Neratinib (HKI-272)

For research use only. Not for use in humans.

製品コードS2150

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.

サイズ

価格(税別)

5mg	JPY 26900
25mg	JPY 80000
100mg	JPY 163000

最寄りの販売代理店を探す

東京
北海道
東北
北関東
南関東
東海
北信越
近畿
中国
四国
九州

お探しのディーラーが見当たらない場合は直接こちらのメールアドレスまでお問い合わせください：[email protected]

バルク問合せ

代表番号: 03-5615-9297 | 電子メール：[email protected]

文献中Selleckの製品使用例(67)

製品安全説明書

HER2阻害剤の選択性比較

生物活性

製品説明

ターゲット

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

体外試験

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]

細胞データ

Cell Lines	Assay Type	Concentration	Incubation Time	Activity Description	PMID
BT-474	MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?			NYjsfHo1UUN3MEywMlAxPSEQvF2=	MVW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDByOUC2OEc,OjRyMEmwOlQ9N2F-
EFM-192A	NEjSRXlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=			NIXIU2dKSzVyPECuNFA2KM7:TR?=	MnfnQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjRyMEmwOlQoRjJ2MEC5NFY1RC:jPh?=
HCC1569	M{SzWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7			MYXJR\|UxRDBwMEC1JO69VQ>?	M1jnVFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MEC5NFY1Lz5{NECwPVA3PDxxYU6=
HCC1954	NU\ueZo5T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=			NELvWmlKSzVyPECuNFA2KM7:TR?=	MlTUQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjRyMEmwOlQoRjJ2MEC5NFY1RC:jPh?=
MDA-MB-175	MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?			NH;ST5NKSzVyPECuNFA2KM7:TR?=	NEf0[2w9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NECwPVA3PCd-MkSwNFkxPjR:L3G+
MDA-MB-361	MoLZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?			MXXJR\|UxRDBwMEC1JO69VQ>?	NIHBSVc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NECwPVA3PCd-MkSwNFkxPjR:L3G+
SK-BR-3	M4Lm[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7			MYHJR\|UxRDBwMEC1JO69VQ>?	NYPFUnJRRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSwNFkxPjRpPkK0NFA6ODZ2PD;hQi=>
UACC-812	M1rMR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7			MXXJR\|UxRDBwMEC1JO69VQ>?	MVy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDByOUC2OEc,OjRyMEmwOlQ9N2F-
UACC-893	NWS0W\|U6T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=			NV[wZ2Z2UUN3MEywMlAxPSEQvF2=	NUnwfoc2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSwNFkxPjRpPkK0NFA6ODZ2PD;hQi=>
SUM-225	NEjYXGVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=			NV\KcVZ2UUN3ME2wMlAyKM7:TR?=	M3[wdlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MEC5NFY1Lz5{NECwPVA3PDxxYU6=
SUM-190	M1XBdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7			NY\TRWV6UUN3ME2wMlAyKM7:TR?=	MV[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDByOUC2OEc,OjRyMEmwOlQ9N2F-
ZR-75-1	NV[1SItjT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=			M{TNcmlEPTB;MD6wN{DPxE1?	Ml:4QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjRyMEmwOlQoRjJ2MEC5NFY1RC:jPh?=
HCC70	NH3afYZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=			MojQTWM2OD1yLkCzJO69VQ>?	NVXHNG1yRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSwNFkxPjRpPkK0NFA6ODZ2PD;hQi=>
BT-20	MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?			MkDnTWM2OD1yLkC3JO69VQ>?	MkjkQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjRyMEmwOlQoRjJ2MEC5NFY1RC:jPh?=
MDA-MB-453	MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?			NIPzeFBKSzVyPUCuNFkh\|ryP	M3vr[lxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MEC5NFY1Lz5{NECwPVA3PDxxYU6=
HCC1187	M2XHXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7			MWXJR\|UxRTBwMUCg{txO	MYe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDByOUC2OEc,OjRyMEmwOlQ9N2F-
EFM-19	MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?			NHHveYJKSzVyPUCuNVEh\|ryP	NELNfYw9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NECwPVA3PCd-MkSwNFkxPjR:L3G+
T-47D	NX3YZY1OT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=			MUXJR\|UxRTBwMU[g{txO	MofJQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjRyMEmwOlQoRjJ2MEC5NFY1RC:jPh?=
MDA-MB-134	MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?			NWLVfXZkUUN3ME2wMlE4KM7:TR?=	M{SzeFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MEC5NFY1Lz5{NECwPVA3PDxxYU6=
HCC38	NHT0V\|ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=			NITqO\|BKSzVyPUCuNlUh\|ryP	MYi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDByOUC2OEc,OjRyMEmwOlQ9N2F-
MDA-MB-435	NGm1T5dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=			MWrJR\|UxRTBwM{Og{txO	NIm4[JU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NECwPVA3PCd-MkSwNFkxPjR:L3G+
MDA-MB-468	NF;SOIpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=			MojVTWM2OD1yLkOzJO69VQ>?	MWe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDByOUC2OEc,OjRyMEmwOlQ9N2F-
CAMA-1	NGrJdnZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=			NILGdHZKSzVyPUCuN\|ch\|ryP	NUTScpkxRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSwNFkxPjRpPkK0NFA6ODZ2PD;hQi=>
MDA-MB-436	NYr1fnE4T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=			Mn;aTWM2OD1yLkSxJO69VQ>?	NHX1OIw9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NECwPVA3PCd-MkSwNFkxPjR:L3G+
MCF-7	NYrtSYw5T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=			NFewPW1KSzVyPUCuOFEh\|ryP	M3vVdlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MEC5NFY1Lz5{NECwPVA3PDxxYU6=
MDA-MB-415	MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?			M{j6NWlEPTB;MD60NkDPxE1?	M{PyZVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MEC5NFY1Lz5{NECwPVA3PDxxYU6=
HCC1806	NUXjdW1ZT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=			NXPmPVBjUUN3ME2wMlQ1KM7:TR?=	MXy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDByOUC2OEc,OjRyMEmwOlQ9N2F-
HCC1395	MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?			NFzSdGNKSzVyPUCuOFkh\|ryP	NWXuSW9PRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSwNFkxPjRpPkK0NFA6ODZ2PD;hQi=>
HCC1937	NFrMbFBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=			NIDOcXNKSzVyPUCuOVAh\|ryP	MnjoQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjRyMEmwOlQoRjJ2MEC5NFY1RC:jPh?=
HCC1143	MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?			NGLYSFVKSzVyPUCuOVQh\|ryP	MWK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDByOUC2OEc,OjRyMEmwOlQ9N2F-
UACC-732	MoLoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?			MX;JR\|UxRTBwNkWg{txO	MnnDQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjRyMEmwOlQoRjJ2MEC5NFY1RC:jPh?=
MDA-MB-231	NWnmSJNQT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=			Mli3TWM2OD1zLkCwJO69VQ>?	M2HGTVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MEC5NFY1Lz5{NECwPVA3PDxxYU6=
MDA-MB-157	MnLZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?			M3vYOGlEPTB;MT6xNkDPxE1?	NHPKXHg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NECwPVA3PCd-MkSwNFkxPjR:L3G+
BT-549	MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?			MlTqTWM2OD1zLkG0JO69VQ>?	MYe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDByOUC2OEc,OjRyMEmwOlQ9N2F-
