Lorlatinib (PF-6463922)

For research use only. Not for use in humans.

目录号：S7536 中文名称：劳拉替尼

Lorlatinib (PF-6463922) Chemical Structure

CAS No. 1454846-35-5

Lorlatinib (PF-6463922)是一个强效的，双重 ALK/ROS1 的抑制剂，对ROS1, ALK (WT), 以及ALK (L1196M)的K_i分别为<0.02 nM, <0.07 nM, 和0.7 nM。PF-06463922 可诱导凋亡。Phase 1。

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价格

库存

购买数量

10mM (1mL in DMSO)	RMB 2432.43	现货
5mg	RMB 1622.95	现货
25mg	RMB 6531.11	现货
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客户使用Selleck生产的Lorlatinib (PF-6463922)发表文献25篇：

Nature, 2019, 10.1038/s41586-019-1472-0

PubMed: 31391581 ( click the link to review the publication )

EMBO J, 2021, e105784

PubMed: 33411331 ( click the link to review the publication )

Clin Cancer Res, 2020, 8

PubMed: 32269053 ( click the link to review the publication )

Cell Rep, 2020, 32(12):108171

PubMed: 32966799 ( click the link to review the publication )

Cancer Discov, 2020, 1 pii: CD-19-1030

PubMed: 32238360 ( click the link to review the publication )

Front Immunol, 2020, 11:527750

PubMed: 33324391 ( click the link to review the publication )

Lung Cancer, 2020, 144:20-29

PubMed: 32353632 ( click the link to review the publication )

Acta Pharmacol Sin, 2020, 10.1038/s41401-020-00513-3

PubMed: 32918045 ( click the link to review the publication )

Bosn J Basic Med Sci, 2020, 10.17305/bjbms.2020.5066

PubMed: 33091333 ( click the link to review the publication )

NPJ Precis Oncol, 2020, 4:21

PubMed: 32802958 ( click the link to review the publication )

J Thorac Oncol, 2020, 15(5):752-765

PubMed: 31972351 ( click the link to review the publication )

EMBO Mol Med, 2019, 10.15252/emmm.201910581

PubMed: 31633304 ( click the link to review the publication )

Clin Cancer Res, 2019, 10.1158/1078-0432.CCR-19-1104

PubMed: 31585938 ( click the link to review the publication )

Oncogene, 2019, 101038/s41388-019-1136-4

PubMed: 31804622 ( click the link to review the publication )

Invest New Drugs, 2019, 10.1007/s10637-019-00795-3

PubMed: 31124056 ( click the link to review the publication )

Biochem Biophys Res Commun, 2019, 511(2):260-265

PubMed: 30791979 ( click the link to review the publication )

Sci Signal, 2018, 11(557)

PubMed: 30459283 ( click the link to review the publication )

Mol Cancer Ther, 2018, 17(11-:2271-2284

PubMed: 30135214 ( click the link to review the publication )

Mol Cancer Res, 2018, 10.1158/1541-7786.MCR-18-0171

PubMed: 30002191 ( click the link to review the publication )

Cancer Discov, 2018, 8(6):714-729

PubMed: 29650534 ( click the link to review the publication )

Biochem Biophys Res Commun, 2018, 501(1):246-252

PubMed: 29723525 ( click the link to review the publication )

Cell Rep, 2017, 21(11):3298-3309

PubMed: 29241554 ( click the link to review the publication )

Int J Oncol, 2017, 51(5):1533-1540

PubMed: 29048652 ( click the link to review the publication )

Cancer Discov, 2016, 6(10):1118-1133

PubMed: 27432227 ( click the link to review the publication )
Oncotarget, 2016, 7(52):87301-87311

PubMed: 27888620 ( click the link to review the publication )

产品安全说明书

ALK抑制剂选择性比较

生物活性

产品描述

靶点

ROS1 ^[1] (Cell-free assay)	ALK ^[1] (Cell-free assay)	ALK (L1196M) ^[1] (Cell-free assay)	LTK (TYK1) ^[1] (Cell-free assay)	FER ^[1] (Cell-free assay)	点击更多
<0.02 nM(Ki)	<0.07 nM(Ki)	0.07 nM(Ki)	2.7 nM	3.3 nM	点击更多

