Neratinib (HKI-272)

For research use only. Not for use in humans.

目录号:S2150 中文名称:来那替尼

Neratinib (HKI-272) Chemical Structure

CAS No. 698387-09-6

Neratinib (HKI-272)是一种高度选择性的HER2EGFR抑制剂,在无细胞试验中IC50分别为59 nM 和 92 nM;微弱抑制KDR和Src,对Akt,CDK1/2/4,IKK-2,MK-2,PDK1,c-Raf和c-Met没有显著的抑制作用。Phase 3。

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RMB 7933.43 现货
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客户使用Selleck生产的Neratinib (HKI-272)发表文献67篇:

产品安全说明书

HER2抑制剂选择性比较

生物活性

产品描述 Neratinib (HKI-272)是一种高度选择性的HER2EGFR抑制剂,在无细胞试验中IC50分别为59 nM 和 92 nM;微弱抑制KDR和Src,对Akt,CDK1/2/4,IKK-2,MK-2,PDK1,c-Raf和c-Met没有显著的抑制作用。Phase 3。
靶点
HER2 [1]
(Cell-free assay)
EGFR [1]
(Cell-free assay)
KDR [1]
(Cell-free assay)
Src [1]
(Cell-free assay)
59 nM 92 nM 800 nM 1.4 μM
体外研究

