Neratinib (HKI-272)

目录号:S2150 中文名称:来那替尼

仅限科研使用

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。

Neratinib (HKI-272) Chemical Structure

CAS: 698387-09-6

规格 价格 库存 购买数量
RMB 1227.96 现货
RMB 3863.92 现货
RMB 7933.43 现货
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客户使用Selleck生产的Neratinib (HKI-272)发表文献85篇:

产品安全说明书

HER2抑制剂选择性比较

相关HER2产品

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 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{nT[GlEPTB:MD6wNFUh|ryP MkLJQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjRyMEmwOlQoRjJ2MEC5NFY1RC:jPh?=
EFM-192A MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mm\MTWM2ODxyLkCwOUDPxE1? MV[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDByOUC2OEc,OjRyMEmwOlQ9N2F-
HCC1569 M1Ptcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWD1cZZFUUN3MEywMlAxPSEQvF2= MkLFQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjRyMEmwOlQoRjJ2MEC5NFY1RC:jPh?=
HCC1954 NFO4UYJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2HLbGlEPTB:MD6wNFUh|ryP NXL3SnRoRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSwNFkxPjRpPkK0NFA6ODZ2PD;hQi=>
MDA-MB-175 MlrvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MULJR|UxRDBwMEC1JO69VQ>? M1j5UVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MEC5NFY1Lz5{NECwPVA3PDxxYU6=
MDA-MB-361 NES1RnpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVHJR|UxRDBwMEC1JO69VQ>? MXq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDByOUC2OEc,OjRyMEmwOlQ9N2F-
SK-BR-3 MmrTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoXvTWM2ODxyLkCwOUDPxE1? MYG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDByOUC2OEc,OjRyMEmwOlQ9N2F-
UACC-812 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4XuTWlEPTB:MD6wNFUh|ryP NXzRZ4hHRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSwNFkxPjRpPkK0NFA6ODZ2PD;hQi=>
UACC-893 NXfjOGh4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmnaTWM2ODxyLkCwOUDPxE1? M2jLWFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MEC5NFY1Lz5{NECwPVA3PDxxYU6=
SUM-225 NYHCV4t3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NESxclVKSzVyPUCuNFEh|ryP MV:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDByOUC2OEc,OjRyMEmwOlQ9N2F-
SUM-190 MnfZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWDmWll7UUN3ME2wMlAyKM7:TR?= MmXUQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjRyMEmwOlQoRjJ2MEC5NFY1RC:jPh?=
ZR-75-1 M4f1R2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmHpTWM2OD1yLkCzJO69VQ>? M1XEWlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MEC5NFY1Lz5{NECwPVA3PDxxYU6=
HCC70 MoTzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1HwSmlEPTB;MD6wN{DPxE1? NGXWXmw9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NECwPVA3PCd-MkSwNFkxPjR:L3G+
BT-20 M{fJeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MY\JR|UxRTBwMEeg{txO MYm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDByOUC2OEc,OjRyMEmwOlQ9N2F-
MDA-MB-453 NXyxVGhIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYjuW5dWUUN3ME2wMlA6KM7:TR?= MWe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDByOUC2OEc,OjRyMEmwOlQ9N2F-
HCC1187 NUDmepNET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlLqTWM2OD1yLkGwJO69VQ>? NXzydYt4RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSwNFkxPjRpPkK0NFA6ODZ2PD;hQi=>
EFM-19 MmHXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWnWOXFYUUN3ME2wMlEyKM7:TR?= NYLpS5RuRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSwNFkxPjRpPkK0NFA6ODZ2PD;hQi=>
T-47D NV;NXllpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFOyWnBKSzVyPUCuNVYh|ryP MYS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDByOUC2OEc,OjRyMEmwOlQ9N2F-
MDA-MB-134 NWHjTFVLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH3Cb3FKSzVyPUCuNVch|ryP M3Tj[lxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MEC5NFY1Lz5{NECwPVA3PDxxYU6=
HCC38 MmSyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXrab45iUUN3ME2wMlI2KM7:TR?= NV\nW4NqRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSwNFkxPjRpPkK0NFA6ODZ2PD;hQi=>
MDA-MB-435 MnPsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{DzeWlEPTB;MD6zN{DPxE1? M3vwOlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MEC5NFY1Lz5{NECwPVA3PDxxYU6=
MDA-MB-468 M{LNSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH:2[ZRKSzVyPUCuN|Mh|ryP NHXnNGY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NECwPVA3PCd-MkSwNFkxPjR:L3G+
CAMA-1 NI\6bFdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXTJR|UxRTBwM{eg{txO NVPmbmVKRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSwNFkxPjRpPkK0NFA6ODZ2PD;hQi=>
MDA-MB-436 MnPYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUOweIo4UUN3ME2wMlQyKM7:TR?= MWC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDByOUC2OEc,OjRyMEmwOlQ9N2F-
MCF-7 NFXtfFNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHXkSGlKSzVyPUCuOFEh|ryP MnftQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjRyMEmwOlQoRjJ2MEC5NFY1RC:jPh?=
MDA-MB-415 M{DYSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYPJR|UxRTBwNEKg{txO MnvYQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjRyMEmwOlQoRjJ2MEC5NFY1RC:jPh?=
HCC1806 NUf5dYtzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUPJR|UxRTBwNESg{txO M1vh[|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MEC5NFY1Lz5{NECwPVA3PDxxYU6=
HCC1395 Mnu2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYDJR|UxRTBwNEmg{txO MmLlQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjRyMEmwOlQoRjJ2MEC5NFY1RC:jPh?=
HCC1937 NGHYd5VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn;hTWM2OD1yLkWwJO69VQ>? NEi4c5o9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NECwPVA3PCd-MkSwNFkxPjR:L3G+
HCC1143 Mk[0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYTJR|UxRTBwNUSg{txO NF\mWG49[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NECwPVA3PCd-MkSwNFkxPjR:L3G+
UACC-732 MnK3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEK0TG5KSzVyPUCuOlUh|ryP NHHCV5U9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NECwPVA3PCd-MkSwNFkxPjR:L3G+
MDA-MB-231 MnGyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4PzRWlEPTB;MT6wNEDPxE1? M2PsS|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MEC5NFY1Lz5{NECwPVA3PDxxYU6=
MDA-MB-157 NHj5VG1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnzuTWM2OD1zLkGyJO69VQ>? MlfmQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjRyMEmwOlQoRjJ2MEC5NFY1RC:jPh?=
BT-549 NHjsfYNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXvJR|UxRTFwMUSg{txO NVLQNYNsRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSwNFkxPjRpPkK0NFA6ODZ2PD;hQi=>
KPL-1 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH24OIpKSzVyPUGuPFkh|ryP NH7ZXHg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NECwPVA3PCd-MkSwNFkxPjR:L3G+
CAL-51 NFntN4VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M33uSWlEPTB;MT64PUDPxE1? NXHET45pRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSwNFkxPjRpPkK0NFA6ODZ2PD;hQi=>
BT474 MkXZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWDSNI9LUUN3ME2wMlAxOzJ|INMxJFAvODByN{Wg{txO NInKN|A9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{ixOlI2PCd-MkO4NVYzPTR:L3G+
SKBR3 MmHCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHrJbJFKSzVyPUCuNFA4PSEEsTCwMlAxPSEQvF2= NYHtR2Q4RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO4NVYzPTRpPkKzPFE3OjV2PD;hQi=>
MDAMB453 NXPBR2NPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2iyVWlEPTB;MT61PUDDuSByLkG3PUDPxE1? MVe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzhzNkK1OEc,OjN6MU[yOVQ9N2F-
KB M4PvSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4jaTWlEPTB;ND6xN{DDuSByLkS3JO69VQ>? M{H6bVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{NEmxPVM2Lz5{MkS5NVk{PTxxYU6=
KBv200 NVrCXZNPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mnj5TWM2OD14LkCzJOKyKDBwNkSg{txO NXXyOIVERGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkK0PVE6OzVpPkKyOFkyQTN3PD;hQi=>
MCF-7 M4e2d2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYDJR|UxRTNwM{CgxtEhOC52MTFOwG0> MnLWQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ2OUG5N|UoRjJ{NEmxPVM2RC:jPh?=
MCF-7/Adr MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MorYTWM2OD1iMj64PEDDuSByLkOwJO69VQ>? M3;wdVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{NEmxPVM2Lz5{MkS5NVk{PTxxYU6=
MCF-7 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3O5UmlEPTB;Mz6wNkDDuSByLkO0JO69VQ>? M3;XcFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{NEmxPVM2Lz5{MkS5NVk{PTxxYU6=
MCF-7/FLV1000 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkXmTWM2OD15LkC5JOKyKDBwN{Gg{txO NVf1XFlQRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkK0PVE6OzVpPkKyOFkyQTN3PD;hQi=>
HL60 NV[0eG5pT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{m4VWlEPTB;Mj6yOkDDuSByLkKzJO69VQ>? MUW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjR7MUmzOUc,OjJ2OUG5N|U9N2F-
HL60/Adr MkHmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH\B[XVKSzVyPUGuOFIhyrFiMD6xOUDPxE1? MXi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjR7MUmzOUc,OjJ2OUG5N|U9N2F-
HEK293/pcDNA3.1 MoToS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHu0cY9KSzVyPUWuNlkhyrFiMD61N{DPxE1? MXy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjR7MUmzOUc,OjJ2OUG5N|U9N2F-
HEK293/ABCB1 NGjzO|ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUjrN3VuUUN3ME22MlkyKMLzIECuO|AhKM7:TR?= M17SflxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{NEmxPVM2Lz5{MkS5NVk{PTxxYU6=
SKBR NGHtXJhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX:wMlAyNTFyMDDuUS=> NY[1O|IyOy15IHS= MXvpcohq[mm2czDj[YxtKGe{b4f0bEBqdiC2aX3lJIFv\CCmb4PlJIRmeGWwZHXueEBu[W6wZYK= MorFQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF2OEe2NFUoRjJzNEi3OlA2RC:jPh?=
L858R(EGFR) MWTD[YxtKF[rYXLpcIl1gSCDc4PhfS=> M2P5eIRm[3KnYYPld{Bk\WyuII\pZYJqdGm2eTDpckB1cW2nIHHu[EBld3OnIHTldIVv\GWwdDDtZY5v\XJ? MVS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yPzNzMUCwNkc,OTd|MUGwNFI9N2F-
L858R/T790M(EGFR) Mnm4R4VtdCCYaXHibYxqfHliQYPzZZk> M3nRV4Rm[3KnYYPld{Bk\WyuII\pZYJqdGm2eTDpckB1cW2nIHHu[EBld3OnIHTldIVv\GWwdDDtZY5v\XJ? MnjvQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTd|MUGwNFIoRjF5M{GxNFAzRC:jPh?=
G776insV_G/C M{KyXGNmdGxiVnnhZoltcXS7IFHzd4F6 Mn36[IVkemWjc3XzJINmdGxidnnhZoltcXS7IHnuJJRqdWViYX7kJIRwe2ViZHXw[Y5l\W62IH3hco5meg>? MVi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yPzNzMUCwNkc,OTd|MUGwNFI9N2F-
