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70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) 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+
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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=>
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Ba/F3 NA C1156Y M{\temdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEi2PWI4OiCq Ml7ETWM2OD1yLkC3NUDPxE1? M4TsXFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3N{K3OFAxLz5{NUeyO|QxODxxYU6=
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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+
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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?=
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Ba/F3 EA S1206Y MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn\oO|IhcA>? MXLJR|UxRTBwMEO4JO69VQ>? MlHHQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV5Mke0NFAoRjJ3N{K3OFAxRC:jPh?=
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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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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=

... 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

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