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Ki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 购买数量
10mM (1mL in DMSO) RMB 1875.51 现货
RMB 1056.51 现货
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

相关ALK产品

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)
点击更多
<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 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+
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KARPAS299 NVzGWnZLSW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= Mlz4O|IhcHK| M1nje2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iS1HSVGFUOjl7IHPlcIx{KGijcnLvdolv\yCQUF2tRWxMKGGodHXyJFczKGi{czDifUBUWkJib4KgR2NMQCCjc4PhfUwhUUN3MDC9JFAvODB|IN88UU4> NWfKSFJpRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkmyPFg6PDBpPkK5Nlg5QTRyPD;hQi=>
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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-
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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?=
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]

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

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 3年 -20°C 粉状
2年 -80°C 溶于溶剂

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)

mg/kg g μL

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,: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: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: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

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)

技术支持

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操作手册

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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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