Neratinib (HKI-272)

For research use only.

Catalog No.S2150

68 publications

Neratinib (HKI-272) Chemical Structure

CAS No. 698387-09-6

Neratinib (HKI-272) is a highly selective HER2 and EGFR inhibitor with IC50 of 59 nM and 92 nM in cell-free assays; weakly inhibits KDR and Src, no significant inhibition to Akt, CDK1/2/4, IKK-2, MK-2, PDK1, c-Raf and c-Met. Phase 3.

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Selleck's Neratinib (HKI-272) has been cited by 68 publications

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Choose Selective HER2 Inhibitors

Biological Activity

Description Neratinib (HKI-272) is a highly selective HER2 and EGFR inhibitor with IC50 of 59 nM and 92 nM in cell-free assays; weakly inhibits KDR and Src, no significant inhibition to Akt, CDK1/2/4, IKK-2, MK-2, PDK1, c-Raf and c-Met. Phase 3.
Targets
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
In vitro

Neratinib weakly inhibits tyrosine kinases KDR and Src with IC50 of 0.8 μM and 1.4 μM, respectively, being 14- and 24-fold less active compared with HER2. Neratinib displays no activity against other serine-threonine kinases such as Akt, cyclin D1/cdk4, cyclin E/cdk2, cyclin B1/cdk1, IKK-2, MK-2, PDK1, c-Raf, and Tpl-2, as well as the tyrosine kinase c-Met. Neratinib selectively inhibits the proliferation of 3T3 cells transfected with the HER2 (3T3/neu), as well as two other HER-2-overexpressing SK-Br-3 and BT474 cells with IC50 values of 2-3 nM, displaying >230-fold potency compared with non-transfected 3T3 cells as well as MDA-MB-435 and SW620 which are EGFR- and HER2-negative. Neratinib also inhibits the proliferation of EGFR-dependent A431 cells with an IC50 of 81 nM. Neratinib reduces HER2 receptor autophosphorylation in BT474 cells with an IC50 of 5 nM, and EGF-dependent phosphorylation of EGFR in A431 cells with IC50 of 3 nM. Blocking of HER-2 by Neratinib results in inhibition of downstream MAPK and Akt pathways with IC50 of 2 nM, more potently than Trastuzumab. Neratinib inhibits the cyclin D1 expression and the phosphorylation of the Rb-susceptibility gene production in BT474 cells with IC50 of 9 nM, leading to G1-S arrest and ultimately decreased cell proliferation. [1]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
BT-474 NVq2eVJpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkfDTWM2ODxyLkCwOUDPxE1? MUS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDByOUC2OEc,OjRyMEmwOlQ9N2F-
EFM-192A MnHSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFTtPGdKSzVyPECuNFA2KM7:TR?= NXTZfGpXRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSwNFkxPjRpPkK0NFA6ODZ2PD;hQi=>
HCC1569 M4qzd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXKyXWhqUUN3MEywMlAxPSEQvF2= MorJQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjRyMEmwOlQoRjJ2MEC5NFY1RC:jPh?=
HCC1954 NH\QO|VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH\yOVhKSzVyPECuNFA2KM7:TR?= M4CyTVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MEC5NFY1Lz5{NECwPVA3PDxxYU6=
MDA-MB-175 NXGzUYpST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYD4Tm5LUUN3MEywMlAxPSEQvF2= MUK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDByOUC2OEc,OjRyMEmwOlQ9N2F-
MDA-MB-361 M13WdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn60TWM2ODxyLkCwOUDPxE1? NHfWTIw9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NECwPVA3PCd-MkSwNFkxPjR:L3G+
SK-BR-3 NHPtVHNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1TxSmlEPTB:MD6wNFUh|ryP NFfDV4k9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NECwPVA3PCd-MkSwNFkxPjR:L3G+
UACC-812 MmmzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHz2WmFKSzVyPECuNFA2KM7:TR?= NY\VT5I{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSwNFkxPjRpPkK0NFA6ODZ2PD;hQi=>
UACC-893 M3Pob2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH\4Z5RKSzVyPECuNFA2KM7:TR?= NEG5Tlc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NECwPVA3PCd-MkSwNFkxPjR:L3G+
SUM-225 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXnFNFBNUUN3ME2wMlAyKM7:TR?= NVPFc41tRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSwNFkxPjRpPkK0NFA6ODZ2PD;hQi=>
SUM-190 MmLXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXLSbnJnUUN3ME2wMlAyKM7:TR?= NG\Wc3M9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NECwPVA3PCd-MkSwNFkxPjR:L3G+
ZR-75-1 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYPJR|UxRTBwMEOg{txO MWG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDByOUC2OEc,OjRyMEmwOlQ9N2F-
HCC70 NHrmUpNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYD5VYQzUUN3ME2wMlA{KM7:TR?= NFfhcoQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NECwPVA3PCd-MkSwNFkxPjR:L3G+
BT-20 M1\CdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mk\hTWM2OD1yLkC3JO69VQ>? M{ewUlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MEC5NFY1Lz5{NECwPVA3PDxxYU6=
MDA-MB-453 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV3NO2FDUUN3ME2wMlA6KM7:TR?= MoLJQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjRyMEmwOlQoRjJ2MEC5NFY1RC:jPh?=
HCC1187 M3;mfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1PJWWlEPTB;MD6xNEDPxE1? NUP3WIU2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSwNFkxPjRpPkK0NFA6ODZ2PD;hQi=>
EFM-19 NH\zTXJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXPIRYNyUUN3ME2wMlEyKM7:TR?= Ml;pQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjRyMEmwOlQoRjJ2MEC5NFY1RC:jPh?=
T-47D M3vse2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGH2NZVKSzVyPUCuNVYh|ryP NWXp[JF4RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSwNFkxPjRpPkK0NFA6ODZ2PD;hQi=>
MDA-MB-134 M2PVUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1\JTmlEPTB;MD6xO{DPxE1? Mn3jQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjRyMEmwOlQoRjJ2MEC5NFY1RC:jPh?=
HCC38 M2TKUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkHPTWM2OD1yLkK1JO69VQ>? M{D5elxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MEC5NFY1Lz5{NECwPVA3PDxxYU6=
MDA-MB-435 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUHUPIVkUUN3ME2wMlM{KM7:TR?= NYPGfJljRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSwNFkxPjRpPkK0NFA6ODZ2PD;hQi=>
MDA-MB-468 M3LWdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVHJR|UxRTBwM{Og{txO MnTpQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjRyMEmwOlQoRjJ2MEC5NFY1RC:jPh?=
CAMA-1 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX7aPFFGUUN3ME2wMlM4KM7:TR?= M4ri[|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MEC5NFY1Lz5{NECwPVA3PDxxYU6=
MDA-MB-436 NXfXb4oyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVTIU4dEUUN3ME2wMlQyKM7:TR?= MYm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDByOUC2OEc,OjRyMEmwOlQ9N2F-
MCF-7 M3ewcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUDJR|UxRTBwNEGg{txO M{ftNVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MEC5NFY1Lz5{NECwPVA3PDxxYU6=
MDA-MB-415 MoS2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVHJR|UxRTBwNEKg{txO M1m2fFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MEC5NFY1Lz5{NECwPVA3PDxxYU6=
HCC1806 NUjWb|R3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1zLb2lEPTB;MD60OEDPxE1? MXS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDByOUC2OEc,OjRyMEmwOlQ9N2F-
HCC1395 Mn;iS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHXOelRKSzVyPUCuOFkh|ryP M4CxcFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MEC5NFY1Lz5{NECwPVA3PDxxYU6=
HCC1937 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXywW2NHUUN3ME2wMlUxKM7:TR?= NHnq[Jk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NECwPVA3PCd-MkSwNFkxPjR:L3G+
HCC1143 M2TRWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH\rV4FKSzVyPUCuOVQh|ryP MYC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDByOUC2OEc,OjRyMEmwOlQ9N2F-
UACC-732 Mo\QS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn;0TWM2OD1yLk[1JO69VQ>? NVnYbHFERGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSwNFkxPjRpPkK0NFA6ODZ2PD;hQi=>
MDA-MB-231 M2jmb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnjQTWM2OD1zLkCwJO69VQ>? MmDZQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjRyMEmwOlQoRjJ2MEC5NFY1RC:jPh?=
MDA-MB-157 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGjxfIJKSzVyPUGuNVIh|ryP MoTKQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjRyMEmwOlQoRjJ2MEC5NFY1RC:jPh?=
BT-549 NH6wT5ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGfwNG5KSzVyPUGuNVQh|ryP NX\GdWc{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSwNFkxPjRpPkK0NFA6ODZ2PD;hQi=>
KPL-1 M1r5fGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFrYWZNKSzVyPUGuPFkh|ryP MnHIQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjRyMEmwOlQoRjJ2MEC5NFY1RC:jPh?=
CAL-51 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmPmTWM2OD1zLki5JO69VQ>? MnnKQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjRyMEmwOlQoRjJ2MEC5NFY1RC:jPh?=
BT474 MkDsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkHjTWM2OD1yLkCwN|I{KMLzIECuNFAxPzVizszN Ml\mQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN6MU[yOVQoRjJ|OEG2NlU1RC:jPh?=
SKBR3 NEH5W3BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVywO3A4UUN3ME2wMlAxPzViwsGgNE4xODVizszN M4jScFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|OEG2NlU1Lz5{M{ixOlI2PDxxYU6=