Neratinib微弱抑制酪氨酸激酶KDR 和Src,IC50分别为0.8 μM 和 1.4 μM,与 HER-2相比,活性分别弱14和24倍。Neratinib 作用于其他丝-苏氨酸激酶如Akt, cyclin D1/cdk4, cyclin E/cdk2, cyclin B1/cdk1, IKK-2, MK-2, PDK1, c-Raf, 和Tpl-2,以及酪氨酸激酶c-Met没有活性。Neratinib选择性抑制转染 HER-2 (3T3/neu)的3T3细胞增殖,也抑制两种其他 HER-2-过表达的SK-Br-3和 BT474 cells细胞增殖,IC50为 2-3 nM,与未转染的3T3细胞及 EGFR-和 HER-2阴性的MDA-MB-435 和 SW620细胞相比,效果高230倍以上。Neratinib也抑制EGFR-依赖的A431细胞增殖,IC50为81 nM。Neratinib 作用于BT474 细胞,降低HER-2受体自磷酸化, IC50 为5 nM,作用于A431细胞,降低EGF依赖的 EGFR磷酸化,IC50 为3 nM。Neratinib抑制 HER-2,导致下游MAPK和Akt通路受抑制,IC50为2 nM,比Trastuzumab更有效。Neratinib 作用于BT474细胞,抑制cyclin D1表达和 Rb-敏感性基因产物的磷酸化,IC50为9 nM,导致细胞周期停在G1-S期,最终降低细胞增殖。[1]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
BT-474 NFPPd5JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Moq2TWM2ODxyLkCwOUDPxE1? Mo\WQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjRyMEmwOlQoRjJ2MEC5NFY1RC:jPh?=
EFM-192A NGDrUJZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF3TZmlKSzVyPECuNFA2KM7:TR?= NXj5VG16RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSwNFkxPjRpPkK0NFA6ODZ2PD;hQi=>
HCC1569 NXHMRY9vT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYC2TJpzUUN3MEywMlAxPSEQvF2= M1PNNlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MEC5NFY1Lz5{NECwPVA3PDxxYU6=
HCC1954 Ml7VS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1j6T2lEPTB:MD6wNFUh|ryP NFvpZpk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NECwPVA3PCd-MkSwNFkxPjR:L3G+
MDA-MB-175 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlfMTWM2ODxyLkCwOUDPxE1? M4fuV|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MEC5NFY1Lz5{NECwPVA3PDxxYU6=
MDA-MB-361 M3PaVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV35RpV5UUN3MEywMlAxPSEQvF2= NVfhZYs3RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSwNFkxPjRpPkK0NFA6ODZ2PD;hQi=>
SK-BR-3 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXHJR|UxRDBwMEC1JO69VQ>? M4flXFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MEC5NFY1Lz5{NECwPVA3PDxxYU6=
UACC-812 NFr4UnNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1mwVmlEPTB:MD6wNFUh|ryP MWi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDByOUC2OEc,OjRyMEmwOlQ9N2F-
UACC-893 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MojBTWM2ODxyLkCwOUDPxE1? M4nxbFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MEC5NFY1Lz5{NECwPVA3PDxxYU6=
SUM-225 M2\KOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MljrTWM2OD1yLkCxJO69VQ>? MXW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDByOUC2OEc,OjRyMEmwOlQ9N2F-
SUM-190 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkDUTWM2OD1yLkCxJO69VQ>? NFjzVGM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NECwPVA3PCd-MkSwNFkxPjR:L3G+
ZR-75-1 MnG3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX7kcXgxUUN3ME2wMlA{KM7:TR?= NGDORpk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NECwPVA3PCd-MkSwNFkxPjR:L3G+
HCC70 NFHaVmpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWjN[GZ3UUN3ME2wMlA{KM7:TR?= Mmi0QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjRyMEmwOlQoRjJ2MEC5NFY1RC:jPh?=
BT-20 NULadHRPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NED0So5KSzVyPUCuNFch|ryP M2mzZ|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MEC5NFY1Lz5{NECwPVA3PDxxYU6=
MDA-MB-453 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3zS[mlEPTB;MD6wPUDPxE1? M2nqUlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MEC5NFY1Lz5{NECwPVA3PDxxYU6=
HCC1187 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV;JR|UxRTBwMUCg{txO Mof3QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjRyMEmwOlQoRjJ2MEC5NFY1RC:jPh?=
EFM-19 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEHlfHhKSzVyPUCuNVEh|ryP NV7aWG9qRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSwNFkxPjRpPkK0NFA6ODZ2PD;hQi=>
T-47D MofTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{m3XmlEPTB;MD6xOkDPxE1? MmCyQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjRyMEmwOlQoRjJ2MEC5NFY1RC:jPh?=
MDA-MB-134 NUe3cFdsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVe3bnV4UUN3ME2wMlE4KM7:TR?= NHLW[|g9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NECwPVA3PCd-MkSwNFkxPjR:L3G+
HCC38 NYDzOnpLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEPMPVNKSzVyPUCuNlUh|ryP MXS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDByOUC2OEc,OjRyMEmwOlQ9N2F-
MDA-MB-435 MmnBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3TNfWlEPTB;MD6zN{DPxE1? M{nrbFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MEC5NFY1Lz5{NECwPVA3PDxxYU6=
MDA-MB-468 NHfWV|NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2LjbWlEPTB;MD6zN{DPxE1? NHH2UIM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NECwPVA3PCd-MkSwNFkxPjR:L3G+
CAMA-1 NXHnZ3hZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnrKTWM2OD1yLkO3JO69VQ>? MXu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDByOUC2OEc,OjRyMEmwOlQ9N2F-
MDA-MB-436 NH2wVJFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGXtS|hKSzVyPUCuOFEh|ryP NILwOWM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NECwPVA3PCd-MkSwNFkxPjR:L3G+
MCF-7 Mme2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NULyRYtDUUN3ME2wMlQyKM7:TR?= M{fmdlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MEC5NFY1Lz5{NECwPVA3PDxxYU6=
MDA-MB-415 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUjyZW9sUUN3ME2wMlQzKM7:TR?= M2XoblxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MEC5NFY1Lz5{NECwPVA3PDxxYU6=
HCC1806 NVPONZlxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVHJR|UxRTBwNESg{txO NFPzenc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NECwPVA3PCd-MkSwNFkxPjR:L3G+
HCC1395 NY[0NlQzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnW2TWM2OD1yLkS5JO69VQ>? NIrubIw9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NECwPVA3PCd-MkSwNFkxPjR:L3G+
HCC1937 MkL3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHvPS5BKSzVyPUCuOVAh|ryP NV3aOpkxRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSwNFkxPjRpPkK0NFA6ODZ2PD;hQi=>
HCC1143 NWHCUmdoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF7xc2pKSzVyPUCuOVQh|ryP NYXnSYloRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSwNFkxPjRpPkK0NFA6ODZ2PD;hQi=>
UACC-732 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYT5S4pjUUN3ME2wMlY2KM7:TR?= NGnIe3Q9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NECwPVA3PCd-MkSwNFkxPjR:L3G+
MDA-MB-231 M{X6TGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHzsbIlKSzVyPUGuNFAh|ryP MVm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDByOUC2OEc,OjRyMEmwOlQ9N2F-
MDA-MB-157 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MW\JR|UxRTFwMUKg{txO NHzqWIw9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NECwPVA3PCd-MkSwNFkxPjR:L3G+
BT-549 NH7Sd5VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3G5VmlEPTB;MT6xOEDPxE1? NHzpboc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NECwPVA3PCd-MkSwNFkxPjR:L3G+
KPL-1 Mki0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn;LTWM2OD1zLki5JO69VQ>? MnzGQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjRyMEmwOlQoRjJ2MEC5NFY1RC:jPh?=
CAL-51 NWT1fmlkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX;XOI13UUN3ME2xMlg6KM7:TR?= M{\FeVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MEC5NFY1Lz5{NECwPVA3PDxxYU6=
BT474 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmW1TWM2OD1yLkCwN|I{KMLzIECuNFAxPzVizszN M1\Od|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|OEG2NlU1Lz5{M{ixOlI2PDxxYU6=
SKBR3 NXH6bmg3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlzTTWM2OD1yLkCwO|UhyrFiMD6wNFUh|ryP NEXxXIg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{ixOlI2PCd-MkO4NVYzPTR:L3G+
MDAMB453 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIPWZZpKSzVyPUGuOVkhyrFiMD6xO|kh|ryP MlXhQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN6MU[yOVQoRjJ|OEG2NlU1RC:jPh?=
KB M37LSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnnKTWM2OD12LkGzJOKyKDBwNEeg{txO NGnINHo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkS5NVk{PSd-MkK0PVE6OzV:L3G+
KBv200 NF;NN3lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmLaTWM2OD14LkCzJOKyKDBwNkSg{txO MV[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjR7MUmzOUc,OjJ2OUG5N|U9N2F-
MCF-7 M4\LWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV62OnAxUUN3ME2zMlMxKMLzIECuOFEh|ryP NVnaVIFiRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkK0PVE6OzVpPkKyOFkyQTN3PD;hQi=>
MCF-7/Adr M3PZcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2fUSWlEPTB;IEKuPFghyrFiMD6zNEDPxE1? NFnmdHU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkS5NVk{PSd-MkK0PVE6OzV:L3G+
MCF-7 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF3qO25KSzVyPUOuNFIhyrFiMD6zOEDPxE1? M3W2N|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{NEmxPVM2Lz5{MkS5NVk{PTxxYU6=
MCF-7/FLV1000 NGfINFlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUXJR|UxRTdwMEmgxtEhOC55MTFOwG0> MWK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjR7MUmzOUc,OjJ2OUG5N|U9N2F-
HL60 NYPmVW5mT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFj5UphKSzVyPUKuNlYhyrFiMD6yN{DPxE1? MneyQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ2OUG5N|UoRjJ{NEmxPVM2RC:jPh?=
HL60/Adr MkDKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV\MTJJOUUN3ME2xMlQzKMLzIECuNVUh|ryP NWPWSYtxRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkK0PVE6OzVpPkKyOFkyQTN3PD;hQi=>
HEK293/pcDNA3.1 NGfvV|lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUHtdFE5UUN3ME21MlI6KMLzIECuOVMh|ryP NWjCR3Q2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkK0PVE6OzVpPkKyOFkyQTN3PD;hQi=>