wild-type NHPNdFZE\WyuIG\pZYJqdGm2eTDBd5NigQ>? M4i5bIRm[3KnYYPld{Bk\WyuII\pZYJqdGm2eTDpckB1cW2nIHHu[EBld3OnIHTldIVv\GWwdDDtZY5v\XJ? M3f4[FxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF5M{GxNFAzLz5zN{OxNVAxOjxxYU6=
A775insYVMA MoDwR4VtdCCYaXHibYxqfHliQYPzZZk> MmP4[IVkemWjc3XzJINmdGxidnnhZoltcXS7IHnuJJRqdWViYX7kJIRwe2ViZHXw[Y5l\W62IH3hco5meg>? NEDuTmw9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zN{OxNVAxOid-MUezNVExODJ:L3G+
G776insV_G/L NIS4N4hE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NGnGUWJl\WO{ZXHz[ZMh[2WubDD2bYFjcWyrdImgbY4hfGmvZTDhcoQh\G:|ZTDk[ZBmdmSnboSgcYFvdmW{ Ml;3QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTd|MUGwNFIoRjF5M{GxNFAzRC:jPh?=
P780insGSP NGrtWHVE\WyuIG\pZYJqdGm2eTDBd5NigQ>? MlH6[IVkemWjc3XzJINmdGxidnnhZoltcXS7IHnuJJRqdWViYX7kJIRwe2ViZHXw[Y5l\W62IH3hco5meg>? MVm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yPzNzMUCwNkc,OTd|MUGwNFI9N2F-
NCI-H1781 NIT3d2dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlPmbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5idHnt[UBidmRiZH;z[UBl\XCnbnTlcpQhdWGwbnXy NUnSdXpwRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMU[4NVg3OThpPkG2PFE5PjF6PD;hQi=>
HCC827 M4jBWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlW0bY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5idHnt[UBidmRiZH;z[UBl\XCnbnTlcpQhdWGwbnXy MUC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yPjhzOE[xPEc,OTZ6MUi2NVg9N2F-
H3255 MkLMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MojObY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5idHnt[UBidmRiZH;z[UBl\XCnbnTlcpQhdWGwbnXy M1rr[|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF4OEG4OlE5Lz5zNkixPFYyQDxxYU6=
NCI-H1975 MkCzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MljnbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5idHnt[UBidmRiZH;z[UBl\XCnbnTlcpQhdWGwbnXy MnL0QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTZ6MUi2NVgoRjF4OEG4OlE5RC:jPh?=
A549 NX3qN3BbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGDLSHJqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjD0bY1mKGGwZDDkc5NmKGSncHXu[IVvfCCvYX7u[ZI> M33TW|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF4OEG4OlE5Lz5zNkixPFYyQDxxYU6=
3T3 NY\XfJBxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4TH[GlEPTB;N{CwJOKyKDd6IH7N M2TlWFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF3MUezNFA5Lz5zNUG3N|AxQDxxYU6=
3T3/neu MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWXJR|UxRTNiwsGgNE4yPCCwTR?= M1vJR|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF3MUezNFA5Lz5zNUG3N|AxQDxxYU6=
SK-Br-3 NXLaSlh{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NInDUo1KSzVyPUKgxtEhOC5zODDuUS=> MmTGQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTVzN{OwNFgoRjF3MUezNFA5RC:jPh?=
BT 474 M1LkSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkHJTWM2OD1{INMxJFAvODZibl2= NIqwd4M9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zNUG3N|AxQCd-MUWxO|MxODh:L3G+
A431 M1;sUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWnESVVlUUN3ME24NUDDuSB7IH7N NFXqNmk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zNUG3N|AxQCd-MUWxO|MxODh:L3G+
MDA-MB-435 Mm[zS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmnKTWM2OD17NkCgxtEhOTZ3IH7N Ml;zQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTVzN{OwNFgoRjF3MUezNFA5RC:jPh?=
SW620 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3PXVGlEPTB;NkmwJOKyKDh2IH7N MmjBQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTVzN{OwNFgoRjF3MUezNFA5RC:jPh?=
SKBR3 NWC3VJFjTnWwY4Tpc44h[XO|YYm= MlXoTY5pcWKrdHnvckBw\iCqdX3hckBJ\XJ{IHnuJHNMSlJ|IHPlcIx{NCCHQ{WwJF0hOC5yMEKg{txONg>? NILGTpU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOEC3O|QzPSd-MUiwO|c1OjV:L3G+
BT474 NF;oeJdHfW6ldHnvckBie3OjeR?= MULJcohq[mm2aX;uJI9nKGi3bXHuJGhmejJiaX6gRnQ1PzRiY3XscJMtKEWFNUCgQUAxNjByMjFOwG0v MnrVQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOThyN{e0NlUoRjF6MEe3OFI2RC:jPh?=
A431 NHXDN3JHfW6ldHnvckBie3OjeR?= NHrjSJhKdmirYnn0bY9vKG:oIHj1cYFvKEinckKgbY4hSTR|MTDj[YxteyxiRVO1NEA:KDBwMEixJO69VS5? M4DvZ|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF6MEe3OFI2Lz5zOEC3O|QzPTxxYU6=
SW620 NVfaNI9QTnWwY4Tpc44h[XO|YYm= NHrjfHZKdmirYnn0bY9vKG:oIHj1cYFvKEinckKgbY4hW1d4MkCgZ4VtdHNuIFXDOVAhRSByLk[5JO69VS5? NHLBbpY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOEC3O|QzPSd-MUiwO|c1OjV:L3G+
BA/F3 NUe1c4c3S3m2b4TvfIlkcXS7IHHzd4F6 NIjxOolEgXSxdH;4bYNqfHliYXfhbY5{fCCvb4Xz[UBDSS:IMzDj[YxteyCneIDy[ZN{cW6pIFXHSnIhVDh3OGKgcZV1[W62LDDJR|UxKD1iMD6wNFM2KM7:TT6= MWO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTJ|OUKyPUc,OTl{M{myNlk9N2F-
BA/F3 M3fU[GN6fG:2b4jpZ4l1gSCjc4PhfS=> MYnDfZRwfG:6aXPpeJkh[WejaX7zeEBud3W|ZTDCRU9HOyClZXzsd{BmgHC{ZYPzbY5oKEWJRmKgUFg2QFJxVEe5NG0hdXW2YX70MEBKSzVyIE2gNE4yQCEQvF2u M3\IWVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7MkO5NlI6Lz5zOUKzPVIzQTxxYU6=
Sf9 NHfMZZVHfW6ldHnvckBie3OjeR?= M3q2UVExKG2rboO= NXL4Z|RNUW6qaXLpeIlwdiCxZjDoeY1idiC5aXzkJJR6eGViRVfGVkBmgHC{ZYPz[YQhcW5iU3[5JINmdGy|IIXzbY5oKFupYX3tZVMzWF1vQWTQJIFnfGW{IEGwJI1qdnNiYomgd4NqdnSrbHzheIlwdiClb4XueIlv\yxiSVO1NEA:KDBwMECyOUDPxE1w MnzOQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR7MEC2OFMoRjJ2OUCwOlQ{RC:jPh?=
Sf9 NIPvNpJHfW6ldHnvckBie3OjeR?= NUPrRmFNOTBibXnudy=> NHnSPIVKdmirYnn0bY9vKG:oIHj1cYFvKEWJRmKgWFc6OE1xTEi1PHIhdXW2YX70JIV5eHKnc4Pl[EBqdiCVZkmgZ4VtdHNidYPpcochY2ejbX3hN|JRZS2DVGCgZYZ1\XJiMUCgcYlveyCkeTDzZ4lvfGmubHH0bY9vKGOxdX70bY5oNCCLQ{WwJF0hOC5yNk[g{txONg>? M1XNVlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2OUCwOlQ{Lz5{NEmwNFY1OzxxYU6=
BAF3 NFvvWohHfW6ldHnvckBie3OjeR?= MoHaO|IhcHK| NGqzdIhKdmirYnn0bY9vKG:oIGTlcE1nfXOnZDDJS2YyWiBqdX7rco94diCxcnnnbY4qKGW6cILld5Nm\CCrbjDtc5V{\SCEQV[zJINmdGy|IHHzd4V{e2WmIHHzJIdzd3e2aDDpcohq[mm2aX;uJIFnfGW{IEeyJIhzeyCkeTDD[YxtXGm2ZYKtS4xwKGG|c3H5MEBIUTVyIE2gNE4yQSEQvF2u MmG4QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh{OEKxNlIoRjJ6MkiyNVIzRC:jPh?=
BAF3 NGixSmtHfW6ldHnvckBie3OjeR?= M1LYclczKGi{cx?= NUfMV|RwUW6qaXLpeIlwdiCxZjDU[Ywu\nW|ZXSgTW5UWiBqdX7rco94diCxcnnnbY4qKGW6cILld5Nm\CCrbjDtc5V{\SCEQV[zJINmdGy|IHHzd4V{e2WmIHHzJIdzd3e2aDDpcohq[mm2aX;uJIFnfGW{IEeyJIhzeyCkeTDD[YxtXGm2ZYKtS4xwKGG|c3H5MEBIUTVyIE2gNE4zQSEQvF2u MWO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDJ6MkGyNkc,Ojh{OEKxNlI9N2F-
BAF3 M1HEUGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NG\Cd2k4OiCqcoO= MkHSS5Jwf3SqIHnubIljcXSrb36gc4YhdW:3c3WgRmFHOyClZXzsd{Bi\nSncjC3NkBpenNiYomgR4VtdFSrdHXyMWdtdyCjc4PhfUwhT0l3MDC9JFEvQSEQvF2u MUO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDJ6MkGyNkc,Ojh{OEKxNlI9N2F-
Assay
Methods Test Index PMID
Western blot pHER2 / HER2 / pAKT / AKT / pERK / ERK p-ERBB2 / ERBB2 / p-ERBB3 / ERBB3 / p-EGFR / p-90RSK 24009064 30118499
Growth inhibition assay Cell viability 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]
  • 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]
  • 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)。
动物实验:[1]
  • 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

溶解度(25°C)

体外

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 3年 -20°C 粉状
2年 -80°C 溶于溶剂

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)

mg/kg g μL

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
%DMSO %

计算结果:

工作液浓度: mg/ml;

DMSO母液配制方法: mg 药物溶于μL DMSO溶液(母液浓度mg/mL,:如该浓度超过该批次药物DMSO溶解度,请先联系Selleck);

体内配方配制方法:μL DMSO母液,加入μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入μL ddH2O,混匀澄清。

体内配方配制方法:μL DMSO母液,加入μL Corn oil,混匀澄清。

注意:1. 首先保证母液是澄清的;
2.一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。

摩尔浓度计算器

质量 浓度 体积 分子量

临床试验信息

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT05388149 Not yet recruiting Drug: Neratinib Breast Cancer|HER2-positive Breast Cancer University Health Network Toronto July 2022 Phase 2
NCT05252988 Not yet recruiting Drug: Neratinib|Drug: Loperamide|Drug: Colesevelam Early-stage Breast Cancer|HER2 Positive Breast Cancer|Hormone Receptor Positive Spanish Breast Cancer Research Group|Puma Biotechnology Inc.|Pierre Fabre Laboratories July 2022 Phase 2
NCT04856475 Withdrawn Drug: Neratinib Breast Cancer|Brain Metastases Jules Bordet Institute November 24 2021 Phase 2
NCT04781374 Terminated Drug: Neratinib Metastatic Prostate Adenocarcinoma|Castration-resistant Prostate Cancer|Prostate Cancer|Prostate Cancer Metastatic Dana-Farber Cancer Institute|Puma Biotechnology Inc. May 21 2021 Phase 2

(data from https://clinicaltrials.gov, updated on 2022-08-01)

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