MDAMB453 NWK1ZoluT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVLJR|UxRTFwNUmgxtEhOC5zN{mg{txO NVuzeIpiRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO4NVYzPTRpPkKzPFE3OjV2PD;hQi=>
KB NFjoXYpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGPiUVRKSzVyPUSuNVMhyrFiMD60O{DPxE1? NEL0dYM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkS5NVk{PSd-MkK0PVE6OzV:L3G+
KBv200 Mor2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVXJR|UxRTZwMEOgxtEhOC54NDFOwG0> Mn;tQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ2OUG5N|UoRjJ{NEmxPVM2RC:jPh?=
MCF-7 NIXORYRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVnRV|k6UUN3ME2zMlMxKMLzIECuOFEh|ryP MXe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjR7MUmzOUc,OjJ2OUG5N|U9N2F-
MCF-7/Adr MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUHPZWtSUUN3ME2gNk45QCEEsTCwMlMxKM7:TR?= MkLPQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ2OUG5N|UoRjJ{NEmxPVM2RC:jPh?=
MCF-7 M1jwN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnHOTWM2OD1|LkCyJOKyKDBwM{Sg{txO MYW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjR7MUmzOUc,OjJ2OUG5N|U9N2F-
MCF-7/FLV1000 NEi3S|VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYe4UFl1UUN3ME23MlA6KMLzIECuO|Eh|ryP Mor2QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ2OUG5N|UoRjJ{NEmxPVM2RC:jPh?=
HL60 MnnsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV7uOoVGUUN3ME2yMlI3KMLzIECuNlMh|ryP MY[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjR7MUmzOUc,OjJ2OUG5N|U9N2F-
HL60/Adr MnPwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEfzeWtKSzVyPUGuOFIhyrFiMD6xOUDPxE1? MlHCQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ2OUG5N|UoRjJ{NEmxPVM2RC:jPh?=
HEK293/pcDNA3.1 M37EUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlXCTWM2OD13LkK5JOKyKDBwNUOg{txO M{L6O|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{NEmxPVM2Lz5{MkS5NVk{PTxxYU6=
HEK293/ABCB1 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mo\MTWM2OD14LkmxJOKyKDBwN{CgJO69VQ>? MVG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjR7MUmzOUc,OjJ2OUG5N|U9N2F-
SKBR MnriS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXHUZWNSOC5yMT2xNFAhdk1? NHTLNJk{NTdiZB?= MmHPbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5idHnt[UBidmRiZH;z[UBl\XCnbnTlcpQhdWGwbnXy NXnEPHVqRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkG0PFc3ODVpPkKxOFg4PjB3PD;hQi=>
L858R(EGFR) NXjRTY9JS2WubDDWbYFjcWyrdImgRZN{[Xl? MV7k[YNz\WG|ZYOgZ4VtdCC4aXHibYxqfHliaX6geIlu\SCjbnSg[I9{\SCmZYDlcoRmdnRibXHucoVz M3LENlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF5M{GxNFAzLz5zN{OxNVAxOjxxYU6=
L858R/T790M(EGFR) M4XybmNmdGxiVnnhZoltcXS7IFHzd4F6 NWLHb5dO\GWlcnXhd4V{KGOnbHygeoli[mmuaYT5JIlvKHSrbXWgZY5lKGSxc3Wg[IVx\W6mZX70JI1idm6nch?= M1nPWFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF5M{GxNFAzLz5zN{OxNVAxOjxxYU6=
G776insV_G/C M3rM[2NmdGxiVnnhZoltcXS7IFHzd4F6 NXrXeVBx\GWlcnXhd4V{KGOnbHygeoli[mmuaYT5JIlvKHSrbXWgZY5lKGSxc3Wg[IVx\W6mZX70JI1idm6nch?= MkTzQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTd|MUGwNFIoRjF5M{GxNFAzRC:jPh?=
wild-type NFTqPVdE\WyuIG\pZYJqdGm2eTDBd5NigQ>? M3;iVoRm[3KnYYPld{Bk\WyuII\pZYJqdGm2eTDpckB1cW2nIHHu[EBld3OnIHTldIVv\GWwdDDtZY5v\XJ? M3zxPFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF5M{GxNFAzLz5zN{OxNVAxOjxxYU6=
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G776insV_G/L MnexR4VtdCCYaXHibYxqfHliQYPzZZk> MVvk[YNz\WG|ZYOgZ4VtdCC4aXHibYxqfHliaX6geIlu\SCjbnSg[I9{\SCmZYDlcoRmdnRibXHucoVz MXO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yPzNzMUCwNkc,OTd|MUGwNFI9N2F-
P780insGSP MofVR4VtdCCYaXHibYxqfHliQYPzZZk> NXfwUIVX\GWlcnXhd4V{KGOnbHygeoli[mmuaYT5JIlvKHSrbXWgZY5lKGSxc3Wg[IVx\W6mZX70JI1idm6nch?= NWTpXoNORGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUezNVExODJpPkG3N|EyODB{PD;hQi=>
NCI-H1781 NES4U|NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlPmbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5idHnt[UBidmRiZH;z[UBl\XCnbnTlcpQhdWGwbnXy NHL3W5M9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zNkixPFYyQCd-MU[4NVg3OTh:L3G+
HCC827 M{W0Zmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXLpWldWcW6qaXLpeJMh[2WubDDndo94fGhiaX6geIlu\SCjbnSg[I9{\SCmZYDlcoRmdnRibXHucoVz M1\GRVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF4OEG4OlE5Lz5zNkixPFYyQDxxYU6=
H3255 NUXKVIxTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUTtXHVwcW6qaXLpeJMh[2WubDDndo94fGhiaX6geIlu\SCjbnSg[I9{\SCmZYDlcoRmdnRibXHucoVz NIH0WGM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zNkixPFYyQCd-MU[4NVg3OTh:L3G+
NCI-H1975 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXvpcohq[mm2czDj[YxtKGe{b4f0bEBqdiC2aX3lJIFv\CCmb4PlJIRmeGWwZHXueEBu[W6wZYK= NWq3S4RORGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMU[4NVg3OThpPkG2PFE5PjF6PD;hQi=>
A549 M2LNNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2O4XYlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIITpcYUh[W6mIHTvd4Uh\GWyZX7k[Y51KG2jbn7ldi=> NUPUfI5TRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMU[4NVg3OThpPkG2PFE5PjF6PD;hQi=>
3T3 Mn;kS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYWzUJM6UUN3ME23NFAhyrFiN{igcm0> MlvWQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTVzN{OwNFgoRjF3MUezNFA5RC:jPh?=
3T3/neu Mn2yS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXfoTHJpUUN3ME2zJOKyKDBwMUSgcm0> MYC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yPTF5M{CwPEc,OTVzN{OwNFg9N2F-
SK-Br-3 M3TPOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmPGTWM2OD1{INMxJFAvOThibl2= NGDnN|M9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zNUG3N|AxQCd-MUWxO|MxODh:L3G+
BT 474 NELkS4tIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1TNemlEPTB;MjFCtUAxNjB4IH7N M2PlPFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF3MUezNFA5Lz5zNUG3N|AxQDxxYU6=
A431 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEnIdo1KSzVyPUixJOKyKDlibl2= MYi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yPTF5M{CwPEc,OTVzN{OwNFg9N2F-
MDA-MB-435 M1nnS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUjJR|UxRTl4MDFCtUAyPjVibl2= MkCxQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTVzN{OwNFgoRjF3MUezNFA5RC:jPh?=
SW620 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXLuSY84UUN3ME22PVAhyrFiOESgcm0> NWOwOW1[RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUWxO|MxODhpPkG1NVc{ODB6PD;hQi=>