KPL-1	M37sbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7			MVvJR\|UxRTFwOEmg{txO	MmLIQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjRyMEmwOlQoRjJ2MEC5NFY1RC:jPh?=
CAL-51	MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?			MVHJR\|UxRTFwOEmg{txO	MlfXQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjRyMEmwOlQoRjJ2MEC5NFY1RC:jPh?=
BT474	MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?			M{HzTGlEPTB;MD6wNFMzOyEEsTCwMlAxODd3IN88US=>	MkfpQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN6MU[yOVQoRjJ\|OEG2NlU1RC:jPh?=
SKBR3	NU\0b\|NST3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=			NWLQ[INSUUN3ME2wMlAxPzViwsGgNE4xODVizszN	Mk\CQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN6MU[yOVQoRjJ\|OEG2NlU1RC:jPh?=
MDAMB453	NXTYOFJpT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=			NXjQWJRyUUN3ME2xMlU6KMLzIECuNVc6KM7:TR?=	M1TuWlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ\|OEG2NlU1Lz5{M{ixOlI2PDxxYU6=
KB	NF\TXmtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=			Mn3nTWM2OD12LkGzJOKyKDBwNEeg{txO	NUj2TmRnRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkK0PVE6OzVpPkKyOFkyQTN3PD;hQi=>
KBv200	MojOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?			M{fvV2lEPTB;Nj6wN{DDuSByLk[0JO69VQ>?	MofDQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ2OUG5N\|UoRjJ{NEmxPVM2RC:jPh?=
MCF-7	M2rHNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7			NXu1SXREUUN3ME2zMlMxKMLzIECuOFEh\|ryP	NXX5ZnhIRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkK0PVE6OzVpPkKyOFkyQTN3PD;hQi=>
MCF-7/Adr	Mom5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?			MYfJR\|UxRSB{Lki4JOKyKDBwM{Cg{txO	MkS5QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ2OUG5N\|UoRjJ{NEmxPVM2RC:jPh?=
MCF-7	NIDrcFlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=			MXvJR\|UxRTNwMEKgxtEhOC5\|NDFOwG0>	M2raUlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{NEmxPVM2Lz5{MkS5NVk{PTxxYU6=
MCF-7/FLV1000	NXHndmVDT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=			MVrJR\|UxRTdwMEmgxtEhOC55MTFOwG0>	NYTvR3FZRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkK0PVE6OzVpPkKyOFkyQTN3PD;hQi=>
HL60	NYfsbVhMT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=			NIC5UJZKSzVyPUKuNlYhyrFiMD6yN{DPxE1?	MmXYQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ2OUG5N\|UoRjJ{NEmxPVM2RC:jPh?=
HL60/Adr	NUXHXpM{T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=			NX;FV21[UUN3ME2xMlQzKMLzIECuNVUh\|ryP	M1LUUlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{NEmxPVM2Lz5{MkS5NVk{PTxxYU6=
HEK293/pcDNA3.1	NVPZfJJET3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=			M3e3VWlEPTB;NT6yPUDDuSByLkWzJO69VQ>?	NFHPU\|Y9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkS5NVk{PSd-MkK0PVE6OzV:L3G+
HEK293/ABCB1	NWe3UWhrT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=			NHH6fnBKSzVyPU[uPVEhyrFiMD63NEAh\|ryP	MmqyQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ2OUG5N\|UoRjJ{NEmxPVM2RC:jPh?=
SKBR	M1zVXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	MonuNE4xOS1zMECgcm0>	MoPaN{04KGR?	NFLRPZVqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjD0bY1mKGGwZDDkc5NmKGSncHXu[IVvfCCvYX7u[ZI>	MoHKQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF2OEe2NFUoRjJzNEi3OlA2RC:jPh?=
L858R(EGFR)	NH;BZZpE\WyuIG\pZYJqdGm2eTDBd5NigQ>?			NGG1[2Nl\WO{ZXHz[ZMh[2WubDD2bYFjcWyrdImgbY4hfGmvZTDhcoQh\G:\|ZTDk[ZBmdmSnboSgcYFvdmW{	MV68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yPzNzMUCwNkc,OTd\|MUGwNFI9N2F-
L858R/T790M(EGFR)	NHfyRpJE\WyuIG\pZYJqdGm2eTDBd5NigQ>?			MUjk[YNz\WG\|ZYOgZ4VtdCC4aXHibYxqfHliaX6geIlu\SCjbnSg[I9{\SCmZYDlcoRmdnRibXHucoVz	M4S5blxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF5M{GxNFAzLz5zN{OxNVAxOjxxYU6=
G776insV_G/C	MljOR4VtdCCYaXHibYxqfHliQYPzZZk>			MXrk[YNz\WG\|ZYOgZ4VtdCC4aXHibYxqfHliaX6geIlu\SCjbnSg[I9{\SCmZYDlcoRmdnRibXHucoVz	NGDIe3Y9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zN{OxNVAxOid-MUezNVExODJ:L3G+
wild-type	Mn;YR4VtdCCYaXHibYxqfHliQYPzZZk>			M2jjVYRm[3KnYYPld{Bk\WyuII\pZYJqdGm2eTDpckB1cW2nIHHu[EBld3OnIHTldIVv\GWwdDDtZY5v\XJ?	NGPyU3A9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zN{OxNVAxOid-MUezNVExODJ:L3G+
A775insYVMA	M172NmNmdGxiVnnhZoltcXS7IFHzd4F6			NHzWcGtl\WO{ZXHz[ZMh[2WubDD2bYFjcWyrdImgbY4hfGmvZTDhcoQh\G:\|ZTDk[ZBmdmSnboSgcYFvdmW{	MVq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yPzNzMUCwNkc,OTd\|MUGwNFI9N2F-
G776insV_G/L	NFTN[YFE\WyuIG\pZYJqdGm2eTDBd5NigQ>?			NGGwcmNl\WO{ZXHz[ZMh[2WubDD2bYFjcWyrdImgbY4hfGmvZTDhcoQh\G:\|ZTDk[ZBmdmSnboSgcYFvdmW{	NFTvZm89[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zN{OxNVAxOid-MUezNVExODJ:L3G+
P780insGSP	MlnhR4VtdCCYaXHibYxqfHliQYPzZZk>			MlWy[IVkemWjc3XzJINmdGxidnnhZoltcXS7IHnuJJRqdWViYX7kJIRwe2ViZHXw[Y5l\W62IH3hco5meg>?	NV[wN3pyRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUezNVExODJpPkG3N\|EyODB{PD;hQi=>
NCI-H1781	NYLDTZlrT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=			M2jUTYlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIITpcYUh[W6mIHTvd4Uh\GWyZX7k[Y51KG2jbn7ldi=>	NHT5cFY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zNkixPFYyQCd-MU[4NVg3OTh:L3G+
HCC827	MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?			NWqw[WZKcW6qaXLpeJMh[2WubDDndo94fGhiaX6geIlu\SCjbnSg[I9{\SCmZYDlcoRmdnRibXHucoVz	NFvmc3E9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zNkixPFYyQCd-MU[4NVg3OTh:L3G+
H3255	NV7t[o12T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=			MkXFbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5idHnt[UBidmRiZH;z[UBl\XCnbnTlcpQhdWGwbnXy	M3nkVVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF4OEG4OlE5Lz5zNkixPFYyQDxxYU6=
NCI-H1975	MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?			NXLNeVVHcW6qaXLpeJMh[2WubDDndo94fGhiaX6geIlu\SCjbnSg[I9{\SCmZYDlcoRmdnRibXHucoVz	MU[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yPjhzOE[xPEc,OTZ6MUi2NVg9N2F-
A549	M1;mS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7			M2HuPIlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIITpcYUh[W6mIHTvd4Uh\GWyZX7k[Y51KG2jbn7ldi=>	NEfn[4U9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zNkixPFYyQCd-MU[4NVg3OTh:L3G+
3T3	MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?			Mom1TWM2OD15MECgxtEhPzhibl2=	NGrB[4w9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zNUG3N\|AxQCd-MUWxO\|MxODh:L3G+
3T3/neu	MlXvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?			M1XncGlEPTB;MzFCtUAxNjF2IH7N	NHrpNWE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zNUG3N\|AxQCd-MUWxO\|MxODh:L3G+
SK-Br-3	NFjIVY9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?=			MlvUTWM2OD1{INMxJFAvOThibl2=	M4nVVVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF3MUezNFA5Lz5zNUG3N\|AxQDxxYU6=
BT 474	MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?			NH7IPIdKSzVyPUKgxtEhOC5yNjDuUS=>	MmHiQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTVzN{OwNFgoRjF3MUezNFA5RC:jPh?=
A431	NHi3VHdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=			MWfJR\|UxRThzINMxJFkhdk1?	M1v1UlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF3MUezNFA5Lz5zNUG3N\|AxQDxxYU6=
MDA-MB-435	MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?			NFHhT2VKSzVyPUm2NEDDuSBzNkWgcm0>	MVy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yPTF5M{CwPEc,OTVzN{OwNFg9N2F-
SW620	NF:zRWZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=			NIfnN5JKSzVyPU[5NEDDuSB6NDDuUS=>	MlOyQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTVzN{OwNFgoRjF3MUezNFA5RC:jPh?=
SKBR3	NHrafmZHfW6ldHnvckBie3OjeR?=			MWfJcohq[mm2aX;uJI9nKGi3bXHuJGhmejJiaX6gV2tDWjNiY3XscJMtKEWFNUCgQUAxNjByMjFOwG0v	MXu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQDB5N{SyOUc,OThyN{e0NlU9N2F-
BT474	MYrGeY5kfGmxbjDhd5NigQ>?			NEf5d3pKdmirYnn0bY9vKG:oIHj1cYFvKEinckKgbY4hSlR2N{SgZ4VtdHNuIFXDOVAhRSByLkCwNkDPxE1w	MoXiQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOThyN{e0NlUoRjF6MEe3OFI2RC:jPh?=
A431	NFf1O3lHfW6ldHnvckBie3OjeR?=			Mlr6TY5pcWKrdHnvckBw\iCqdX3hckBJ\XJ{IHnuJGE1OzFiY3XscJMtKEWFNUCgQUAxNjB6MTFOwG0v	NYjafohURGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUiwO\|c1OjVpPkG4NFc4PDJ3PD;hQi=>
SW620	NVW2fYdWTnWwY4Tpc44h[XO\|YYm=			MXXJcohq[mm2aX;uJI9nKGi3bXHuJGhmejJiaX6gV3c3OjBiY3XscJMtKEWFNUCgQUAxNjZ7IN88UU4>	MYK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQDB5N{SyOUc,OThyN{e0NlU9N2F-
BA/F3	NF\jfoJEgXSxdH;4bYNqfHliYYPzZZk>			M1qyfGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KG2xdYPlJGJCN0Z\|IHPlcIx{KGW6cILld5NqdmdiRVfGVkBNQDV6UjDteZRidnRuIFnDOVAhRSByLkCwN\|Uh\|ryPLh?=	MlXoQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl{M{myNlkoRjF7MkO5NlI6RC:jPh?=
BA/F3	NYL0[HFsS3m2b4TvfIlkcXS7IHHzd4F6			MVnDfZRwfG:6aXPpeJkh[WejaX7zeEBud3W\|ZTDCRU9HOyClZXzsd{BmgHC{ZYPzbY5oKEWJRmKgUFg2QFJxVEe5NG0hdXW2YX70MEBKSzVyIE2gNE4yQCEQvF2u	Mk[5QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl{M{myNlkoRjF7MkO5NlI6RC:jPh?=
Sf9	M2TOR2Z2dmO2aX;uJIF{e2G7		NIT5e28yOCCvaX7z	NFvZOm5KdmirYnn0bY9vKG:oIHj1cYFvKHerbHSgeJlx\SCHR1\SJIV5eHKnc4Pl[EBqdiCVZkmgZ4VtdHNidYPpcochY2ejbX3hN\|JRZS2DVGCgZYZ1\XJiMUCgcYlveyCkeTDzZ4lvfGmubHH0bY9vKGOxdX70bY5oNCCLQ{WwJF0hOC5yMEK1JO69VS5?	NGT2O5E9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEmwNFY1Oyd-MkS5NFA3PDN:L3G+
Sf9	NVmyVHUzTnWwY4Tpc44h[XO\|YYm=		NUXybY9vOTBibXnudy=>	MnHrTY5pcWKrdHnvckBw\iCqdX3hckBGT0[UIGS3PVBON0x6NUjSJI12fGGwdDDlfJBz\XO\|ZXSgbY4hW2Z7IHPlcIx{KHW\|aX7nJHto[W2vYUOyVH0uSVSSIHHmeIVzKDFyIH3pcpMh[nlic3PpcpRqdGyjdHnvckBkd3WwdHnu[{whUUN3MDC9JFAvODZ4IN88UU4>	NHjufWI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEmwNFY1Oyd-MkS5NFA3PDN:L3G+
BAF3	M33ydWZ2dmO2aX;uJIF{e2G7		NFnvNlg4OiCqcoO=	M3jSXWlvcGmkaYTpc44hd2ZiVHXsMYZ2e2WmIFnHSlFTKCi3bnvuc5dvKG:{aXfpckkh\XiycnXzd4VlKGmwIH3veZNmKEKDRkOgZ4VtdHNiYYPz[ZN{\WRiYYOg[5Jwf3SqIHnubIljcXSrb36gZYZ1\XJiN{KgbJJ{KGK7IFPlcIxVcXSncj3HcI8h[XO\|YYmsJGdKPTBiPTCwMlE6KM7:TT6=	NFmwdpk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEK4NlEzOid-MkiyPFIyOjJ:L3G+
BAF3	NGLo[2VHfW6ldHnvckBie3OjeR?=		MonhO\|IhcHK\|	MX;Jcohq[mm2aX;uJI9nKFSnbD3meZNm\CCLTmPSJEh2dmuwb4fuJI9zcWerbjmg[ZhxemW\|c3XkJIlvKG2xdYPlJGJCTjNiY3XscJMh[XO\|ZYPz[YQh[XNiZ4Lve5RpKGmwaHnibZRqd25iYX\0[ZIhPzJiaILzJIJ6KEOnbHzUbZRmei2JbH:gZZN{[XluIFfJOVAhRSByLkK5JO69VS5?	MlnhQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh{OEKxNlIoRjJ6MkiyNVIzRC:jPh?=
BAF3	MkPRS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl?		NG\pUlc4OiCqcoO=	MV3Hdo94fGhiaX7obYJqfGmxbjDv[kBud3W\|ZTDCRWY{KGOnbHzzJIFnfGW{IEeyJIhzeyCkeTDD[YxtXGm2ZYKtS4xwKGG\|c3H5MEBIUTVyIE2gNU46KM7:TT6=	Mn\VQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh{OEKxNlIoRjJ6MkiyNVIzRC:jPh?=

他の多くの細胞株試験データをご覧になる場合はこちらをクリックして下さい

アッセイ

Methods	Test Index	PMID
Western blot	pHER2 / HER2 / pAKT / AKT / pERK / ERK ; PubMed: 24009064 Oncotarget 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 PLoS One (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 PLoS One 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

体内試験

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]

お薦めの試験操作（参考用のみ）

キナーゼ試験：^[1]	- 合併 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.
細胞試験： ^[1]	- 合併細胞株： 3T3, 3T3/neu, A431, BT474, SK-Br-3, MDA-MB-435, and SW480 濃度： Dissolved in DMSO, final concentrations 0.5 ng/mL-5 μg/mL 反応時間： 2 or 6 days 実験の流れ： 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. (参考用のみ)
動物試験：^[1]	- 合併動物モデル： Female athymic (nude) mice implanted s.c. with 3T3/neu, BT474, MCF-7, or SK-OV-3 cells 投薬量： ~80 mg/kg/day 投与方法： Gavage (参考用のみ)

参考

[1] Rabindran SK, et al. Cancer Res, 2004, 64(11), 3958-3965.

溶解度 (25°C)

体外	DMSO	5 mg/mL (8.97 mM) warming
	Water	Insoluble
	Ethanol	Insoluble
体内	左から（NMPから）右の順に溶剤を製品に加えます(文献ではなく、Selleckの実験によるデータ): 30% PEG400+0.5% Tween80+5% propylene glycol 混合させたのち直ちに使用することを推奨します。	5 mg/mL

* 溶解度測定はSelleck技術部門によって行われており、その他文献に示されている溶解度と差異がある可能性がありますが、同一ロットの生産工程で起きる正常な現象ですからご安心ください。

化学情報 Neratinib (HKI-272) SDFをダウンロードする

分子量	557.04
化学式	C₃₀H₂₉ClN₆O₃
CAS No.	698387-09-6
Storage	3 years-20°C powder 2 years-80°C in solvent
別名	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

投与溶媒組成計算器(クリア溶液)

ステップ１：実験データを入力してください。（実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します）

投与量

mg/kg

動物平均体重

投与体積（動物毎）

動物数

匹

ステップ２：投与溶媒の組成を入力してください。（ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください）

% DMSO+ % + % Tween 80+ % ddH₂O

計算リセット

計算結果:

投与溶媒濃度： mg/ml；

DMSOストック溶液調製方法： mg 試薬を μL DMSOに溶解する（濃度 mg/mL，注：濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。）

投与溶媒調製方法：μL DMSOストック溶液に μL PEG300，を加え、完全溶解後μL Tween 80，を加えて完全溶解させた後 μL ddH₂O，を加え完全に溶解させます。

注意：１.ストック溶液に沈殿、混濁などがないことをご確認ください；
２.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。

便利ツール

モル濃度計算器

求めたい質量、体積または濃度を計算してください。

質量 (mg) = 濃度 (mM) x 体積 (mL) x 分子量 (g/mol)

モル濃度計算器方程式

質量

濃度

体積

分子量
=

×

×

*貯蔵液を準備するとき、常に、オンであるとわかる製品のバッチに特有の分子量を使って、を通してラベルとMSDS/COA（製品ページで利用可能な）。

希釈計算器

貯蔵液を準備するために必要な希釈率を計算してください。Selleck希釈計算器は、以下の方程式に基づきます：

開始濃度 x 開始体積 = 最終濃度 x 最終体積

希釈の計算式

この方程式は、一般に略語を使われます：C1V1 = C2V2 ( 入力出力 )

C1

V1

C2

V2
×

=

×

常に貯蔵液を準備するとき、小びんラベルとMSDS/COA（オンラインで利用できる）で見つかる製品のバッチに特有の分子量を使ってください。

連続希釈計算器方程式

連続希釈剤
初めの濃度：
稀釈倍数：

計算結果

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):

分子量計算器

分子量计算器

そのモル質量と元素組成を計算するために、合成物の化学式を入力してください：

チップス: 化学式は大文字と小文字の区別ができます。C10H16N2O2 c10h16n2o2

モル濃度計算器

質量	濃度	体積	分子量
=	×	×

臨床試験 (data from https://clinicaltrials.gov, updated on 2021-01-06)

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	--

技術サポート

ストックの作り方、阻害剤の保管方法、細胞実験や動物実験の際に注意すべき点など、製品を取扱う時に問い合わせが多かった質問に対しては取扱説明書でお答えしています。

Handling Instructions

他に質問がある場合は、お気軽にお問い合わせください。

* 必須
*大学・企業名:
*名前:
*電子メール:
*電話番号:
*内容:

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Most Potent HER2 Inhibitor

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FDA-approved HER2 Inhibitor

Lapatinib : Approved by FDA for breast cancer.
Classic HER2 Inhibitor

Lapatinib (GW-572016) Ditosylate : Dual EGFR/ErbB2 inhibitor, IC50=10.8/9.2 nM.

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研究分野別

製品類型

Neratinib (HKI-272)

文献中Selleckの製品使用例(67)

製品安全説明書

HER2阻害剤の選択性比較

生物活性

お薦めの試験操作（参考用のみ）

参考

溶解度 (25°C)

化学情報 Neratinib (HKI-272) SDFをダウンロードする

投与溶媒組成計算器(クリア溶液)

便利ツール

モル濃度計算器

質量 (mg) = 濃度 (mM) x 体積 (mL) x 分子量 (g/mol)

モル濃度計算器方程式

希釈計算器

開始濃度 x 開始体積 = 最終濃度 x 最終体積

希釈の計算式

連続希釈計算器方程式

連続希釈剤

計算結果

分子量计算器

総分子量：g/mol

モル濃度計算器

臨床試験 (data from https://clinicaltrials.gov, updated on 2021-01-06)

技術サポート

HER2シグナル伝達経路

HER2 Inhibitors with Unique Features

相関HER2製品