HEK293/ABCB1 MojwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVTJR|UxRTZwOUGgxtEhOC55MDCg{txO NFXxO409[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkS5NVk{PSd-MkK0PVE6OzV:L3G+
SKBR M4HYO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYSwMlAyNTFyMDDuUS=> MUizMVch\A>? M3nRWolvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIITpcYUh[W6mIHTvd4Uh\GWyZX7k[Y51KG2jbn7ldi=> MWm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTR6N{[wOUc,OjF2OEe2NFU9N2F-
L858R(EGFR) MXfD[YxtKF[rYXLpcIl1gSCDc4PhfS=> MYLk[YNz\WG|ZYOgZ4VtdCC4aXHibYxqfHliaX6geIlu\SCjbnSg[I9{\SCmZYDlcoRmdnRibXHucoVz M{CzflxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF5M{GxNFAzLz5zN{OxNVAxOjxxYU6=
L858R/T790M(EGFR) MVfD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NG\6fo5l\WO{ZXHz[ZMh[2WubDD2bYFjcWyrdImgbY4hfGmvZTDhcoQh\G:|ZTDk[ZBmdmSnboSgcYFvdmW{ NV3VUFN4RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUezNVExODJpPkG3N|EyODB{PD;hQi=>
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wild-type MVnD[YxtKF[rYXLpcIl1gSCDc4PhfS=> M{WwfYRm[3KnYYPld{Bk\WyuII\pZYJqdGm2eTDpckB1cW2nIHHu[EBld3OnIHTldIVv\GWwdDDtZY5v\XJ? Ml64QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTd|MUGwNFIoRjF5M{GxNFAzRC:jPh?=
A775insYVMA M130[2NmdGxiVnnhZoltcXS7IFHzd4F6 MY\k[YNz\WG|ZYOgZ4VtdCC4aXHibYxqfHliaX6geIlu\SCjbnSg[I9{\SCmZYDlcoRmdnRibXHucoVz NFHGXnQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zN{OxNVAxOid-MUezNVExODJ:L3G+
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P780insGSP MX3D[YxtKF[rYXLpcIl1gSCDc4PhfS=> M{f5[4Rm[3KnYYPld{Bk\WyuII\pZYJqdGm2eTDpckB1cW2nIHHu[EBld3OnIHTldIVv\GWwdDDtZY5v\XJ? NYqydXpHRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUezNVExODJpPkG3N|EyODB{PD;hQi=>
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MDA-MB-435 Moi3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NE\PZXdKSzVyPUm2NEDDuSBzNkWgcm0> MV28ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yPTF5M{CwPEc,OTVzN{OwNFg9N2F-
SW620 NF;SW2RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1[3NGlEPTB;NkmwJOKyKDh2IH7N NX;WfGVTRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUWxO|MxODhpPkG1NVc{ODB6PD;hQi=>
SKBR3 NVv3[JQ3TnWwY4Tpc44h[XO|YYm= MVvJcohq[mm2aX;uJI9nKGi3bXHuJGhmejJiaX6gV2tDWjNiY3XscJMtKEWFNUCgQUAxNjByMjFOwG0v M1rkWFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF6MEe3OFI2Lz5zOEC3O|QzPTxxYU6=
BT474 MVfGeY5kfGmxbjDhd5NigQ>? NUf4epBTUW6qaXLpeIlwdiCxZjDoeY1idiCKZYKyJIlvKEKWNEe0JINmdGy|LDDFR|UxKD1iMD6wNFIh|ryPLh?= MlnqQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOThyN{e0NlUoRjF6MEe3OFI2RC:jPh?=
A431 M{HNcGZ2dmO2aX;uJIF{e2G7 NEnXS3ZKdmirYnn0bY9vKG:oIHj1cYFvKEinckKgbY4hSTR|MTDj[YxteyxiRVO1NEA:KDBwMEixJO69VS5? MWm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQDB5N{SyOUc,OThyN{e0NlU9N2F-
SW620 NXT1PWQ1TnWwY4Tpc44h[XO|YYm= MYjJcohq[mm2aX;uJI9nKGi3bXHuJGhmejJiaX6gV3c3OjBiY3XscJMtKEWFNUCgQUAxNjZ7IN88UU4> MXS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQDB5N{SyOUc,OThyN{e0NlU9N2F-
BA/F3 MkG2R5l1d3SxeHnjbZR6KGG|c3H5 NVWx[5FTS3m2b4TvfIlkcXS7IHHnZYlve3RibX;1d4UhSkFxRkOgZ4VtdHNiZYjwdoV{e2mwZzDFS2ZTKEx6NUjSJI12fGGwdDygTWM2OCB;IECuNFA{PSEQvF2u NFG0OZQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUKzPVIzQSd-MUmyN|kzOjl:L3G+
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Sf9 Mnq4SpVv[3Srb36gZZN{[Xl? MnL6NVAhdWmwcx?= MoXyTY5pcWKrdHnvckBw\iCqdX3hckB4cWymIIT5dIUhTUeIUjDlfJBz\XO|ZXSgbY4hW2Z7IHPlcIx{KHW|aX7nJHto[W2vYUOyVH0uSVSSIHHmeIVzKDFyIH3pcpMh[nlic3PpcpRqdGyjdHnvckBkd3WwdHnu[{whUUN3MDC9JFAvODB{NTFOwG0v Mnv1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR7MEC2OFMoRjJ2OUCwOlQ{RC:jPh?=
Sf9 NFO2TIdHfW6ldHnvckBie3OjeR?= MXuxNEBucW6| NX:3UIh[UW6qaXLpeIlwdiCxZjDoeY1idiCHR1\SJHQ4QTCPL1y4OVhTKG23dHHueEBmgHC{ZYPz[YQhcW5iU3[5JINmdGy|IIXzbY5oKFupYX3tZVMzWF1vQWTQJIFnfGW{IEGwJI1qdnNiYomgd4NqdnSrbHzheIlwdiClb4XueIlv\yxiSVO1NEA:KDBwME[2JO69VS5? NYHkepk{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS5NFA3PDNpPkK0PVAxPjR|PD;hQi=>
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BAF3 NYfqT4lxTnWwY4Tpc44h[XO|YYm= Mm\FO|IhcHK| NEHpPY9KdmirYnn0bY9vKG:oIGTlcE1nfXOnZDDJUnNTKCi3bnvuc5dvKG:{aXfpckkh\XiycnXzd4VlKGmwIH3veZNmKEKDRkOgZ4VtdHNiYYPz[ZN{\WRiYYOg[5Jwf3SqIHnubIljcXSrb36gZYZ1\XJiN{KgbJJ{KGK7IFPlcIxVcXSncj3HcI8h[XO|YYmsJGdKPTBiPTCwMlI6KM7:TT6= MluxQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh{OEKxNlIoRjJ6MkiyNVIzRC:jPh?=
BAF3 NVq3S3BDT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NIDpZo44OiCqcoO= NYTrZpI1T3Kxd4ToJIlvcGmkaYTpc44hd2ZibX;1d4UhSkGIMzDj[YxteyCjZoTldkA4OiCqcoOgZpkhS2WubGTpeIVzNUeubzDhd5NigSxiR1m1NEA:KDFwOTFOwG0v NGPzSVI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEK4NlEzOid-MkiyPFIyOjJ:L3G+

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
pHER2 / HER2 / pAKT / AKT / pERK / ERK ; 

PubMed: 24009064     


BT474 (right) and SKBR3 (left) cell were treated for 1 hour or 1 day with increasing concentrations of neratinib. After lysis, protein levels were assessed using western blotting techniques.

p-ERBB2 / ERBB2 / p-ERBB3 / ERBB3 / p-EGFR / p-90RSK ; 

PubMed: 30118499     


(A) Effects of MEK162 alone, neratinib alone, and the combination of MEK162 plus neratinib were assessed in sensitive, inflammatory subtype cell lines (NCI-H747, SW-837), (B) resistant, stem-like subtype cell lines (SW480, SW620). Cell lines were cultured䲧疝Ỵ疞㧀疜膉痘 瘿삨ՂᾰƌՂĀ 㺣痖帉痖Ѐ瑖堘𢡄빢᎒ՂĀ鑸᎒彿堙奋堙巫堙᎒ﻺ᎒彿堙ﻮ᎒塚堙ﻺ᎒ꍈ堞빢᎒學堙漸堞圔堙빢᎒圞堙圭堙𢡄玚Wᾰƌ ᾰƌ戤瘯Ɖ뙠ෆ䐺痖暼瘿뙠ෆᾰƌ 뙠ෆÐ㺣痖뙠ෆ€𢡄뙤ෆ€䀷痗뙤ෆ౴뙤ෆ㵶痗뙤ෆ뺖᎒泌Itemセ᎒

24009064 30118499
Growth inhibition assay
Cell viability ; 

PubMed: 30118499     


NCI-H747, SW837, SW1116, SW1463, NCI-H508, SNU-C1, SW480, SW620, C2BBE1, Hs675.T, and HCT116 cells were treated with a constant dose of MEK162 (0.5 μM) in combination with different doses of neratinib for 72 hours. Dimethyl sulfoxide (DMSO) (0.01%) was us䲧疝Ỵ疞㧀疜膉痘 瘿삨ՂᾰƌՂĀ 㺣痖帉痖Ѐ瑖堘𢡄빢᎒

30118499
体内研究 Neratinib每天按10, 20, 40, 和80 mg/kg剂量口服处理给药3T3/neu 移植瘤,显著抑制生长,分别抑制34%, 53%, 98%, 和 98%。Neratinib每天按40 mg/kg剂量处理,1小时内抑制 84% HER-2磷酸化,相应地,Neratinib 每天按5, 10, 和 40 mg/kg剂量处理BT474 移植瘤,抑制分别为70-82%, 67%, 和 93%。Neratinib也有效作用于SK-OV-3移植瘤,每天按 5 和 60 mg/kg剂量处理,抑制分别为 31% 和85% 。Neratinib作用于EGFR依赖性A431移植瘤比作用于HER-2-依赖性肿瘤效果弱, 每天按5 和 20 mg/kg剂量处理,抑制分别为32%和44%。Neratinib作用于表达低水平HER-2和EGFR的MCF-7和 MX-1移植瘤几乎没有活性, 每天按80 mg/kg剂量处理抑制只为28%,说明Neratinib 选择性作用于表达HER-2或EGFR的细胞。[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

使用时间-分辨荧光分析无细胞自磷酸化:

Neratinib 在DMSO 中制备成10 mg/mL 储液,然后在25 mM HEPES (pH 7.5; 0.002 ng/mL-20 μg/mL)中稀释。纯化重组的HER-2 COOH末端片段(第676-1255位氨基酸) 或EGFR COOH末端片段(第 645-1186位氨基酸)[在100 mM HEPES (pH 7.5) 和50% 甘油中稀释] 与浓度不断增高的Neratinib 在96-孔ELISA板上室温下温育15分钟,孔中含4 mM HEPES (pH 7.5), 0.4 mM MnCl2, 20 μM 钒酸钠,及 0.2 mM DTT 。加入 40 μM ATP 和20 mM MgCl2开始激酶反应,然后在室温下反应1小时。冲洗实验板, 使用铕标记的抗-磷酸化-酪氨酸抗体 (15 ng/每孔)检测磷酸化。冲洗后,使用Victor2 荧光读数仪 (激发波长为340 nm,发射波长为615 nm)测定信号。通过抑制曲线测定抑50%受体磷酸时的Neratinib 浓度 (IC50) 。
细胞实验:[1]
- 合并
  • Cell lines: 3T3, 3T3/neu, A431, BT474, SK-Br-3, MDA-MB-435, 和SW480
  • Concentrations: 溶于DMSO, 终浓度为0.5 ng/mL-5 μg/mL
  • Incubation Time: 2, 或6天
  • Method: 使用不同浓度Neratinib处理细胞 2, 或6 天。使用sulforhodamine B, 一种蛋白结合染料,测定细胞增殖。细胞与10% 三氯乙酸混合,然后使用水广泛冲洗。使用 0.1% sulforhodamine B对细胞进行染色,使用在5% 乙酸中清洗。蛋白-结合染10 mM Tris中,然后在450 nM处测定吸光度。通过抑制曲线测定抑制50% 细胞增殖时的Neratinib 浓度(IC50)。
    (Only for Reference)
动物实验:[1]
- 合并
  • Animal Models: 皮下移植3T3/neu, BT474, MCF-7, 或 SK-OV-3 细胞的雌性无胸腺裸鼠
  • Dosages: ~80 mg/kg/day
  • Administration: 口服饲喂
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 5 mg/mL warmed (8.97 mM)
Water Insoluble
Ethanol Insoluble
体内 从左到右依次将纯溶剂加入产品,现配现用(数据来自Selleck实验检测而非文献):
30% PEG400+0.5% Tween80+5% propylene glycol
5 mg/mL

* 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 557.04
化学式

C30H29ClN6O3

CAS号 698387-09-6
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
NCT04388384 Recruiting Drug: Neratinib Breast Neoplasm Pierre Fabre Pharma GmbH|iOMEDICO AG|Pierre Fabre Pharma Austria|Pierre Fabre Pharma AG April 20 2020 --
NCT03812393 Recruiting Drug: Neratinib Triple Negative Breast Cancer|Early-stage Breast Cancer|HER2-positive Breast Cancer West Cancer Center|Celcuity|Puma Biotechnology Inc. June 21 2019 Phase 2
NCT03919292 Recruiting Drug: Neratinib|Drug: Divalproex Sodium Solid Tumor Adult Virginia Commonwealth University|Puma Biotechnology Inc. May 1 2019 Phase 1|Phase 2
NCT03786107 Recruiting Diagnostic Test: Almac HER-Seq Assay Hormone Receptor-Positive HER2-Negative Metastatic Breast Cancer|Metastatic Cervical Cancer Puma Biotechnology Inc. March 14 2019 --

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。

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID