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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HER2和EGFR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。

CAS: 698387-09-6

规格	价格	库存
5mg	RMB 1227.96	现货
25mg	RMB 3863.92	现货
100mg	RMB 7933.43	现货
大包装	有超大折扣

今日订购，明日送达全国免运费分装免费分装成小规格产品（单支最小为1mg）如1支10mg产品可分装为10支1mg产品全国免费电话：400-668-6834 \| Email：info@selleck.cn

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

生物活性

产品描述

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-

Click to View More Cell Line Experimental Data

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]

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

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

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 点击购买： PEG400 Tween 80	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
储存条件	2年	-80°C	溶于溶剂

Download Neratinib (HKI-272) SDF

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 μL 动物数量只

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，注：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：取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：取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
=	×	×

稀释计算器分子量计算器

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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