Neratinib (HKI-272)

For research use only. Not for use in humans.

目录号：S2150 中文名称：来那替尼

CAS No. 698387-09-6

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。

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5mg	RMB 1227.96	现货
25mg	RMB 3863.92	现货
100mg	RMB 7933.43	现货
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客户使用Selleck生产的Neratinib (HKI-272)发表文献82篇：

Cell Metab, 2022, 34(1):90-105.e7

PubMed: 34986341 ( click the link to review the publication )

Cancer Cell, 2021, S1535-6108(21)00284-1

PubMed: 34171264 ( click the link to review the publication )

Cancer Cell, 2020, 37(2):183-199

PubMed: 31978326 ( click the link to review the publication )

Nat Genet, 2019, 51(2):207-216

PubMed: 30531871 ( click the link to review the publication )

Cancer Cell, 2019, 10.1016/j.ccell.2019.09.001

PubMed: 31588020 ( click the link to review the publication )

Cancer Discov, 2013, 3(2):168-81

PubMed: 23229345 ( click the link to review the publication )

Cancer Discov, 2013, 3(2):224-37

PubMed: 23220880 ( click the link to review the publication )

Cancer Discov, 2012, 2(5):458-71

PubMed: 22588883 ( click the link to review the publication )

JCO Precis Oncol, 2022, 6:e2100325

PubMed: 35171661 ( click the link to review the publication )

Biomedicines, 2022, 10(3)638

PubMed: 35327440 ( click the link to review the publication )

Cell Commun Signal, 2022, 20(1):4

PubMed: 34998412 ( click the link to review the publication )

Cell Rep Med, 2022, 3(1):100492

PubMed: 35106508 ( click the link to review the publication )

Nat Commun, 2021, 12(1):6377

PubMed: 34737261 ( click the link to review the publication )

Nat Commun, 2021, 12(1):6667

PubMed: 34795269 ( click the link to review the publication )

Clin Cancer Res, 2021, 10.1158/1078-0432.CCR-21-2660

PubMed: 34433654 ( click the link to review the publication )

Breast Cancer Res, 2021, 23(1):81

PubMed: 34344439 ( click the link to review the publication )

Lung Cancer, 2021, 162:79-85

PubMed: 34741886 ( click the link to review the publication )

Dis Model Mech, 2021, dmm.047621

PubMed: 34841430 ( click the link to review the publication )

Cancer Med, 2021, 10(7):2370-2379

PubMed: 33665980 ( click the link to review the publication )

Molecules, 2021, 26(15)4537

PubMed: 34361688 ( click the link to review the publication )

Biomed Chromatogr, 2021, e5221

PubMed: 34331710 ( click the link to review the publication )

Acta Neuropathol, 2020, 17

PubMed: 32303840 ( click the link to review the publication )

Nat Commun, 2020, 11(1):385

PubMed: 31959756 ( click the link to review the publication )

Sci Adv, 2020, 6(34):eaba8968

PubMed: 32937365 ( click the link to review the publication )
EMBO Mol Med, 2020, 8;12(5):e11498

PubMed: 32329582 ( click the link to review the publication )

Genome Med, 2020, 18;12(1):17

PubMed: 32070411 ( click the link to review the publication )

Cell Rep, 2020, 31(12):107800

PubMed: 32579927 ( click the link to review the publication )

Cancers (Basel), 2020, 13;12(2) pii: E436

PubMed: 32069833 ( click the link to review the publication )

Cancers (Basel), 2020, 12(10)E2838

PubMed: 33019652 ( click the link to review the publication )

Front Oncol, 2020, 10:554704

PubMed: 33330026 ( click the link to review the publication )

Int J Mol Sci, 2020, 18;21(8):2825

PubMed: 32325639 ( click the link to review the publication )

J Genet Genomics, 2020, 47(7):389-395

PubMed: 33004309 ( click the link to review the publication )

J Cancer Res Clin Oncol, 2020, 146(3):605-619

PubMed: 32036454 ( click the link to review the publication )

Pharmaceuticals (Basel), 2020, 14(1)E9

PubMed: 33374155 ( click the link to review the publication )

Cancer Sci, 2020, 111(3):849-856

PubMed: 31856375 ( click the link to review the publication )

Cancers (Basel), 2019, 11(4)

PubMed: 31018595 ( click the link to review the publication )

Breast Cancer Res, 2019, 21(1):135

PubMed: 31801615 ( click the link to review the publication )

Cell Commun Signal, 2019, 17(1):15

PubMed: 30786890 ( click the link to review the publication )

Cell Cycle, 2019, 18(13):1513-1522

PubMed: 31135266 ( click the link to review the publication )

Leuk Res, 2019, 78:12-20

PubMed: 30660961 ( click the link to review the publication )

Oncol Lett, 2019, 17(3):2729-2736

PubMed: 30854046 ( click the link to review the publication )

NPJ Precis Oncol, 2019, 03:18

PubMed: 31341951 ( click the link to review the publication )

Cell Syst, 2018, 6(3):329-342

PubMed: 29550255 ( click the link to review the publication )

Clin Cancer Res, 2018, 24(4):807-820

PubMed: 28974546 ( click the link to review the publication )

Sci Signal, 2018, 11(549)

PubMed: 30254057 ( click the link to review the publication )

Mol Cancer Ther, 2018, 17(10):2144-2155

PubMed: 30065098 ( click the link to review the publication )

Mol Cell Proteomics, 2018, 17(6):1245-1258

PubMed: 29531020 ( click the link to review the publication )

Lung Cancer, 2018, 126:72-79

PubMed: 30527195 ( click the link to review the publication )
Biochim Biophys Acta, 2018, 1865(8):1073-1087

PubMed: 29733883 ( click the link to review the publication )

J Biol Chem, 2018, 293(35):13401-13414

PubMed: 29997256 ( click the link to review the publication )

Front Chem, 2018, 6:47

PubMed: 29564326 ( click the link to review the publication )

Clin Cancer Res, 2017, 23(17):5123-5134

PubMed: 28487443 ( click the link to review the publication )

Genome Med, 2017, 9(1):40

PubMed: 28446242 ( click the link to review the publication )

Breast Cancer Res, 2017, 19(1):105

PubMed: 28886748 ( click the link to review the publication )

Mol Cancer Ther, 2017,

PubMed: 27913578 ( click the link to review the publication )

Sci Rep, 2017,

PubMed: 28638122 ( click the link to review the publication )

BMC Cancer, 2017,

PubMed: 28806950 ( click the link to review the publication )

Oncotarget, 2017,

PubMed: 29285221 ( click the link to review the publication )

Curr Protoc Chem Biol, 2017, 9(2):55-74

PubMed: 28628199 ( click the link to review the publication )

Gut, 2016, 1296-305

PubMed: 26001389 ( click the link to review the publication )

Clin Cancer Res, 2016, 22(19):4859-4869

PubMed: 27697991 ( click the link to review the publication )

Cancer Lett, 2016, 382(2):176-185

PubMed: 27597738 ( click the link to review the publication )

Mol Cancer Ther, 2016,

PubMed: 27678331 ( click the link to review the publication )

Oral Dis, 2016, 22(8):797-804

PubMed: 27476950 ( click the link to review the publication )

Oncotarget, 2016, 7(36):58038-58050

PubMed: 27487128 ( click the link to review the publication )

Gut, 2015, 10.1136/gutjnl-2014-309026

PubMed: ( click the link to review the publication )

Clin Cancer Res, 2015, 10.1158/1078-0432.CCR-14-2789

PubMed: 25948633 ( click the link to review the publication )

Clin Cancer Res, 2015, 21(23):5305-13

PubMed: 26206867 ( click the link to review the publication )

Proc Natl Acad Sci USA, 2015,

PubMed: 26508629 ( click the link to review the publication )

Oncol Rep, 2015, 34(3):1613-9

PubMed: 26166014 ( click the link to review the publication )

PLoS One, 2015, 10(4):e0123623

PubMed: 25853726 ( click the link to review the publication )

Oncotarget, 2015,

PubMed: 26375550 ( click the link to review the publication )
Oncotarget, 2015,

PubMed: 25965827 ( click the link to review the publication )

Drug Metab Dispos, 2014, 42(11):1851-7

PubMed: 25165131 ( click the link to review the publication )

Invest New Drugs, 2014, 32(6):1096-104

PubMed: 25081321 ( click the link to review the publication )

Genes Cancer, 2014, 5(7-8):261-72

PubMed: 25221644 ( click the link to review the publication )

Drug Metab Lett, 2014, 8(1):19-30

PubMed: 24628405 ( click the link to review the publication )

Assay Drug Dev Technol, 2014, 12(9-10):514-26

PubMed: 25506801 ( click the link to review the publication )

Breast Cancer Res, 2013,

PubMed: 24044505 ( click the link to review the publication )

J Genet Syndr Gene Ther, 2013, 4

PubMed: 25520884 ( click the link to review the publication )

Genetic Syndromes & Gene Therapy, 2013, 4:6

PubMed: ( click the link to review the publication )

Mol Cell Proteomics, 2012, 11(6):M112.017764

PubMed: 22345495 ( click the link to review the publication )

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	Activity Description	PMID
BT-474	MmLaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?			NF;kfWlKSzVyPECuNFA2KM7:TR?=	MkGzQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjRyMEmwOlQoRjJ2MEC5NFY1RC:jPh?=
EFM-192A	M1fNXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7			MoPpTWM2ODxyLkCwOUDPxE1?	MUK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDByOUC2OEc,OjRyMEmwOlQ9N2F-
HCC1569	MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?			NHS2V\|JKSzVyPECuNFA2KM7:TR?=	MojPQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjRyMEmwOlQoRjJ2MEC5NFY1RC:jPh?=
HCC1954	NHzaR3JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=			NVvZdppEUUN3MEywMlAxPSEQvF2=	Ml;mQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjRyMEmwOlQoRjJ2MEC5NFY1RC:jPh?=
MDA-MB-175	NX;uUFNCT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=			MULJR\|UxRDBwMEC1JO69VQ>?	MWO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDByOUC2OEc,OjRyMEmwOlQ9N2F-
MDA-MB-361	M2j3eGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7			MUDJR\|UxRDBwMEC1JO69VQ>?	Ml7NQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjRyMEmwOlQoRjJ2MEC5NFY1RC:jPh?=
SK-BR-3	MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?			MUHJR\|UxRDBwMEC1JO69VQ>?	NY\k[3BSRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSwNFkxPjRpPkK0NFA6ODZ2PD;hQi=>
UACC-812	MlzMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?			NHOzXJRKSzVyPECuNFA2KM7:TR?=	NX7jXnRqRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSwNFkxPjRpPkK0NFA6ODZ2PD;hQi=>
UACC-893	NV21[HNuT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=			NV\tR5ZwUUN3MEywMlAxPSEQvF2=	NEGyW2M9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NECwPVA3PCd-MkSwNFkxPjR:L3G+
SUM-225	NX30RWhbT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=			M1\YW2lEPTB;MD6wNUDPxE1?	M1fnUVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MEC5NFY1Lz5{NECwPVA3PDxxYU6=
SUM-190	M4\IU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7			NV\ZOmxFUUN3ME2wMlAyKM7:TR?=	NXTKSHJtRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSwNFkxPjRpPkK0NFA6ODZ2PD;hQi=>
ZR-75-1	NX2wVmJtT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=			NETj[W9KSzVyPUCuNFMh\|ryP	M{SyPFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MEC5NFY1Lz5{NECwPVA3PDxxYU6=
HCC70	MmD0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?			NXn1TopIUUN3ME2wMlA{KM7:TR?=	M{PISlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MEC5NFY1Lz5{NECwPVA3PDxxYU6=
BT-20	MnPBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?			MmLYTWM2OD1yLkC3JO69VQ>?	MkHvQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjRyMEmwOlQoRjJ2MEC5NFY1RC:jPh?=
MDA-MB-453	MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?			MVzJR\|UxRTBwMEmg{txO	MoTkQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjRyMEmwOlQoRjJ2MEC5NFY1RC:jPh?=
HCC1187	M37ZW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7			NX7QNWUzUUN3ME2wMlExKM7:TR?=	M{TkSFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MEC5NFY1Lz5{NECwPVA3PDxxYU6=
EFM-19	NGfOS29Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?=			NFvmN3JKSzVyPUCuNVEh\|ryP	NY[5bINXRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSwNFkxPjRpPkK0NFA6ODZ2PD;hQi=>
T-47D	NVjYWWI6T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=			Mnv6TWM2OD1yLkG2JO69VQ>?	NGHmc5c9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NECwPVA3PCd-MkSwNFkxPjR:L3G+
MDA-MB-134	MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?			NYXIPGVSUUN3ME2wMlE4KM7:TR?=	NVTJ[3U5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSwNFkxPjRpPkK0NFA6ODZ2PD;hQi=>
HCC38	NWDQVJpuT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=			MljoTWM2OD1yLkK1JO69VQ>?	NFjJSW89[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NECwPVA3PCd-MkSwNFkxPjR:L3G+
MDA-MB-435	M1HvNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7			MkPFTWM2OD1yLkOzJO69VQ>?	NIPHUGo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NECwPVA3PCd-MkSwNFkxPjR:L3G+
MDA-MB-468	M3vt[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7			NVzU[41GUUN3ME2wMlM{KM7:TR?=	MmftQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjRyMEmwOlQoRjJ2MEC5NFY1RC:jPh?=
CAMA-1	MnvNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?			NELUemxKSzVyPUCuN\|ch\|ryP	NETTTHY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NECwPVA3PCd-MkSwNFkxPjR:L3G+
MDA-MB-436	MmHKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?			NXPTZVZOUUN3ME2wMlQyKM7:TR?=	NWfYT25WRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSwNFkxPjRpPkK0NFA6ODZ2PD;hQi=>
MCF-7	M2X0NWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7			M{j1UmlEPTB;MD60NUDPxE1?	Ml;HQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjRyMEmwOlQoRjJ2MEC5NFY1RC:jPh?=
MDA-MB-415	MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?			M134NGlEPTB;MD60NkDPxE1?	NUDUU4I1RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSwNFkxPjRpPkK0NFA6ODZ2PD;hQi=>
HCC1806	NGfTeYJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=			MmGzTWM2OD1yLkS0JO69VQ>?	NHq5NoM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NECwPVA3PCd-MkSwNFkxPjR:L3G+
HCC1395	MoS4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?			NInsU5VKSzVyPUCuOFkh\|ryP	M4XkelxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MEC5NFY1Lz5{NECwPVA3PDxxYU6=
HCC1937	Ml;jS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?			MlXFTWM2OD1yLkWwJO69VQ>?	NGHWcII9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NECwPVA3PCd-MkSwNFkxPjR:L3G+
HCC1143	NELoSYRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=			NEn3cnlKSzVyPUCuOVQh\|ryP	NX\STY51RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSwNFkxPjRpPkK0NFA6ODZ2PD;hQi=>
UACC-732	M{TVd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7			M1TYO2lEPTB;MD62OUDPxE1?	NInVXpk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NECwPVA3PCd-MkSwNFkxPjR:L3G+
MDA-MB-231	NGjOV3dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=			NUD0TGZuUUN3ME2xMlAxKM7:TR?=	MUG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDByOUC2OEc,OjRyMEmwOlQ9N2F-
MDA-MB-157	MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?			NFKxTIFKSzVyPUGuNVIh\|ryP	NWDXSHY5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSwNFkxPjRpPkK0NFA6ODZ2PD;hQi=>
BT-549	MoLsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?			MnfYTWM2OD1zLkG0JO69VQ>?	M{jTOVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MEC5NFY1Lz5{NECwPVA3PDxxYU6=
KPL-1	MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?			M1fq[mlEPTB;MT64PUDPxE1?	NIGyTmU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NECwPVA3PCd-MkSwNFkxPjR:L3G+
CAL-51	NHfGSW5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?=			M3XmVWlEPTB;MT64PUDPxE1?	NF3JNGg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NECwPVA3PCd-MkSwNFkxPjR:L3G+
BT474	MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?			M33G[WlEPTB;MD6wNFMzOyEEsTCwMlAxODd3IN88US=>	NX7TZ3dQRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO4NVYzPTRpPkKzPFE3OjV2PD;hQi=>
SKBR3	MoSyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?			MUTJR\|UxRTBwMEC3OUDDuSByLkCwOUDPxE1?	MlLQQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN6MU[yOVQoRjJ\|OEG2NlU1RC:jPh?=
MDAMB453	M2X1Smdzd3e2aDDJcohq[mm2aX;uJGF{e2G7			Mmr2TWM2OD1zLkW5JOKyKDBwMUe5JO69VQ>?	MYq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzhzNkK1OEc,OjN6MU[yOVQ9N2F-
KB	NGrMfVhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=			NVjwTGdmUUN3ME20MlE{KMLzIECuOFch\|ryP	NF:3V5c9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkS5NVk{PSd-MkK0PVE6OzV:L3G+
KBv200	NVK4UZpUT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=			M4nmc2lEPTB;Nj6wN{DDuSByLk[0JO69VQ>?	M2r1NFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{NEmxPVM2Lz5{MkS5NVk{PTxxYU6=
MCF-7	MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?			NEnKZWtKSzVyPUOuN\|AhyrFiMD60NUDPxE1?	MmPqQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ2OUG5N\|UoRjJ{NEmxPVM2RC:jPh?=
MCF-7/Adr	M3LG[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7			NU\MXZRCUUN3ME2gNk45QCEEsTCwMlMxKM7:TR?=	MYW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjR7MUmzOUc,OjJ2OUG5N\|U9N2F-
MCF-7	M4nYWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7			NHTTdZZKSzVyPUOuNFIhyrFiMD6zOEDPxE1?	MYm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjR7MUmzOUc,OjJ2OUG5N\|U9N2F-
MCF-7/FLV1000	NGPxSoVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=			M3PldmlEPTB;Nz6wPUDDuSByLkexJO69VQ>?	NXnrSGRURGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkK0PVE6OzVpPkKyOFkyQTN3PD;hQi=>
HL60	MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?			NWrEU4pnUUN3ME2yMlI3KMLzIECuNlMh\|ryP	MW[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjR7MUmzOUc,OjJ2OUG5N\|U9N2F-
HL60/Adr	NIq4e4FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=			NG\GeWdKSzVyPUGuOFIhyrFiMD6xOUDPxE1?	MXO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjR7MUmzOUc,OjJ2OUG5N\|U9N2F-
HEK293/pcDNA3.1	NED5[pZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=			Mn33TWM2OD13LkK5JOKyKDBwNUOg{txO	M1fkXFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{NEmxPVM2Lz5{MkS5NVk{PTxxYU6=
HEK293/ABCB1	NGPENIpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=			MVvJR\|UxRTZwOUGgxtEhOC55MDCg{txO	NEPzV3Y9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkS5NVk{PSd-MkK0PVE6OzV:L3G+
SKBR	M3L3XWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	MUKwMlAyNTFyMDDuUS=>	MVmzMVch\A>?	NUDCVYd[cW6qaXLpeJMh[2WubDDndo94fGhiaX6geIlu\SCjbnSg[I9{\SCmZYDlcoRmdnRibXHucoVz	M3z6TlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzNEi3OlA2Lz5{MUS4O\|YxPTxxYU6=
L858R(EGFR)	NWW2W\|FmS2WubDDWbYFjcWyrdImgRZN{[Xl?			NUPnfVB5\GWlcnXhd4V{KGOnbHygeoli[mmuaYT5JIlvKHSrbXWgZY5lKGSxc3Wg[IVx\W6mZX70JI1idm6nch?=	NVvCW3VmRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUezNVExODJpPkG3N\|EyODB{PD;hQi=>
L858R/T790M(EGFR)	MVrD[YxtKF[rYXLpcIl1gSCDc4PhfS=>			NYmwZ5l3\GWlcnXhd4V{KGOnbHygeoli[mmuaYT5JIlvKHSrbXWgZY5lKGSxc3Wg[IVx\W6mZX70JI1idm6nch?=	MnfRQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTd\|MUGwNFIoRjF5M{GxNFAzRC:jPh?=
G776insV_G/C	MoX5R4VtdCCYaXHibYxqfHliQYPzZZk>			M3L0ToRm[3KnYYPld{Bk\WyuII\pZYJqdGm2eTDpckB1cW2nIHHu[EBld3OnIHTldIVv\GWwdDDtZY5v\XJ?	M2r4TVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF5M{GxNFAzLz5zN{OxNVAxOjxxYU6=
wild-type	NHf2c5dE\WyuIG\pZYJqdGm2eTDBd5NigQ>?			MV;k[YNz\WG\|ZYOgZ4VtdCC4aXHibYxqfHliaX6geIlu\SCjbnSg[I9{\SCmZYDlcoRmdnRibXHucoVz	Mn\BQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTd\|MUGwNFIoRjF5M{GxNFAzRC:jPh?=
A775insYVMA	MofpR4VtdCCYaXHibYxqfHliQYPzZZk>			NX7neJZq\GWlcnXhd4V{KGOnbHygeoli[mmuaYT5JIlvKHSrbXWgZY5lKGSxc3Wg[IVx\W6mZX70JI1idm6nch?=	M1jmTFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF5M{GxNFAzLz5zN{OxNVAxOjxxYU6=
G776insV_G/L	NVPGTpFJS2WubDDWbYFjcWyrdImgRZN{[Xl?			MnrK[IVkemWjc3XzJINmdGxidnnhZoltcXS7IHnuJJRqdWViYX7kJIRwe2ViZHXw[Y5l\W62IH3hco5meg>?	NV7nWFRlRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUezNVExODJpPkG3N\|EyODB{PD;hQi=>
P780insGSP	MnPPR4VtdCCYaXHibYxqfHliQYPzZZk>			NH;rW\|Jl\WO{ZXHz[ZMh[2WubDD2bYFjcWyrdImgbY4hfGmvZTDhcoQh\G:\|ZTDk[ZBmdmSnboSgcYFvdmW{	M37nW\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF5M{GxNFAzLz5zN{OxNVAxOjxxYU6=
NCI-H1781	Mn;2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?			NYf2cJV[cW6qaXLpeJMh[2WubDDndo94fGhiaX6geIlu\SCjbnSg[I9{\SCmZYDlcoRmdnRibXHucoVz	Ml3BQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTZ6MUi2NVgoRjF4OEG4OlE5RC:jPh?=
HCC827	MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?			M1fqVIlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIITpcYUh[W6mIHTvd4Uh\GWyZX7k[Y51KG2jbn7ldi=>	NFjNV3g9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zNkixPFYyQCd-MU[4NVg3OTh:L3G+
H3255	M4jldGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7			NYLqbWw3cW6qaXLpeJMh[2WubDDndo94fGhiaX6geIlu\SCjbnSg[I9{\SCmZYDlcoRmdnRibXHucoVz	NX76b21QRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMU[4NVg3OThpPkG2PFE5PjF6PD;hQi=>
NCI-H1975	NVHUeYRyT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=			NYjldpo6cW6qaXLpeJMh[2WubDDndo94fGhiaX6geIlu\SCjbnSg[I9{\SCmZYDlcoRmdnRibXHucoVz	NGXJXHM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zNkixPFYyQCd-MU[4NVg3OTh:L3G+
A549	M2OyPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7			NWraNpREcW6qaXLpeJMh[2WubDDndo94fGhiaX6geIlu\SCjbnSg[I9{\SCmZYDlcoRmdnRibXHucoVz	MnLoQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTZ6MUi2NVgoRjF4OEG4OlE5RC:jPh?=
3T3	MnfpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?			M{CxSmlEPTB;N{CwJOKyKDd6IH7N	NUjmNJF2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUWxO\|MxODhpPkG1NVc{ODB6PD;hQi=>
3T3/neu	NX34UnFrT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=			NHjse5JKSzVyPUOgxtEhOC5zNDDuUS=>	MkDBQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTVzN{OwNFgoRjF3MUezNFA5RC:jPh?=
SK-Br-3	M3rXe2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7			M3fMPWlEPTB;MjFCtUAxNjF6IH7N	M1TFTFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF3MUezNFA5Lz5zNUG3N\|AxQDxxYU6=
BT 474	NXvXO4Z7T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=			MYjJR\|UxRTJiwsGgNE4xPiCwTR?=	M3mzTFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF3MUezNFA5Lz5zNUG3N\|AxQDxxYU6=
A431	NWTaV\|NiT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=			M17aTmlEPTB;OEGgxtEhQSCwTR?=	M3;PelxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF3MUezNFA5Lz5zNUG3N\|AxQDxxYU6=
MDA-MB-435	MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?			M2\x[2lEPTB;OU[wJOKyKDF4NTDuUS=>	NImwSY49[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zNUG3N\|AxQCd-MUWxO\|MxODh:L3G+
SW620	MkLmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?			NXHkU2F6UUN3ME22PVAhyrFiOESgcm0>	NW\R[4p2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUWxO\|MxODhpPkG1NVc{ODB6PD;hQi=>
SKBR3	MnzxSpVv[3Srb36gZZN{[Xl?			NGXXXIhKdmirYnn0bY9vKG:oIHj1cYFvKEinckKgbY4hW0uEUkOgZ4VtdHNuIFXDOVAhRSByLkCwNkDPxE1w	NXTqeVJIRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUiwO\|c1OjVpPkG4NFc4PDJ3PD;hQi=>
BT474	M1j4SGZ2dmO2aX;uJIF{e2G7			MX\Jcohq[mm2aX;uJI9nKGi3bXHuJGhmejJiaX6gRnQ1PzRiY3XscJMtKEWFNUCgQUAxNjByMjFOwG0v	MmjKQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOThyN{e0NlUoRjF6MEe3OFI2RC:jPh?=
A431	MXXGeY5kfGmxbjDhd5NigQ>?			MWjJcohq[mm2aX;uJI9nKGi3bXHuJGhmejJiaX6gRVQ{OSClZXzsd{whTUN3MDC9JFAvODhzIN88UU4>	NF\sR5M9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOEC3O\|QzPSd-MUiwO\|c1OjV:L3G+
SW620	MkT1SpVv[3Srb36gZZN{[Xl?			MkOxTY5pcWKrdHnvckBw\iCqdX3hckBJ\XJ{IHnuJHNYPjJyIHPlcIx{NCCHQ{WwJF0hOC54OTFOwG0v	MYS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQDB5N{SyOUc,OThyN{e0NlU9N2F-
BA/F3	M3\XO2N6fG:2b4jpZ4l1gSCjc4PhfS=>			M{TSOGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KG2xdYPlJGJCN0Z\|IHPlcIx{KGW6cILld5NqdmdiRVfGVkBNQDV6UjDteZRidnRuIFnDOVAhRSByLkCwN\|Uh\|ryPLh?=	MUS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTJ\|OUKyPUc,OTl{M{myNlk9N2F-
BA/F3	NIrVVHREgXSxdH;4bYNqfHliYYPzZZk>			MUfDfZRwfG:6aXPpeJkh[WejaX7zeEBud3W\|ZTDCRU9HOyClZXzsd{BmgHC{ZYPzbY5oKEWJRmKgUFg2QFJxVEe5NG0hdXW2YX70MEBKSzVyIE2gNE4yQCEQvF2u	M1;uOlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7MkO5NlI6Lz5zOUKzPVIzQTxxYU6=
Sf9	NInW[JNHfW6ldHnvckBie3OjeR?=		M4Dm[\|ExKG2rboO=	M1zicWlvcGmkaYTpc44hd2ZiaIXtZY4hf2muZDD0fZBmKEWJRmKg[ZhxemW\|c3XkJIlvKFOoOTDj[YxteyC3c3nu[{Bc\2GvbXGzNnBeNUGWUDDh[pRmeiBzMDDtbY5{KGK7IIPjbY51cWyuYYTpc44h[2:3boTpcoctKEmFNUCgQUAxNjByMkWg{txONg>?	M2jERVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2OUCwOlQ{Lz5{NEmwNFY1OzxxYU6=
Sf9	MmXtSpVv[3Srb36gZZN{[Xl?		MlLGNVAhdWmwcx?=	M2rXdGlvcGmkaYTpc44hd2ZiaIXtZY4hTUeIUjDUO\|kxVS:OOEW4VkBufXSjboSg[ZhxemW\|c3XkJIlvKFOoOTDj[YxteyC3c3nu[{Bc\2GvbXGzNnBeNUGWUDDh[pRmeiBzMDDtbY5{KGK7IIPjbY51cWyuYYTpc44h[2:3boTpcoctKEmFNUCgQUAxNjB4NjFOwG0v	MnzXQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR7MEC2OFMoRjJ2OUCwOlQ{RC:jPh?=
BAF3	NFvidIhHfW6ldHnvckBie3OjeR?=		M3XmfVczKGi{cx?=	NWXXSHpPUW6qaXLpeIlwdiCxZjDU[Ywu\nW\|ZXSgTWdHOVJiKIXub45wf25ib4Lp[4lvMSCneIDy[ZN{\WRiaX6gcY92e2ViQlHGN{Bk\WyuczDhd5Nme3OnZDDhd{Boem:5dHigbY5pcWKrdHnvckBi\nSncjC3NkBpenNiYomgR4VtdFSrdHXyMWdtdyCjc4PhfUwhT0l3MDC9JFAvOTlizszNMi=>	NFf6W3U9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEK4NlEzOid-MkiyPFIyOjJ:L3G+
BAF3	M4D1fWZ2dmO2aX;uJIF{e2G7		MYS3NkBpenN?	M2faPGlvcGmkaYTpc44hd2ZiVHXsMYZ2e2WmIFnOV3IhMHWwa37ve44hd3KrZ3nuLUBmgHC{ZYPz[YQhcW5ibX;1d4UhSkGIMzDj[YxteyCjc4Pld5Nm\CCjczDndo94fGhiaX7obYJqfGmxbjDh[pRmeiB5MjDodpMh[nliQ3XscHRqfGW{LVfsc{Bie3OjeTygS2k2OCB;IECuNlkh\|ryPLh?=	Mk\lQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh{OEKxNlIoRjJ6MkiyNVIzRC:jPh?=
BAF3	NILCTIhIem:5dHigbY5pcWKrdHnvckBie3OjeR?=		MX63NkBpenN?	NIfQd3JIem:5dHigbY5pcWKrdHnvckBw\iCvb4Xz[UBDSUZ\|IHPlcIx{KGGodHXyJFczKGi{czDifUBE\WyuVHn0[ZIuT2yxIHHzd4F6NCCJSUWwJF0hOS57IN88UU4>	NFP2cYU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEK4NlEzOid-MkiyPFIyOjJ:L3G+

... Click to View More Cell Line Experimental Data

Assay

Methods	Test Index	PMID
Western blot	pHER2 / HER2 / pAKT / AKT / pERK / ERK ; PubMed: 24009064 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]	- 合并使用时间-分辨荧光分析无细胞自磷酸化: Neratinib 在DMSO 中制备成10 mg/mL 储液，然后在25 mM HEPES (pH 7.5; 0.002 ng/mL-20 μg/mL)中稀释。纯化重组的HER-2 COOH末端片段(第676-1255位氨基酸) 或EGFR COOH末端片段(第 645-1186位氨基酸)[在100 mM HEPES (pH 7.5) 和50% 甘油中稀释] 与浓度不断增高的Neratinib 在96-孔ELISA板上室温下温育15分钟，孔中含4 mM HEPES (pH 7.5), 0.4 mM MnCl₂, 20 μM 钒酸钠，及 0.2 mM DTT 。加入 40 μM ATP 和20 mM MgCl₂开始激酶反应，然后在室温下反应1小时。冲洗实验板, 使用铕标记的抗-磷酸化-酪氨酸抗体 (15 ng/每孔)检测磷酸化。冲洗后，使用Victor2 荧光读数仪 (激发波长为340 nm,发射波长为615 nm)测定信号。通过抑制曲线测定抑50%受体磷酸时的Neratinib 浓度 (IC50) 。
细胞实验：^[1]	- 合并 Cell lines: 3T3, 3T3/neu, A431, BT474, SK-Br-3, MDA-MB-435, 和SW480 Concentrations: 溶于DMSO, 终浓度为0.5 ng/mL-5 μg/mL Incubation Time: 2, 或6天 Method: 使用不同浓度Neratinib处理细胞 2, 或6 天。使用sulforhodamine B, 一种蛋白结合染料，测定细胞增殖。细胞与10% 三氯乙酸混合，然后使用水广泛冲洗。使用 0.1% sulforhodamine B对细胞进行染色，使用在5% 乙酸中清洗。蛋白-结合染10 mM Tris中,然后在450 nM处测定吸光度。通过抑制曲线测定抑制50% 细胞增殖时的Neratinib 浓度(IC50)。 (Only for Reference)
动物实验：^[1]	- 合并 Animal Models: 皮下移植3T3/neu, BT474, MCF-7, 或 SK-OV-3 细胞的雌性无胸腺裸鼠 Dosages: ~80 mg/kg/day Administration: 口服饲喂 (Only for Reference)

参考文献

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

溶解度 (25°C)

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

* 溶解度检测是由Selleck技术部门检测的，可能会和文献中提供的溶解度有所差异，这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。

化学数据 Download Neratinib (HKI-272) SDF

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
别名	N/A

动物体内配方计算器 (澄清溶液)

第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）

给药剂量

mg/kg

动物平均体重

每只动物给药体积

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

计算重置

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。

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。

计算器

摩尔浓度计算器

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为:

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)

摩尔浓度计算公式

质量

浓度

体积

分子量
=

×

×

*在配置溶液时，请务必参考Selleck产品标签上、SDS / COA（可在Selleck的产品页面获得）批次特异的分子量使用本工具。

稀释计算器

用本工具协助配置特定浓度的溶液，使用的计算公式为：

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入输出 )

C1

V1

C2

V2
×

=

×

在配置溶液时，请务必参考Selleck产品标签上、SDS / COA（可在Selleck的产品页面获得）批次特异的分子量使用本工具。.

连续稀释计算器方程

连续稀释
初始浓度:
稀释倍数:

计算结果

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):

分子量计算器

通过输入化合物的化学式来计算其分子量：

注：化学分子式大小写敏感。C10H16N2O2 c10h16n2o2

摩尔浓度计算器

质量	浓度	体积	分子量
=	×	×
计算

临床试验信息 (data from https://clinicaltrials.gov, updated on 2022-01-17)

NCT Number	Recruitment	interventions	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT04856475	Withdrawn	Drug: Neratinib	Breast Cancer\|Brain Metastases	Jules Bordet Institute	November 24 2021	Phase 2
NCT04781374	Recruiting	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
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 Inc.\|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

技术支持

在订购、运输、储存和使用我们的产品的任何阶段，您遇到的任何问题，均可以通过拨打我们的热线电话400-668-6834，或者技术支持邮箱tech@selleck.cn，直接联系到我们。我们会在24小时内尽快联系您。

操作手册

如果有其他问题，请给我们留言。

HER2 Signaling Pathway Map

HER2 Inhibitors with Unique Features

选择性强的HER2抑制剂

CP-724714 : HER2/ErbB2-selective, IC50=10 nM.
活性最高的HER2抑制剂

Mubritinib (TAK 165) : HER2/ErbB2, IC50=6 nM.
FDA批准的HER2抑制剂

Lapatinib : Approved by FDA for breast cancer.
经典的HER2抑制剂

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

研究领域

产品类型

定制您的化合物库

Neratinib (HKI-272)

客户使用Selleck生产的Neratinib (HKI-272)发表文献82篇：

产品安全说明书

HER2抑制剂选择性比较

生物活性

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)

参考文献

溶解度 (25°C)

化学数据 Download Neratinib (HKI-272) SDF

动物体内配方计算器 (澄清溶液)

计算器

摩尔浓度计算器

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)

摩尔浓度计算公式

稀释计算器

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

连续稀释计算器方程

连续稀释

计算结果

分子量计算器

总分子量：g/mol

摩尔浓度计算器

临床试验信息 (data from https://clinicaltrials.gov, updated on 2022-01-17)

技术支持

HER2 Signaling Pathway Map

HER2 Inhibitors with Unique Features

相关HER2产品