体外研究

PF-06463922对ALK和大量ALK临床突变型表现出显著的细胞活性，IC50范围为0.2 nM-77 nM。^[1]在含有SLC34A2-ROS1 融合物的HCC78人NSCLC细胞和表达人CD74-ROS1的BaF3-CD74-ROS1细胞中，PF-06463922显著抑制细胞增殖，并诱导细胞凋亡。^[2] 在含有非突变型ALK或突变型ALK融合物的NSCLC 细胞中，PF-06463922也表现出有效的生长抑制活性，并诱导细胞凋亡。^[3]

Cell Data

Cell Lines	Assay Type	Incubation Time	Activity Description	PMID
NIH-3T3	M3vKXmZ2dmO2aX;uJIF{e2G7	MXexJIhz	NVvGRnlLUW6qaXLpeIlwdiCxZjDoeY1idiCHTVy0MYZ2e2WmIFHMT{BHOTF5NFygcZV1[W62IHX4dJJme3OnZDDpckBud3W\|ZTDOTWguO1R\|IHPlcIx{KGG\|c3Xzd4VlKGG\|IIDoc5NxcG9vQVzLJIxmfmWuIHHmeIVzKDFiaIKgZpkhe2GwZIfpZ4ghTUyLU1GsJGlEPTBiPTCwMlAxODJizszNMi=>	M2jNd\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2OEG5NVE3Lz5{NEixPVEyPjxxYU6=
NIH/3T3	MXLGeY5kfGmxbjDhd5NigQ>?		Mmf6TY5pcWKrdHnvckBw\iC5aXzkJJR6eGViRV3MOE9CVEtiRkGxO\|RNKG23dHHueEApfW6tbn;3ckBwemmpaX6pJIV5eHKnc4Pl[EBqdiCQSVivN3Q{KGOnbHzzMEBKSzVyIE2gNE4xODB{IN88UU4>	MUO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDR\|MUO0NEc,Ojh2M{GzOFA9N2F-
BAF3	MXHBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>?	MWq3NkBpenN?	NEnnNoNCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JI1wfXOnIFLBSlMh[2WubIOgbIFz[m:{aX7nJGNFPzRvUl;TNUBi\nSncjC3NkBpenNiYomgV3JDKG:{IFPDT\|gh[XO\|YYmsJGlEPTBiPTCwMlAxOTJizszNMi=>	MoXoQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl{OEi5OFAoRjJ7Mki4PVQxRC:jPh?=
NIH-3T3	NEPVWXFHfW6ldHnvckBie3OjeR?=	MmDwNUBpeg>?	NVXRUodTUW6qaXLpeIlwdiCxZjD3bYxlKHS7cHWgbJVu[W5iRV3MOE1nfXOnZDDBUGsh\XiycnXzd4VlKGmwIH3veZNmKE6LSD2zWFMh[2WubIOgZZN{\XO\|ZXSgZZMheGixc4Doc5J6dGG2ZXSgRWxMKGyndnXsJIFnfGW{IEGgbJIh[nlic3Hu[Jdq[2hiRVzJV2EtKEmFNUCgQUAxNjByMUOg{txONg>?	NUjid4xERGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS4NVkyOTZpPkK0PFE6OTF4PD;hQi=>
NIH/3T3	NYD5[4lrTnWwY4Tpc44h[XO\|YYm=		NFvmR5ZKdmirYnn0bY9vKG:oIIfpcIQhfHmyZTDFUWw1N0GOSzCoeY5sdm:5bjDvdolocW5rIHX4dJJme3OnZDDpckBPUUhxM2SzJINmdGy\|LDDJR\|UxKD1iMD6wNFE{KM7:TT6=	MXG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDR\|MUO0NEc,Ojh2M{GzOFA9N2F-
NIH-3T3	NGLXepRHfW6ldHnvckBie3OjeR?=	MkTJNUBpeg>?	M1izWGlvcGmkaYTpc44hd2ZiaIXtZY4hTU2OND3meZNm\CCDTFugR\|EyPT[\IH31eIFvfCCneIDy[ZN{\WRiaX6gcY92e2ViTlnIMVNVOyClZXzsd{Bie3Onc4Pl[EBieyCyaH;zdIhwNUGOSzDs[ZZmdCCjZoTldkAyKGi{IHL5JJNidmS5aXPoJGVNUVODLDDJR\|UxKD1iMD6wNFE3KM7:TT6=	MmLwQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR6MUmxNVYoRjJ2OEG5NVE3RC:jPh?=
NIH/3T3	NVn2TmQxTnWwY4Tpc44h[XO\|YYm=		MYXJcohq[mm2aX;uJI9nKHerbHSgeJlx\SCHTVy0M2FNUyCFMUG1OnkhdXW2YX70JEh2dmuwb4fuJI9zcWerbjmg[ZhxemW\|c3XkJIlvKE6LSD:zWFMh[2WubIOsJGlEPTBiPTCwMlAxOTZizszNMi=>	MnHEQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh2M{GzOFAoRjJ6NEOxN\|QxRC:jPh?=
BAF3	MVvBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>?	MXq3NkBpenN?	MXPBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IH3veZNmKEKDRkOgZ4VtdHNiaHHyZo9zcW6pIFXNUFQuSUyNIHHmeIVzKDd{IHjyd{BjgSCVUlKgc5IhS0ONODDhd5NigSxiSVO1NEA:KDBwMECyPUDPxE1w	NFrPcnY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUK4PFk1OCd-MkmyPFg6PDB:L3G+
KARPAS299	M4fWZ2FvfGmycn;sbYZmemG2aY\lJIF{e2G7	MVq3NkBpenN?	Ml7aRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6\|dDDoeY1idiCNQWLQRXMzQTliY3XscJMhcGG{Yn;ybY5oKE6STT3BUGsh[W[2ZYKgO\|IhcHK\|IHL5JHNTSiCxcjDDR2s5KGG\|c3H5MEBKSzVyIE2gNE4xODNizszNMi=>	NGHa[FY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUK4PFk1OCd-MkmyPFg6PDB:L3G+
NIH-3T3	Ml3ZSpVv[3Srb36gZZN{[Xl?	MYmxJIhz	NXuyWYM3UW6qaXLpeIlwdiCxZjDoeY1idiCHTVy0MYZ2e2WmIFHMT{BUOTJyNmmgcZV1[W62IHX4dJJme3OnZDDpckBud3W\|ZTDOTWguO1R\|IHPlcIx{KGG\|c3Xzd4VlKGG\|IIDoc5NxcG9vQVzLJIxmfmWuIHHmeIVzKDFiaIKgZpkhe2GwZIfpZ4ghTUyLU1GsJGlEPTBiPTCwMlAxPDJizszNMi=>	M1vRWVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2OEG5NVE3Lz5{NEixPVEyPjxxYU6=
NIH/3T3	NEfEeGRHfW6ldHnvckBie3OjeR?=		NIrIPHNKdmirYnn0bY9vKG:oIIfpcIQhfHmyZTDFUWw1N0GOSzDTNVIxPllibYX0ZY51KCi3bnvuc5dvKG:{aXfpckkh\XiycnXzd4VlKGmwIF7JTE8{XDNiY3XscJMtKEmFNUCgQUAxNjByNEKg{txONg>?	MWq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDR\|MUO0NEc,Ojh2M{GzOFA9N2F-
SU-DHL1	NGTsPYFCdnSrcILvcIln\XKjdHn2[UBie3OjeR?=	NFOyVYQ4OiCqcoO=	MWjBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFOXLVTIUFEh[2WubIOgbIFz[m:{aX7nJG5RVS2DTFugZYZ1\XJiN{KgbJJ{KGK7IGPSRkBweiCFQ1u4JIF{e2G7LDDJR\|UxKD1iMD6wNFQ6KM7:TT6=	MmDxQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl{OEi5OFAoRjJ7Mki4PVQxRC:jPh?=
NCI-H3122	MUnBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>?	MnrwO\|IhcHK\|	M1jQfWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTlPJMWg{OTJ{IHPlcIx{KGGodHXyJFczKGi{czDifUBUWkJib4KgR2NMQCCjc4PhfUwhUUN3MDC9JFAvODB5ODFOwG0v	MmXpQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl{OEi5OFAoRjJ7Mki4PVQxRC:jPh?=
NIH-3T3	NVHLN4t5TnWwY4Tpc44h[XO\|YYm=	NYTFUHFqOSCqch?=	MUPJcohq[mm2aX;uJI9nKGi3bXHuJGVOVDRvZoXz[YQhSUyNIFyxNVUzWiCvdYThcpQh\XiycnXzd4VlKGmwIH3veZNmKE6LSD2zWFMh[2WubIOgZZN{\XO\|ZXSgZZMheGixc4Doc{1CVEtibHX2[Ywh[W[2ZYKgNUBpeiCkeTDzZY5lf2mlaDDFUGlUSSxiSVO1NEA:KDBwMEC5JO69VS5?	M3zzdVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2OEG5NVE3Lz5{NEixPVEyPjxxYU6=
NIH/3T3	MWPGeY5kfGmxbjDhd5NigQ>?		NUPvOYRwUW6qaXLpeIlwdiCxZjD3bYxlKHS7cHWgSW1NPC:DTFugUFEyPTKUIH31eIFvfCBqdX7rco94diCxcnnnbY4qKGW6cILld5Nm\CCrbjDOTWgwO1R\|IHPlcIx{NCCLQ{WwJF0hOC5yMEmg{txONg>?	Mo\mQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh2M{GzOFAoRjJ6NEOxN\|QxRC:jPh?=
NIH-3T3	MlS4SpVv[3Srb36gZZN{[Xl?	M2\pNlEhcHJ?	MXHJcohq[mm2aX;uJI9nKGi3bXHuJGVOVDRvZoXz[YQhSUyNIFexNlY6SSCvdYThcpQh\XiycnXzd4VlKGmwIH3veZNmKE6LSD2zWFMh[2WubIOgZZN{\XO\|ZXSgZZMheGixc4Doc{1CVEtibHX2[Ywh[W[2ZYKgNUBpeiCkeTDzZY5lf2mlaDDFUGlUSSxiSVO1NEA:KDBwMEG1JO69VS5?	NVWzR5lFRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS4NVkyOTZpPkK0PFE6OTF4PD;hQi=>
NIH/3T3	NV3OT3M3TnWwY4Tpc44h[XO\|YYm=		M1fpTmlvcGmkaYTpc44hd2Zid3ns[EB1gXCnIFXNUFQwSUyNIFexNlY6SSCvdYThcpQhMHWwa37ve44hd3KrZ3nuLUBmgHC{ZYPz[YQhcW5iTlnIM\|NVOyClZXzsd{whUUN3MDC9JFAvODF3IN88UU4>	NEThWFU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OESzNVM1OCd-Mki0N\|E{PDB:L3G+
NIH-3T3	MoLxSpVv[3Srb36gZZN{[Xl?	M2m2bVEhcHJ?	NHfTfWxKdmirYnn0bY9vKG:oIHj1cYFvKEWPTESt[pV{\WRiQVzLJGwyOTl4TTDteZRidnRiZYjwdoV{e2WmIHnuJI1wfXOnIF7JTE0{XDNiY3XscJMh[XO\|ZYPz[YQh[XNicHjvd5Bpdy2DTFugcIV3\WxiYX\0[ZIhOSCqcjDifUB{[W6md3njbEBGVEmVQTygTWM2OCB;IECuNFIyKM7:TT6=	MW[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDhzOUGxOkc,OjR6MUmxNVY9N2F-
NIH/3T3	NFfxSZlHfW6ldHnvckBie3OjeR?=		NVLiPZBjUW6qaXLpeIlwdiCxZjD3bYxlKHS7cHWgSW1NPC:DTFugUFEyQT[PIH31eIFvfCBqdX7rco94diCxcnnnbY4qKGW6cILld5Nm\CCrbjDOTWgwO1R\|IHPlcIx{NCCLQ{WwJF0hOC5yMkGg{txONg>?	NHzCbms9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OESzNVM1OCd-Mki0N\|E{PDB:L3G+
NIH-3T3	NUnNdYgyTnWwY4Tpc44h[XO\|YYm=	M3i1UlEhcHJ?	MkDrTY5pcWKrdHnvckBw\iCqdX3hckBGVUx2LX\1d4VlKEGOSzCxNVUyXGmwczDteZRidnRiZYjwdoV{e2WmIHnuJI1wfXOnIF7JTE0{XDNiY3XscJMh[XO\|ZYPz[YQh[XNicHjvd5Bpdy2DTFugcIV3\WxiYX\0[ZIhOSCqcjDifUB{[W6md3njbEBGVEmVQTygTWM2OCB;IECuNFM5KM7:TT6=	NVv3PG1QRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS4NVkyOTZpPkK0PFE6OTF4PD;hQi=>
NIH/3T3	M3jnbmZ2dmO2aX;uJIF{e2G7		M1zn[GlvcGmkaYTpc44hd2Zid3ns[EB1gXCnIFXNUFQwSUyNIEGxOVFVcW6\|IH31eIFvfCBqdX7rco94diCxcnnnbY4qKGW6cILld5Nm\CCrbjDOTWgwO1R\|IHPlcIx{NCCLQ{WwJF0hOC5yM{ig{txONg>?	NHTWOIQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OESzNVM1OCd-Mki0N\|E{PDB:L3G+
BAF3	NWj0c\|VrSW62aYDyc4xq\mW{YYTpeoUh[XO\|YYm=	MWi3NkBpenN?	MVvBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IH3veZNmKEKDRkOgZ4VtdHNiaHHyZo9zcW6pIFXNUFQuSUyNIFyxNVk3VSCvdYThcpQh[W[2ZYKgO\|IhcHK\|IHL5JHNTSiCxcjDDR2s5KGG\|c3H5MEBKSzVyIE2gNE4xPDJ2IN88UU4>	NGrJZ489[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUK4PFk1OCd-MkmyPFg6PDB:L3G+
NIH-3T3	NXvVPFRPTnWwY4Tpc44h[XO\|YYm=	NXjybnBGOSCqch?=	MULJcohq[mm2aX;uJI9nKGi3bXHuJGVOVDRvZoXz[YQhSUyNIFexNlAzWiCvdYThcpQh\XiycnXzd4VlKGmwIH3veZNmKE6LSD2zWFMh[2WubIOgZZN{\XO\|ZXSgZZMheGixc4Doc{1CVEtibHX2[Ywh[W[2ZYKgNUBpeiCkeTDzZY5lf2mlaDDFUGlUSSxiSVO1NEA:KDBwMEe3JO69VS5?	MYm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDhzOUGxOkc,OjR6MUmxNVY9N2F-
NIH/3T3	NHjKO2lHfW6ldHnvckBie3OjeR?=		NU[xc5BSUW6qaXLpeIlwdiCxZjD3bYxlKHS7cHWgSW1NPC:DTFugS\|EzODKUIH31eIFvfCBqdX7rco94diCxcnnnbY4qKGW6cILld5Nm\CCrbjDOTWgwO1R\|IHPlcIx{NCCLQ{WwJF0hOC5yN{eg{txONg>?	Mlm1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh2M{GzOFAoRjJ6NEOxN\|QxRC:jPh?=
BAF3	MVnBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>?	NInmdoo4OiCqcoO=	MYTBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IH3veZNmKEKDRkOgZ4VtdHNiaHHyZo9zcW6pIFXNUFQuSUyNIFexNlAzWiCvdYThcpQh[W[2ZYKgO\|IhcHK\|IHL5JHNTSiCxcjDDR2s5KGG\|c3H5MEBKSzVyIE2gNE4zKM7:TT6=	MlfkQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl{OEi5OFAoRjJ7Mki4PVQxRC:jPh?=
BAF3	M2HDRWFvfGmycn;sbYZmemG2aY\lJIF{e2G7	M3js[VczKGi{cx?=	NGrRfFlCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JI1wfXOnIFLBSlMh[2WubIOgbIFz[m:{aX7nJGNFPzRvUl;TNUBIOjB\|MmKgcZV1[W62IHHmeIVzKDd{IHjyd{BjgSCVUlKgc5IhS0ONODDhd5NigSxiSVO1NEA:KDBwMk[yJO69VS5?	Moi5QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl{OEi5OFAoRjJ7Mki4PVQxRC:jPh?=
HCC78	MVLBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>?	MXm3NkBpenN?	NUPUN3ZrSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDIR2M4QCClZXzsd{Bp[XKkb4LpcochW0yFM{TBNk1TV1NzIHHmeIVzKDd{IHjyd{BjgSCVUlKgc5IhS0ONODDhd5NigSxiSVO1NEA:KDBwM{W3JO69VS5?	M33PXVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7Mki4PVQxLz5{OUK4PFk1ODxxYU6=
SU-DHL1	NH\LTlJHfW6ldHnvckBie3OjeR?=		Mn3vTY5pcWKrdHnvckBw\iCDTFugbY4hcHWvYX6gV3UuTEiOMTDj[YxteyCjc4Pld5Nm\CCjczDy[YR2[3Srb36gbY4hW1SDVEOgdIhwe3Cqb4L5cIF1cW:wIHH0JHk4ODVicnXzbYR2\SCjdDCyNEB1dyB6MDDuUUBi\nSncjCxJIhzKGK7IGfld5Rmem5iYnzveEBidmGueYPpdy=>	NHi4[ZY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUK4PFk1OCd-MkmyPFg6PDB:L3G+
SU-DHL1	NIfJSnBHfW6ldHnvckBie3OjeR?=		MmnLTY5pcWKrdHnvckBw\iCDTFugbY4hcHWvYX6gV3UuTEiOMTDj[YxteyCjc4Pld5Nm\CCjczDy[YR2[3Srb36gbY4hSWu2IIDoc5NxcG:{eXzheIlwdiCjdDDTOFc{KHKnc3nkeYUh[XRiMkCgeI8hQDBibl2gZYZ1\XJiMTDodkBjgSCZZYP0[ZJvKGKub4SgZY5idHm\|aYO=	NYTrVXVCRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkmyPFg6PDBpPkK5Nlg5QTRyPD;hQi=>
SU-DHL1	MVHGeY5kfGmxbjDhd5NigQ>?		M1m2ZWlvcGmkaYTpc44hd2ZiQVzLJJBpd3OyaH;yfYxifGmxbjDheEB[OTJ5ODDy[ZNq\HWnIHnuJIh2dWGwIGPVMWRJVDFiY3XscJMh[XRiMkCgeI8hQDBibl2gZYZ1\XJiMTDodkBjgSCZZYP0[ZJvKGKub4SgZY5idHm\|aYO=	MkDxQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl{OEi5OFAoRjJ7Mki4PVQxRC:jPh?=
SU-DHL1	M13NUWZ2dmO2aX;uJIF{e2G7		MUDJcohq[mm2aX;uJI9nKEGOSzDpckBpfW2jbjDTWU1FUExzIHPlcIx{KGG\|c3Xzd4VlKGG\|IILl[JVkfGmxbjDpckBGWkticHjvd5Bpd3K7bHH0bY9vKGG2IGSyNFIwN1l{MESgdoV{cWS3ZYOgZZQhOjBidH:gPFAhdk1iYX\0[ZIhOSCqcjDifUBY\XO2ZYLuJIJtd3RiYX7hcJl{cXN?	MX68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTJ6OEm0NEc,Ojl{OEi5OFA9N2F-
NCI-H3122	NEfvdm5HfW6ldHnvckBie3OjeR?=		MWPJcohq[mm2aX;uJI9nKEGOSzDwbI9{eGixconsZZRqd25iYYSgXVEzPzhicnXzbYR2\SCrbjDoeY1idiCQQ1mtTFMyOjJiY3XscJMh[XRiMkCgeI8hQDBibl2gZYZ1\XJiMTDodkBjgSCZZYP0[ZJvKGKub4SgZY5idHm\|aYO=	MVS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTJ6OEm0NEc,Ojl{OEi5OFA9N2F-
NCI-H3122	NHzSS\|ZHfW6ldHnvckBie3OjeR?=		NGH0b5FKdmirYnn0bY9vKG:oIFHMT{BqdiCqdX3hckBPS0lvSEOxNlIh[2WubIOgZZN{\XO\|ZXSgZZMhemWmdXP0bY9vKGmwIGPURXQ{KHCqb4PwbI9zgWyjdHnvckBifCC\N{C1JJJme2mmdXWgZZQhOjBidH:gPFAhdk1iYX\0[ZIhOSCqcjDifUBY\XO2ZYLuJIJtd3RiYX7hcJl{cXN?	NI\1OYM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUK4PFk1OCd-MkmyPFg6PDB:L3G+
NCI-H3122	MVnGeY5kfGmxbjDhd5NigQ>?		MVTJcohq[mm2aX;uJI9nKEGOSzDpckBpfW2jbjDOR2kuUDNzMkKgZ4VtdHNiYYPz[ZN{\WRiYYOgdoVlfWO2aX;uJIlvKEGtdDDwbI9{eGixconsZZRqd25iYYSgV\|Q4OyC{ZYPp[JVmKGG2IEKwJJRwKDhyIH7NJIFnfGW{IEGgbJIh[nliV3XzeIVzdiCkbH;0JIFv[Wy7c3nz	NGrZV2w9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUK4PFk1OCd-MkmyPFg6PDB:L3G+
NCI-H3122	M{jsOWZ2dmO2aX;uJIF{e2G7		NVPZWYg5UW6qaXLpeIlwdiCxZjDBUGshcW5iaIXtZY4hVkOLLVizNVIzKGOnbHzzJIF{e2W\|c3XkJIF{KHKnZIXjeIlwdiCrbjDFVmsheGixc4Doc5J6dGG2aX;uJIF1KFR{MEKvM3kzODRicnXzbYR2\XNiYYSgNlAhfG9iOECgcm0h[W[2ZYKgNUBpeiCkeTDX[ZN1\XKwIHLsc5Qh[W6jbInzbZM>	NYL4OpU6RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkmyPFg6PDBpPkK5Nlg5QTRyPD;hQi=>

... Click to View More Cell Line Experimental Data

Assay

Methods	Test Index	PMID
Western blot	p-ALK / ALK; PubMed: 29650534 Cancer Discov ALK phosphorylation in the same Ba/F3 models treated with lorlatinib, as assessed by immunoblotting of cell lysates. Lorlatinib potently suppresses ALK activation in non-mutant and single mutant EML4-ALK models, but fails to inhibit ALK in Ba/F3 cells expressing the compound mutant.	29650534

体内研究

在大鼠体内，PF-06463922显示出低血浆清除率，适度的分布容积，合理的半衰期，对低P-糖蛋白1介导的外排敏感性低，且生物利用度为100%。^[1]在体内，表达人CD74-ROS1 和 Fig-ROS1的NIH3T3异种移植模型中，PF-06463922表现出细胞减少性抗癌作用，通过抑制ROS1磷酸化和下游信号分子，以及对肿瘤中细胞周期蛋白D1的抑制发挥作用。^[2]在负荷肿瘤移植物，过表达EML4-ALK，EML4-ALK-L1196M，EML4-ALK-G1269A，EML4-ALK-G1202R 或NPM-ALK的小鼠体内，PF-06463922也表现出显著的抗肿瘤活性。^[3]

参考文献

溶解度 (25°C)

体外	DMSO	81 mg/mL warmed (199.3 mM)
	Water	Insoluble
	Ethanol	'30 mg/mL warmed
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)： 2% DMSO+30% PEG 300+ddH2O	5mg/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 Lorlatinib (PF-6463922) SDF

分子量	406.41
化学式	C₂₁H₁₉FN₆O₂
CAS号	1454846-35-5
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、MSDS / 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、MSDS / 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 2020-01-06)

NCT Number	Recruitment	interventions	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT03726333	Recruiting	Drug: lorlatinib	Advanced Cancers	Pfizer	January 14 2020	Phase 1
NCT03505554	Recruiting	Drug: Lorlatinib	Anaplastic Large Cell Lymphoma ALK-Positive	University of Milano Bicocca\|Pfizer	October 10 2017	Phase 2
NCT03107988	Recruiting	Drug: Lorlatinib\|Drug: Cyclophosphamide\|Drug: Topotecan	Neuroblastoma	New Approaches to Neuroblastoma Therapy Consortium\|Pfizer\|University of Southern California\|Solving Kids'' Cancer US/EU\|Children''s Neuroblastoma Cancer Foundation\|The Band of Parents\|The Evan Foundation\|Wade''s Army\|Ronan Thompson Foundation\|The Catherine Elizabeth Blair Memorial Foundation\|Cookies for Kids'' Cancer	September 1 2017	Phase 1
NCT03184168	Completed	Drug: [14C]lorlatinib	Healthy Volunteers	Pfizer	July 5 2017	Phase 1
NCT03439215	Unknown status	Drug: Lorlatinib	Carcinoma Non-Small-Cell Lung	Fondazione Ricerca Traslazionale\|Clinical Research Technology S.r.l.	June 13 2017	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。

常见问题及建议解决方法

问题 1：
Do you have any special suggestions for solution of S7536, Lorlatinib (PF-6463922) to be applied to mouse models?
回答：
For S7536, we recommend 2% DMSO+30% PEG 300+ddH2O (up to 5mg/ml) for in vivo application.

研究领域

产品类型

定制您的化合物库

Lorlatinib (PF-6463922)

客户使用Selleck生产的Lorlatinib (PF-6463922)发表文献25篇：

产品安全说明书

ALK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 Lorlatinib (PF-6463922) 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 2020-01-06)

技术支持

常见问题及建议解决方法

ALK Signaling Pathway Map

相关ALK产品