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Ki分别为<0.02 nM, <0.07 nM, 和0.7 nM。PF-06463922 可诱导凋亡。Phase 1。

规格 价格 库存 购买数量  
10mM (1mL in DMSO) RMB 2432.43 现货
RMB 1622.95 现货
RMB 6531.11 现货
有超大折扣

今日订购,明日送达,全国免运费!

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25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 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Ki分别为<0.02 nM, <0.07 nM, 和0.7 nM。PF-06463922 可诱导凋亡。Phase 1。
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)
<0.02 nM(Ki) <0.07 nM(Ki) 0.07 nM(Ki) 2.7 nM 3.3 nM
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 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     


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]

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)

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

分子量 406.41
化学式

C21H19FN6O2

CAS号 1454846-35-5
储存条件 粉状
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 g 每只动物给药体积 ul 动物数量
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

计算器

摩尔浓度计算器

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

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

  • 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

分子量计算器

通过输入化合物的化学式来计算其分子量:

总分子量:g/mol

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

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。

  • * 必填项

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.

ALK Signaling Pathway Map

相关ALK产品

Tags: 购买Lorlatinib (PF-6463922) | Lorlatinib (PF-6463922)供应商 | 采购Lorlatinib (PF-6463922) | Lorlatinib (PF-6463922)价格 | Lorlatinib (PF-6463922)生产 | 订购Lorlatinib (PF-6463922) | Lorlatinib (PF-6463922)代理商
×
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID