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Lorlatinib (PF-6463922)

目录号：S7536 中文名称：劳拉替尼

仅限科研使用

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。

Lorlatinib (PF-6463922) Chemical Structure

CAS: 1454846-35-5

规格	价格	库存
10mM (1mL in DMSO)	RMB 1875.51	现货
5mg	RMB 1056.51	现货
25mg	RMB 3169.53	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Lorlatinib (PF-6463922)发表文献44篇：

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	Concentration	Incubation Time	Formulation	Activity Description	PMID

NIH-3T3	NI[1[GtHfW6ldHnvckBie3OjeR?=	MVexJIhz	NVyz[nZRUW6qaXLpeIlwdiCxZjDoeY1idiCHTVy0MYZ2e2WmIFHMT{BHOTF5NFygcZV1[W62IHX4dJJme3OnZDDpckBud3W\|ZTDOTWguO1R\|IHPlcIx{KGG\|c3Xzd4VlKGG\|IIDoc5NxcG9vQVzLJIxmfmWuIHHmeIVzKDFiaIKgZpkhe2GwZIfpZ4ghTUyLU1GsJGlEPTBiPTCwMlAxODJizszNMi=>	MoXhQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR6MUmxNVYoRjJ2OEG5NVE3RC:jPh?=
NIH/3T3	MXLGeY5kfGmxbjDhd5NigQ>?		NYn3eJpyUW6qaXLpeIlwdiCxZjD3bYxlKHS7cHWgSW1NPC:DTFugSlEyPzSOIH31eIFvfCBqdX7rco94diCxcnnnbY4qKGW6cILld5Nm\CCrbjDOTWgwO1R\|IHPlcIx{NCCLQ{WwJF0hOC5yMECyJO69VS5?	NGHUO4U9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OESzNVM1OCd-Mki0N\|E{PDB:L3G+
BAF3	NYSySHJiSW62aYDyc4xq\mW{YYTpeoUh[XO\|YYm=	MlHuO\|IhcHK\|	MnfURY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6\|dDDtc5V{\SCEQV[zJINmdGy\|IHjhdoJwemmwZzDDSFc1NVKRU{GgZYZ1\XJiN{KgbJJ{KGK7IGPSRkBweiCFQ1u4JIF{e2G7LDDJR\|UxKD1iMD6wNFEzKM7:TT6=	NWXZb25sRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkmyPFg6PDBpPkK5Nlg5QTRyPD;hQi=>
NIH-3T3	MmLFSpVv[3Srb36gZZN{[Xl?	M3nzflEhcHJ?	M2LpTmlvcGmkaYTpc44hd2Zid3ns[EB1gXCnIHj1cYFvKEWPTESt[pV{\WRiQVzLJIV5eHKnc4Pl[EBqdiCvb4Xz[UBPUUhvM2SzJINmdGy\|IHHzd4V{e2WmIHHzJJBpd3OyaH;yfYxifGWmIFHMT{Bt\X[nbDDh[pRmeiBzIHjyJIJ6KHOjbnT3bYNpKEWOSWPBMEBKSzVyIE2gNE4xODF\|IN88UU4>	MYW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDhzOUGxOkc,OjR6MUmxNVY9N2F-
NIH/3T3	MYLGeY5kfGmxbjDhd5NigQ>?		MmDyTY5pcWKrdHnvckBw\iC5aXzkJJR6eGViRV3MOE9CVEtiKIXub45wf25ib4Lp[4lvMSCneIDy[ZN{\WRiaX6gUmlJNzOWMzDj[YxteyxiSVO1NEA:KDBwMECxN{DPxE1w	NVKxbm02RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMki0N\|E{PDBpPkK4OFMyOzRyPD;hQi=>
NIH-3T3	MXvGeY5kfGmxbjDhd5NigQ>?	NHv2XZYyKGi{	Mo\kTY5pcWKrdHnvckBw\iCqdX3hckBGVUx2LX\1d4VlKEGOSzDDNVE2PllibYX0ZY51KGW6cILld5Nm\CCrbjDtc5V{\SCQSVitN3Q{KGOnbHzzJIF{e2W\|c3XkJIF{KHCqb4PwbI8uSUyNIHzleoVtKGGodHXyJFEhcHJiYomgd4Fv\HerY3igSWxKW0FuIFnDOVAhRSByLkCwNVYh\|ryPLh?=	M3fJcVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2OEG5NVE3Lz5{NEixPVEyPjxxYU6=
NIH/3T3	M1PG[GZ2dmO2aX;uJIF{e2G7		Mmf0TY5pcWKrdHnvckBw\iC5aXzkJJR6eGViRV3MOE9CVEtiQ{GxOVZ[KG23dHHueEApfW6tbn;3ckBwemmpaX6pJIV5eHKnc4Pl[EBqdiCQSVivN3Q{KGOnbHzzMEBKSzVyIE2gNE4xODF4IN88UU4>	NF:0Vnc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OESzNVM1OCd-Mki0N\|E{PDB:L3G+
BAF3	M3zXfGFvfGmycn;sbYZmemG2aY\lJIF{e2G7	MYW3NkBpenN?	M17tcmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgcY92e2ViQlHGN{Bk\WyuczDoZZJjd3KrbnegSW1NPC2DTFugZYZ1\XJiN{KgbJJ{KGK7IGPSRkBweiCFQ1u4JIF{e2G7LDDJR\|UxKD1iMD6wNFI6KM7:TT6=	M{Pm[VxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7Mki4PVQxLz5{OUK4PFk1ODxxYU6=
KARPAS299	NVzGWnZLSW62aYDyc4xq\mW{YYTpeoUh[XO\|YYm=	Mlz4O\|IhcHK\|	M1nje2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iS1HSVGFUOjl7IHPlcIx{KGijcnLvdolv\yCQUF2tRWxMKGGodHXyJFczKGi{czDifUBUWkJib4KgR2NMQCCjc4PhfUwhUUN3MDC9JFAvODB\|IN88UU4>	NWfKSFJpRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkmyPFg6PDBpPkK5Nlg5QTRyPD;hQi=>
NIH-3T3	MWLGeY5kfGmxbjDhd5NigQ>?	Moi0NUBpeg>?	NYPyU3ROUW6qaXLpeIlwdiCxZjDoeY1idiCHTVy0MYZ2e2WmIFHMT{BUOTJyNmmgcZV1[W62IHX4dJJme3OnZDDpckBud3W\|ZTDOTWguO1R\|IHPlcIx{KGG\|c3Xzd4VlKGG\|IIDoc5NxcG9vQVzLJIxmfmWuIHHmeIVzKDFiaIKgZpkhe2GwZIfpZ4ghTUyLU1GsJGlEPTBiPTCwMlAxPDJizszNMi=>	MVu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDhzOUGxOkc,OjR6MUmxNVY9N2F-
NIH/3T3	M4jwfmZ2dmO2aX;uJIF{e2G7		MUjJcohq[mm2aX;uJI9nKHerbHSgeJlx\SCHTVy0M2FNUyCVMUKwOnkhdXW2YX70JEh2dmuwb4fuJI9zcWerbjmg[ZhxemW\|c3XkJIlvKE6LSD:zWFMh[2WubIOsJGlEPTBiPTCwMlAxPDJizszNMi=>	M2CwPVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6NEOxN\|QxLz5{OESzNVM1ODxxYU6=
SU-DHL1	MUTBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>?	M3uzOlczKGi{cx?=	MWDBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFOXLVTIUFEh[2WubIOgbIFz[m:{aX7nJG5RVS2DTFugZYZ1\XJiN{KgbJJ{KGK7IGPSRkBweiCFQ1u4JIF{e2G7LDDJR\|UxKD1iMD6wNFQ6KM7:TT6=	M2qzR\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7Mki4PVQxLz5{OUK4PFk1ODxxYU6=
NCI-H3122	MlXRRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl?	MYC3NkBpenN?	MYTBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE6FST3IN\|EzOiClZXzsd{Bi\nSncjC3NkBpenNiYomgV3JDKG:{IFPDT\|gh[XO\|YYmsJGlEPTBiPTCwMlAxPzhizszNMi=>	NVfKdZdGRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkmyPFg6PDBpPkK5Nlg5QTRyPD;hQi=>
NIH-3T3	M4f3cmZ2dmO2aX;uJIF{e2G7	MkmzNUBpeg>?	NGfpU\|hKdmirYnn0bY9vKG:oIHj1cYFvKEWPTESt[pV{\WRiQVzLJGwyOTV{UjDteZRidnRiZYjwdoV{e2WmIHnuJI1wfXOnIF7JTE0{XDNiY3XscJMh[XO\|ZYPz[YQh[XNicHjvd5Bpdy2DTFugcIV3\WxiYX\0[ZIhOSCqcjDifUB{[W6md3njbEBGVEmVQTygTWM2OCB;IECuNFA6KM7:TT6=	NVzJWGNuRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS4NVkyOTZpPkK0PFE6OTF4PD;hQi=>
NIH/3T3	MkjpSpVv[3Srb36gZZN{[Xl?		NXfIT\|JLUW6qaXLpeIlwdiCxZjD3bYxlKHS7cHWgSW1NPC:DTFugUFEyPTKUIH31eIFvfCBqdX7rco94diCxcnnnbY4qKGW6cILld5Nm\CCrbjDOTWgwO1R\|IHPlcIx{NCCLQ{WwJF0hOC5yMEmg{txONg>?	MXy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDR\|MUO0NEc,Ojh2M{GzOFA9N2F-
NIH-3T3	M3\NcWZ2dmO2aX;uJIF{e2G7	MnLqNUBpeg>?	MU\Jcohq[mm2aX;uJI9nKGi3bXHuJGVOVDRvZoXz[YQhSUyNIFexNlY6SSCvdYThcpQh\XiycnXzd4VlKGmwIH3veZNmKE6LSD2zWFMh[2WubIOgZZN{\XO\|ZXSgZZMheGixc4Doc{1CVEtibHX2[Ywh[W[2ZYKgNUBpeiCkeTDzZY5lf2mlaDDFUGlUSSxiSVO1NEA:KDBwMEG1JO69VS5?	MVq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDhzOUGxOkc,OjR6MUmxNVY9N2F-
NIH/3T3	NG[xVVdHfW6ldHnvckBie3OjeR?=		NHnJPHJKdmirYnn0bY9vKG:oIIfpcIQhfHmyZTDFUWw1N0GOSzDHNVI3QUFibYX0ZY51KCi3bnvuc5dvKG:{aXfpckkh\XiycnXzd4VlKGmwIF7JTE8{XDNiY3XscJMtKEmFNUCgQUAxNjBzNTFOwG0v	MYq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDR\|MUO0NEc,Ojh2M{GzOFA9N2F-
NIH-3T3	MUfGeY5kfGmxbjDhd5NigQ>?	NFXHeXcyKGi{	NUPPcZhpUW6qaXLpeIlwdiCxZjDoeY1idiCHTVy0MYZ2e2WmIFHMT{BNOTF7Nl2gcZV1[W62IHX4dJJme3OnZDDpckBud3W\|ZTDOTWguO1R\|IHPlcIx{KGG\|c3Xzd4VlKGG\|IIDoc5NxcG9vQVzLJIxmfmWuIHHmeIVzKDFiaIKgZpkhe2GwZIfpZ4ghTUyLU1GsJGlEPTBiPTCwMlAzOSEQvF2u	MljqQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR6MUmxNVYoRjJ2OEG5NVE3RC:jPh?=
NIH/3T3	MmXSSpVv[3Srb36gZZN{[Xl?		MkfMTY5pcWKrdHnvckBw\iC5aXzkJJR6eGViRV3MOE9CVEtiTEGxPVZOKG23dHHueEApfW6tbn;3ckBwemmpaX6pJIV5eHKnc4Pl[EBqdiCQSVivN3Q{KGOnbHzzMEBKSzVyIE2gNE4xOjFizszNMi=>	MnPvQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh2M{GzOFAoRjJ6NEOxN\|QxRC:jPh?=
NIH-3T3	Moq2SpVv[3Srb36gZZN{[Xl?	Moq5NUBpeg>?	Mm\QTY5pcWKrdHnvckBw\iCqdX3hckBGVUx2LX\1d4VlKEGOSzCxNVUyXGmwczDteZRidnRiZYjwdoV{e2WmIHnuJI1wfXOnIF7JTE0{XDNiY3XscJMh[XO\|ZYPz[YQh[XNicHjvd5Bpdy2DTFugcIV3\WxiYX\0[ZIhOSCqcjDifUB{[W6md3njbEBGVEmVQTygTWM2OCB;IECuNFM5KM7:TT6=	MnraQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR6MUmxNVYoRjJ2OEG5NVE3RC:jPh?=
NIH/3T3	MmDNSpVv[3Srb36gZZN{[Xl?		NXvRZldEUW6qaXLpeIlwdiCxZjD3bYxlKHS7cHWgSW1NPC:DTFugNVE2OVSrboOgcZV1[W62IDj1cotvd3ewIH;ybYdqdiliZYjwdoV{e2WmIHnuJG5KUC9\|VEOgZ4VtdHNuIFnDOVAhRSByLkCzPEDPxE1w	NV7tZoxVRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMki0N\|E{PDBpPkK4OFMyOzRyPD;hQi=>
BAF3	NUn0R2F4SW62aYDyc4xq\mW{YYTpeoUh[XO\|YYm=	MX23NkBpenN?	NIXZU45CdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JI1wfXOnIFLBSlMh[2WubIOgbIFz[m:{aX7nJGVOVDRvQVzLJGwyOTl4TTDteZRidnRiYX\0[ZIhPzJiaILzJIJ6KFOUQjDvdkBES0t6IHHzd4F6NCCLQ{WwJF0hOC5yNEK0JO69VS5?	MVK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTJ6OEm0NEc,Ojl{OEi5OFA9N2F-
NIH-3T3	MY\GeY5kfGmxbjDhd5NigQ>?	MVqxJIhz	NELnUW1KdmirYnn0bY9vKG:oIHj1cYFvKEWPTESt[pV{\WRiQVzLJGcyOjB{UjDteZRidnRiZYjwdoV{e2WmIHnuJI1wfXOnIF7JTE0{XDNiY3XscJMh[XO\|ZYPz[YQh[XNicHjvd5Bpdy2DTFugcIV3\WxiYX\0[ZIhOSCqcjDifUB{[W6md3njbEBGVEmVQTygTWM2OCB;IECuNFc4KM7:TT6=	MkHOQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR6MUmxNVYoRjJ2OEG5NVE3RC:jPh?=
NIH/3T3	MmfiSpVv[3Srb36gZZN{[Xl?		MVrJcohq[mm2aX;uJI9nKHerbHSgeJlx\SCHTVy0M2FNUyCJMUKwNnIhdXW2YX70JEh2dmuwb4fuJI9zcWerbjmg[ZhxemW\|c3XkJIlvKE6LSD:zWFMh[2WubIOsJGlEPTBiPTCwMlA4PyEQvF2u	NI\qZYw9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OESzNVM1OCd-Mki0N\|E{PDB:L3G+
BAF3	NVjVNm9PSW62aYDyc4xq\mW{YYTpeoUh[XO\|YYm=	NInBPGM4OiCqcoO=	M1vlb2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgcY92e2ViQlHGN{Bk\WyuczDoZZJjd3KrbnegSW1NPC2DTFugS\|EzODKUIH31eIFvfCCjZoTldkA4OiCqcoOgZpkhW1KEIH;yJGNEUzhiYYPzZZktKEmFNUCgQUAxNjJizszNMi=>	M3;pWlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7Mki4PVQxLz5{OUK4PFk1ODxxYU6=
BAF3	NYTYSmhwSW62aYDyc4xq\mW{YYTpeoUh[XO\|YYm=	MofaO\|IhcHK\|	NFnpZlZCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JI1wfXOnIFLBSlMh[2WubIOgbIFz[m:{aX7nJGNFPzRvUl;TNUBIOjB\|MmKgcZV1[W62IHHmeIVzKDd{IHjyd{BjgSCVUlKgc5IhS0ONODDhd5NigSxiSVO1NEA:KDBwMk[yJO69VS5?	M1XSWVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7Mki4PVQxLz5{OUK4PFk1ODxxYU6=
HCC78	MUfBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>?	Mn\hO\|IhcHK\|	NXH1PHpDSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDIR2M4QCClZXzsd{Bp[XKkb4LpcochW0yFM{TBNk1TV1NzIHHmeIVzKDd{IHjyd{BjgSCVUlKgc5IhS0ONODDhd5NigSxiSVO1NEA:KDBwM{W3JO69VS5?	MnnZQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl{OEi5OFAoRjJ7Mki4PVQxRC:jPh?=
SU-DHL1	Ml7jSpVv[3Srb36gZZN{[Xl?		M{LrRWlvcGmkaYTpc44hd2ZiQVzLJIlvKGi3bXHuJHNWNUSKTEGgZ4VtdHNiYYPz[ZN{\WRiYYOgdoVlfWO2aX;uJIlvKFOWQWSzJJBpd3OyaH;yfYxifGmxbjDheEB[PzB3IILld4llfWViYYSgNlAhfG9iOECgcm0h[W[2ZYKgNUBpeiCkeTDX[ZN1\XKwIHLsc5Qh[W6jbInzbZM>	M3fxPFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7Mki4PVQxLz5{OUK4PFk1ODxxYU6=
SU-DHL1	MkTOSpVv[3Srb36gZZN{[Xl?		NFPyPY9KdmirYnn0bY9vKG:oIFHMT{BqdiCqdX3hckBUXS2GSFyxJINmdGy\|IHHzd4V{e2WmIHHzJJJm\HWldHnvckBqdiCDa4SgdIhwe3Cqb4L5cIF1cW:wIHH0JHM1PzNicnXzbYR2\SCjdDCyNEB1dyB6MDDuUUBi\nSncjCxJIhzKGK7IGfld5Rmem5iYnzveEBidmGueYPpdy=>	NImxeXQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUK4PFk1OCd-MkmyPFg6PDB:L3G+
SU-DHL1	NVmwfG5tTnWwY4Tpc44h[XO\|YYm=		NFr0fZdKdmirYnn0bY9vKG:oIFHMT{BxcG:\|cHjvdplt[XSrb36gZZQhYTF{N{igdoV{cWS3ZTDpckBpfW2jbjDTWU1FUExzIHPlcIx{KGG2IEKwJJRwKDhyIH7NJIFnfGW{IEGgbJIh[nliV3XzeIVzdiCkbH;0JIFv[Wy7c3nz	M1XNVlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7Mki4PVQxLz5{OUK4PFk1ODxxYU6=
SU-DHL1	MWrGeY5kfGmxbjDhd5NigQ>?		MUHJcohq[mm2aX;uJI9nKEGOSzDpckBpfW2jbjDTWU1FUExzIHPlcIx{KGG\|c3Xzd4VlKGG\|IILl[JVkfGmxbjDpckBGWkticHjvd5Bpd3K7bHH0bY9vKGG2IGSyNFIwN1l{MESgdoV{cWS3ZYOgZZQhOjBidH:gPFAhdk1iYX\0[ZIhOSCqcjDifUBY\XO2ZYLuJIJtd3RiYX7hcJl{cXN?	MkLqQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl{OEi5OFAoRjJ7Mki4PVQxRC:jPh?=
NCI-H3122	NU\KZ\|hXTnWwY4Tpc44h[XO\|YYm=		M3HCS2lvcGmkaYTpc44hd2ZiQVzLJJBpd3OyaH;yfYxifGmxbjDheEB[OTJ5ODDy[ZNq\HWnIHnuJIh2dWGwIF7DTU1JOzF{MjDj[YxteyCjdDCyNEB1dyB6MDDuUUBi\nSncjCxJIhzKGK7IGfld5Rmem5iYnzveEBidmGueYPpdy=>	MVq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTJ6OEm0NEc,Ojl{OEi5OFA9N2F-
NCI-H3122	MYfGeY5kfGmxbjDhd5NigQ>?		MoHZTY5pcWKrdHnvckBw\iCDTFugbY4hcHWvYX6gUmNKNUh\|MUKyJINmdGy\|IHHzd4V{e2WmIHHzJJJm\HWldHnvckBqdiCVVFHUN{BxcG:\|cHjvdplt[XSrb36gZZQhYTdyNTDy[ZNq\HWnIHH0JFIxKHSxIEiwJI5OKGGodHXyJFEhcHJiYomgW4V{fGW{bjDicI91KGGwYXz5d4l{	NUXU[5V1RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkmyPFg6PDBpPkK5Nlg5QTRyPD;hQi=>
NCI-H3122	NHrJb3hHfW6ldHnvckBie3OjeR?=		M4qyUGlvcGmkaYTpc44hd2ZiQVzLJIlvKGi3bXHuJG5EUS2KM{GyNkBk\WyuczDhd5Nme3OnZDDhd{Bz\WS3Y4Tpc44hcW5iQXv0JJBpd3OyaH;yfYxifGmxbjDheEBUPDd\|IILld4llfWViYYSgNlAhfG9iOECgcm0h[W[2ZYKgNUBpeiCkeTDX[ZN1\XKwIHLsc5Qh[W6jbInzbZM>	Mn72QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl{OEi5OFAoRjJ7Mki4PVQxRC:jPh?=
NCI-H3122	NEH4cYJHfW6ldHnvckBie3OjeR?=		MXvJcohq[mm2aX;uJI9nKEGOSzDpckBpfW2jbjDOR2kuUDNzMkKgZ4VtdHNiYYPz[ZN{\WRiYYOgdoVlfWO2aX;uJIlvKEWUSzDwbI9{eGixconsZZRqd25iYYSgWFIxOi9xWUKwOEBz\XOrZIXld{BifCB{MDD0c{A5OCCwTTDh[pRmeiBzIHjyJIJ6KFenc4Tldo4h[myxdDDhcoFtgXOrcx?=	MmPIQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl{OEi5OFAoRjJ7Mki4PVQxRC:jPh?=

Click to View More Cell Line Experimental Data

Assay

Methods	Test Index	PMID

Western blot

p-ALK / ALK

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	[1] Johnson TW, et al. J Med Chem. 2014, 57(11), 4720-4744. [2] Zou HY, et al. Mol Cancer Ther. 2013, 12, A277. [3] Zou HY, et al. Mol Cancer Ther. 2013, 12, C253.

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)： 2% DMSO+30% PEG 300+ddH2O 点击购买： PEG300	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

分子量	406.41
化学式	C₂₁H₁₉FN₆O₂
CAS号	1454846-35-5
储存条件	3年	-20°C	粉状
储存条件	2年	-80°C	溶于溶剂

Download Lorlatinib (PF-6463922) 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
NCT05224609	Recruiting	Drug: Lorlatinib	Moderate Hepatic Impairment\|Severe Hepatic Impairment\|Healthy Volunteers	Pfizer	April 28 2022	Phase 1
NCT04979988	Completed	Drug: Lortlatinib	ALK-positive Non-small-cell Lung Cancer	Pfizer	August 2 2021	--
NCT03726333	Terminated	Drug: lorlatinib	Advanced Cancers	Pfizer	January 14 2020	Phase 1
NCT03542305	Completed	Drug: Lorlatinib	Renal Impairment	Pfizer	August 23 2018	Phase 1
NCT03505554	Recruiting	Drug: Lorlatinib	Anaplastic Large Cell Lymphoma ALK-Positive	University of Milano Bicocca\|Pfizer	October 10 2017	Phase 2

(data from https://clinicaltrials.gov, updated on 2022-08-01)

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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.

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