SKBR3 MoDSSpVv[3Srb36gZZN{[Xl? M{Lzc2lvcGmkaYTpc44hd2ZiaIXtZY4hUGW{MjDpckBUU0KUMzDj[YxteyxiRVO1NEA:KDBwMECyJO69VS5? M3PreVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF6MEe3OFI2Lz5zOEC3O|QzPTxxYU6=
BT474 MmLTSpVv[3Srb36gZZN{[Xl? NEniW2tKdmirYnn0bY9vKG:oIHj1cYFvKEinckKgbY4hSlR2N{SgZ4VtdHNuIFXDOVAhRSByLkCwNkDPxE1w NVf6UIFQRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUiwO|c1OjVpPkG4NFc4PDJ3PD;hQi=>
A431 NF\mdm9HfW6ldHnvckBie3OjeR?= NGH0fJdKdmirYnn0bY9vKG:oIHj1cYFvKEinckKgbY4hSTR|MTDj[YxteyxiRVO1NEA:KDBwMEixJO69VS5? NYf2[5pCRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUiwO|c1OjVpPkG4NFc4PDJ3PD;hQi=>
SW620 NE\QeGRHfW6ldHnvckBie3OjeR?= MVLJcohq[mm2aX;uJI9nKGi3bXHuJGhmejJiaX6gV3c3OjBiY3XscJMtKEWFNUCgQUAxNjZ7IN88UU4> M{fadlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF6MEe3OFI2Lz5zOEC3O|QzPTxxYU6=
BA/F3 NIn2OIREgXSxdH;4bYNqfHliYYPzZZk> NXj4XoZPS3m2b4TvfIlkcXS7IHHnZYlve3RibX;1d4UhSkFxRkOgZ4VtdHNiZYjwdoV{e2mwZzDFS2ZTKEx6NUjSJI12fGGwdDygTWM2OCB;IECuNFA{PSEQvF2u NFXDOG49[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUKzPVIzQSd-MUmyN|kzOjl:L3G+
BA/F3 NUjMVlZQS3m2b4TvfIlkcXS7IHHzd4F6 Mnn1R5l1d3SxeHnjbZR6KGGpYXnud5QhdW:3c3WgRmEwTjNiY3XscJMh\XiycnXzd4lv\yCHR1\SJGw5PTiUL2S3PVBOKG23dHHueEwhUUN3MDC9JFAvOThizszNMi=> NG\OZnQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUKzPVIzQSd-MUmyN|kzOjl:L3G+
Sf9 MmrmSpVv[3Srb36gZZN{[Xl? MYSxNEBucW6| MXHJcohq[mm2aX;uJI9nKGi3bXHuJJdqdGRidInw[UBGT0[UIHX4dJJme3OnZDDpckBU\jliY3XscJMhfXOrbnegX4didW2jM{LQYU1CXFBiYX\0[ZIhOTBibXnud{BjgSC|Y3nueIltdGG2aX;uJINwfW62aX7nMEBKSzVyIE2gNE4xODJ3IN88UU4> Ml;LQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR7MEC2OFMoRjJ2OUCwOlQ{RC:jPh?=
Sf9 M{TzRmZ2dmO2aX;uJIF{e2G7 NUTRfnd6OTBibXnudy=> NX\zdW5GUW6qaXLpeIlwdiCxZjDoeY1idiCHR1\SJHQ4QTCPL1y4OVhTKG23dHHueEBmgHC{ZYPz[YQhcW5iU3[5JINmdGy|IIXzbY5oKFupYX3tZVMzWF1vQWTQJIFnfGW{IEGwJI1qdnNiYomgd4NqdnSrbHzheIlwdiClb4XueIlv\yxiSVO1NEA:KDBwME[2JO69VS5? MYK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDlyME[0N{c,OjR7MEC2OFM9N2F-
BAF3 NGPXeHBHfW6ldHnvckBie3OjeR?= MUO3NkBpenN? MXrJcohq[mm2aX;uJI9nKFSnbD3meZNm\CCLR1[xVkApfW6tbn;3ckBwemmpaX6pJIV5eHKnc4Pl[EBqdiCvb4Xz[UBDSUZ|IHPlcIx{KGG|c3Xzd4VlKGG|IHfyc5d1cCCrbnjpZol1cW:wIHHmeIVzKDd{IHjyd{BjgSCFZXzsWIl1\XJvR3zvJIF{e2G7LDDHTVUxKD1iMD6xPUDPxE1w M1Tqd|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6MkiyNVIzLz5{OEK4NlEzOjxxYU6=
BAF3 M37pcWZ2dmO2aX;uJIF{e2G7 NW\PZ5N7PzJiaILz MVnJcohq[mm2aX;uJI9nKFSnbD3meZNm\CCLTmPSJEh2dmuwb4fuJI9zcWerbjmg[ZhxemW|c3XkJIlvKG2xdYPlJGJCTjNiY3XscJMh[XO|ZYPz[YQh[XNiZ4Lve5RpKGmwaHnibZRqd25iYX\0[ZIhPzJiaILzJIJ6KEOnbHzUbZRmei2JbH:gZZN{[XluIFfJOVAhRSByLkK5JO69VS5? M2KzWlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6MkiyNVIzLz5{OEK4NlEzOjxxYU6=
BAF3 MlrWS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M3TaU|czKGi{cx?= MWjHdo94fGhiaX7obYJqfGmxbjDv[kBud3W|ZTDCRWY{KGOnbHzzJIFnfGW{IEeyJIhzeyCkeTDD[YxtXGm2ZYKtS4xwKGG|c3H5MEBIUTVyIE2gNU46KM7:TT6= M1LZ[|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6MkiyNVIzLz5{OEK4NlEzOjxxYU6=

... 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
In vivo Oral administration of Neratinib significantly inhibits the growth of 3T3/neu xenografts, with inhibition of 34%, 53%, 98%, and 98% at dose of 10, 20, 40, and 80 mg/kg/day, respectively. Consistent with the inhibition of HER-2 phosphorylation by 84% within 1 hour of administration at 40 mg/kg/day, Neratinib inhibits the growth of BT474 xenografts by 70-82%, 67%, and 93% at dose of 5, 10, and 40 mg/kg/day, respectively. Neratinib is also effective against SK-OV-3 xenografts with inhibition of 31% and 85% at 5 and 60 mg/kg/day, respectively. Neratinib is less potent against EGFR-dependent A431 xenografts than HER-2-dependent tumors, with 32% and 44% inhibition at 5 and 20 mg/kg/day, respectively. Neratinib displays little activity against MCF-7 and MX-1 xenografts expressing low levels of HER-2 and EGFR, with only 28% inhibition at 80 mg/kg/day, suggesting that Neratinib has selective activity for cells expressing HER-2 or EGFR. [1]

Protocol

Kinase Assay:[1]
- Collapse

Cell-free autophosphorylation assay using time-resolved fluorometry:

Neratinib is prepared as 10 mg/mL stocks in DMSO and diluted in 25 mM HEPES (pH 7.5; 0.002 ng/mL-20 μg/mL). Purified recombinant COOH-terminal fragments of HER2 (amino acids 676-1255) or epidermal growth factor receptor (EGFR) (amino acids 645-1186) [diluted in 100 mM HEPES (pH 7.5) and 50% glycerol] is incubated with increasing concentrations of Neratinib in 4 mM HEPES (pH 7.5), 0.4 mM MnCl2, 20 μM sodium vanadate, and 0.2 mM DTT for 15 minutes at room temperature in 96-well ELISA plates. The kinase reaction is initiated by the addition of 40 μM ATP and 20 mM MgCl2 and allowed to proceed for 1 hour at room temperature. Plates are washed, and phosphorylation is detected using Europium-labeled anti-phospho-tyrosine antibodies (15 ng/well). After washing and enhancement steps, signal is detected using a Victor2 fluorescence reader (excitation wavelength 340 nm, emission wavelength 615 nm). The concentration of Neratinib that inhibits receptor phosphorylation by 50% (IC50) is calculated from inhibition curves.
Cell Research:[1]
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  • Cell lines: 3T3, 3T3/neu, A431, BT474, SK-Br-3, MDA-MB-435, and SW480
  • Concentrations: Dissolved in DMSO, final concentrations 0.5 ng/mL-5 μg/mL
  • Incubation Time: 2 or 6 days
  • Method: Cells are exposed to various concentrations of Neratinib for 2, or 6 days. Cell proliferation is determined using sulforhodamine B, a protein binding dye. Briefly, cells are fixed with 10% trichloroacetic acid and washed extensively with water. Cells are then stained with 0.1% sulforhodamine B and washed in 5% acetic acid. Protein-associated dye is solubilized in 10 mM Tris, and absorbance is measured at 450 nM. The concentration of Neratinib that inhibits cell proliferation by 50% (IC50) is determined from inhibition curves.
    (Only for Reference)
Animal Research:[1]
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  • Animal Models: Female athymic (nude) mice implanted s.c. with 3T3/neu, BT474, MCF-7, or SK-OV-3 cells
  • Dosages: ~80 mg/kg/day
  • Administration: Gavage
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 5 mg/mL warmed (8.97 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
30% PEG400+0.5% Tween80+5% propylene glycol
For best results, use promptly after mixing.
5 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 557.04
Formula

C30H29ClN6O3

CAS No. 698387-09-6
Storage powder
in solvent
Synonyms N/A
Smiles CCOC1=C(C=C2C(=C1)N=CC(=C2NC3=CC(=C(C=C3)OCC4=CC=CC=N4)Cl)C#N)NC(=O)C=CCN(C)C

In vivo Formulation Calculator (Clear solution)

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Dosage mg/kg Average weight of animals g Dosing volume per animal ul Number of animals
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    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):
Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04781374 Not yet recruiting Drug: Neratinib Metastatic Prostate Adenocarcinoma|Castration-resistant Prostate Cancer|Prostate Cancer|Prostate Cancer Metastatic Dana-Farber Cancer Institute|Puma Biotechnology Inc. August 2021 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
NCT01128842 Completed Drug: Neratinib|Drug: Capecitabine Advanced Malignant Solid Tumors Puma Biotechnology Inc. April 2010 Phase 1
NCT00878709 Completed Drug: neratinib|Other: placebo Breast Cancer Puma Biotechnology Inc. July 9 2009 Phase 3
NCT00814060 Completed Drug: neratinib Healthy Subjects Puma Biotechnology Inc. January 2009 Phase 1
NCT00741260 Completed Drug: Neratinib|Drug: Capecitabine Breast Cancer Puma Biotechnology Inc. December 9 2008 Phase 1|Phase 2

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

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HER2 Signaling Pathway Map

HER2 Inhibitors with Unique Features

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID