCQUF2t[pV{\WRiQVzLJEh2dmuwb4fuJI9zcWerbjmg[ZhxemW|c3XkJIlvKG2xdYPlJGJCTjNiY3XscJMh[W[2ZYKgNkB1dyB|IHThfZMh[nlibIXjbYZmemG|ZTDy[ZBwenSncjDn[Y5mKGG|c3H5MEBKSzVyIE2gNE4xOjZizszNMi=> NUHZdokzRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO3OFIzPTJpPkKzO|QzOjV{PD;hQi=>
BA/F3 NEXEcYdEgXSxdH;4bYNqfHliYYPzZZk> M{DCcmN6fG:2b4jpZ4l1gSCjZ3HpcpN1KG2xdYPlJGJCN0Z|IHPlcIx{KGW6cILld5NqdmdiTmDNMWFNUyCodYPpc44h\2WwZTDhd5Nme3OnZDDhd{Boem:5dHigbY5pcWKrdHnvckwhUUN3MDC9JFAvODJ4IN88UU4> MXG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzh|N{e5O{c,OjN6M{e3PVc9N2F-
KARPAS299 MVHBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? Mn2xO|IhcHK| M4PVemFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iS1HSVGFUOjl7IHPlcIx{KGijcnLvdolv\yCQUF2tRWxMKGGodHXyJFczKGi{czDifUBOXFRiYYPzZZktKEmFNUCgQUAxNjB{NjFOwG0v MUS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTF5NEiwPUc,OjlzN{S4NFk9N2F-
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NCI-H3122 MVrGeY5kfGmxbjDhd5NigQ>? MUiyNEB1dyB{MECgcm0> M1rjOFEhcHJ? MoLkTY5pcWKrdHnvckBw\iCDTFugdIhwe3Cqb4L5cIF1cW:wIHH0JHkyOjd6IILld4llfWViaX6gbJVu[W5iTlPJMWg{OTJ{IHPlcIx{KGG2IEKwJJRwKDJyMDDuUUBi\nSncjCxJIhzKGK7IGfld5Rmem5iYnzveEBidmGueYPpdy=> MX:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTJ6OEm0NEc,Ojl{OEi5OFA9N2F-
NCI-H3122 MYLGeY5kfGmxbjDhd5NigQ>? NV;VVlFpOjBidH:gNlAxKG6P NXPTbXRyOSCqch?= MVTJcohq[mm2aX;uJI9nKEGOSzDpckBpfW2jbjDOR2kuUDNzMkKgZ4VtdHNiYYPz[ZN{\WRiYYOgdoVlfWO2aX;uJIlvKFOWQWSzJJBpd3OyaH;yfYxifGmxbjDheEB[PzB3IILld4llfWViYYSgNlAhfG9iMkCwJI5OKGGodHXyJFEhcHJiYomgW4V{fGW{bjDicI91KGGwYXz5d4l{ M2D3O|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7Mki4PVQxLz5{OUK4PFk1ODxxYU6=
SU-DHL1 MkSxSpVv[3Srb36gZZN{[Xl? MYGzNEBvVQ>? MlHpNVYhcHK| NYPlbm1CUW6qaXLpeIlwdiCxZjDBUGsh[XW2b4Doc5NxcG:{eXzheIlwdiCjdDDZNVUxPyC{ZYPp[JVmKGmwIHj1cYFvKFOXLVTIUFEh[2WubIOgZZQhOzBibl2gZYZ1\XJiMU[gbJJ{KGK7IGfld5Rmem5iYnzveEBidmGueYPpdy=> NUixVZpuRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm2Nlc4OjVpPkK5OlI4PzJ3PD;hQi=>
SU-DHL1 Mn3USpVv[3Srb36gZZN{[Xl? NWPySoVzOzBibl2= MVKxOkBpenN? NFPOS2VKdmirYnn0bY9vKG:oIFHMT{BqdiCqdX3hckBUXS2GSFyxJINmdGy|IHHzd4V{e2WmIHHzJJJm\HWldHnvckBqdiCVVFHUN{BxcG:|cHjvdplt[XSrb36gZZQhYTdyNTDy[ZNq\HWnIHH0JFMxKG6PIHHmeIVzKDF4IHjyd{BjgSCZZYP0[ZJvKGKub4SgZY5idHm|aYO= NX7JeolmRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm2Nlc4OjVpPkK5OlI4PzJ3PD;hQi=>
NCI-H3122 MX;GeY5kfGmxbjDhd5NigQ>? MoD6OVAhfG9iMkWwJI5O NHS5bnQyPiCqcoO= MlTkTY5lfWO2aX;uJI9nKEGOSzDk[Ydz[WSjdHnvckBqdiCqdX3hckBPS0lvSEOxNlIh[2WubIOgZZN{\XO|ZXSgZZMh\GWlcnXhd4UhcW5iQVzLJJBpd3OyaH;yfYxifGmxbjDheEB[OTZyNDDheEA2OCC2bzCyOVAhdk1iYX\0[ZIhOTZiaILzJIJ6KGmvbYXuc4Jtd3RibXX0bI9l M1e2ZlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7Nk[wPVg1Lz5{OU[2NFk5PDxxYU6=
SH-SY5Y MYPBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? NIjhboE4OiCqcoO= MWLBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFOKLWPZOXkh[2WubIOgZYZ1\XJiN{KgbJJ{KGK7IFPlcIxVcXSncj3HcI8hdHWvaX7ld4NmdnRiY3XscEB3cWGkaXzpeJkh[XO|YYm= MlTHQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl4NkC5PFQoRjJ7Nk[wPVg1RC:jPh?=
CHLA20 M3Lk[GFvfGmycn;sbYZmemG2aY\lJIF{e2G7 NUHKT2Z{PzJiaILz Ml7PRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCFSFzBNlAh[2WubIOgZYZ1\XJiN{KgbJJ{KGK7IFPlcIxVcXSncj3HcI8hdHWvaX7ld4NmdnRiY3XscEB3cWGkaXzpeJkh[XO|YYm= MnfqQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl4NkC5PFQoRjJ7Nk[wPVg1RC:jPh?=
SH-SY5Y M1TOfGFvfGmycn;sbYZmemG2aY\lJIF{e2G7 MXy3NkBpenN? M2CzbmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iU1itV3k2YSClZXzsd{Bi\nSncjC3NkBpenNiaX6gdJJme2WwY3Wgc4YhSUKFQkGgbY5pcWKrdH;yJJRiemmzdXnkZZIh[nliQ3XscHRqfGW{LVfsc{BtfW2rbnXzZ4VvfCClZXzsJJZq[WKrbHn0fUBie3OjeR?= NFnrUVI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OU[2NFk5PCd-Mkm2OlA6QDR:L3G+
KARPAS299 NGTHTYdHfW6ldHnvckBie3OjeR?= MYS1NEB1dyB{NUCgcm0> MWCxOkBpenN? NISyOIJKdmS3Y4Tpc44hd2ZiQVzLJIRm\3KjZHH0bY9vKGmwIHj1cYFvKEuDUmDBV|I6QSClZXzsd{Bie3Onc4Pl[EBieyCmZXPy[YF{\SCrbjDBUGsheGixc4Doc5J6dGG2aX;uJIF1KFlzNkC0JIF1KDVyIITvJFI2OCCwTTDh[pRmeiBzNjDodpMh[nliaX3teY5w[myxdDDt[ZRpd2R? M2T6[FxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7Nk[wPVg1Lz5{OU[2NFk5PDxxYU6=
CHLA20 NUn2ZmdFSW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= M2LGeVczKGi{cx?= MlTuRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCFSFzBNlAh[2WubIOgZYZ1\XJiN{KgbJJ{KGmwIIDy[ZNmdmOnIH;mJGFDS0JzIHnubIljcXSxcjD0ZZJqeXWrZHHyJIJ6KEOnbHzUbZRmei2JbH:gcJVucW6nc3PlcpQh[2WubDD2bYFjcWyrdImgZZN{[Xl? NU\sZW5nRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm2OlA6QDRpPkK5OlYxQTh2PD;hQi=>
NCI-H3122 MojORY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? MmLBO|IhcHK| Mn;CRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCQQ1mtTFMyOjJiY3XscJMh[W[2ZYKgO|IhcHK|IHL5JGNmdGyWaYTldk1IdG9ibIXtbY5me2OnboSgZ4VtdCC4aXHibYxqfHliYYPzZZk> NHrRb4U9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OU[2NFk5PCd-Mkm2OlA6QDR:L3G+
KARPAS299 NWrlNZBwSW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= M{joRlczKGi{cx?= M1ztcmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iS1HSVGFUOjl7IHPlcIx{KGGodHXyJFczKGi{czDifUBE\WyuVHn0[ZIuT2yxIHz1cYlv\XOlZX70JINmdGxidnnhZoltcXS7IHHzd4F6 NGXQe|M9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OU[2NFk5PCd-Mkm2OlA6QDR:L3G+
SU-DHL1 MkLyRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? MnywO|IhcHK| NHnLZW9CdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIGPVMWRJVDFiY3XscJMh[W[2ZYKgO|IhcHK|IHL5JGNmdGyWaYTldk1IdG9ibIXtbY5me2OnboSgZ4VtdCC4aXHibYxqfHliYYPzZZk> Mnf3QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl4NkC5PFQoRjJ7Nk[wPVg1RC:jPh?=
KARPAS299 MmnkRZBweHSxc3nzJIF{e2G7 MVu1NEBvVQ>? MoPMNlQhcHK| MUXJcoR2[3Srb36gc4Yh[XCxcITvd4l{KGmwIHj1cYFvKEuDUmDBV|I6QSClZXzsd{Bie3Onc4Pl[EBieyC3bnPs[YFzKGOnbHygd4hzcW6tYXflJIF1KDVyIH7NJIFnfGW{IEK0JIhzeyCkeTDIc4VkcHO2IEOzNlU5KHO2YXnubY5oKGKjc3XkJIlvfmW{dHXkJIZtfW:{ZYPj[Y5k\SCvaXPyc5Nkd3C7 NXL6TnNCRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{CyNlMyOjBpPkOwNlI{OTJyPD;hQi=>
KARPAS299 MWfBdI9xfG:|aYOgZZN{[Xl? MnPkOVAhdk1? NV;RSGhJOjRiaILz MlXuTY5lfWO2aX;uJI9nKGGyb4D0c5NqeyCrbjDoeY1idiCNQWLQRXMzQTliY3XscJMh[XO|ZYPz[YQh[XNibHH0[UBieG:ydH;0bYMh[2WubIOgZZQhPTBibl2gZYZ1\XJiMkSgbJJ{KGK7IFHPM2VDKGSxdXLs[UB{fGGrbnnu[{Bj[XOnZDDpcpZmenSnZDDmcJVwemW|Y3XuZ4UhdWmlcn;zZ49xgQ>? MofBQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzB{MkOxNlAoRjNyMkKzNVIxRC:jPh?=
KARPAS299 MlfsRZBweHSxc3nzJIF{e2G7 M1PSdlUxKG6P MVqyOEBpenN? Mk\mTY5lfWO2aX;uJI9nKGGyb4D0c5NqeyCrbjDoeY1idiCNQWLQRXMzQTliY3XscJMh[XO|ZYPz[YQh[XNiZoLh[41mdnSjdHnvckBifCB3MDDuUUBi\nSncjCyOEBpenNiYomgTI9m[2i|dDCzN|I2QCC|dHHpcolv\yCkYYPl[EBqdn[ncoTl[EBndHWxcnXzZ4Vv[2VibXnjdo9{[2:yeR?= NFfFVHU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEKyN|EzOCd-M{CyNlMyOjB:L3G+

... 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、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

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

  • 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

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID