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
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客户使用Selleck生产的Lorlatinib (PF-6463922)发表文献33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 MV3GeY5kfGmxbjDhd5NigQ>? NWniWVhMOSCqch?= MV;Jcohq[mm2aX;uJI9nKGi3bXHuJGVOVDRvZoXz[YQhSUyNIF[xNVc1VCCvdYThcpQh\XiycnXzd4VlKGmwIH3veZNmKE6LSD2zWFMh[2WubIOgZZN{\XO|ZXSgZZMheGixc4Doc{1CVEtibHX2[Ywh[W[2ZYKgNUBpeiCkeTDzZY5lf2mlaDDFUGlUSSxiSVO1NEA:KDBwMECwNkDPxE1w NETGSnc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEixPVEyPid-MkS4NVkyOTZ:L3G+
NIH/3T3 MlHnSpVv[3Srb36gZZN{[Xl? MnLjTY5pcWKrdHnvckBw\iC5aXzkJJR6eGViRV3MOE9CVEtiRkGxO|RNKG23dHHueEApfW6tbn;3ckBwemmpaX6pJIV5eHKnc4Pl[EBqdiCQSVivN3Q{KGOnbHzzMEBKSzVyIE2gNE4xODB{IN88UU4> NYX1b2kyRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMki0N|E{PDBpPkK4OFMyOzRyPD;hQi=>
BAF3 M4XqT2FvfGmycn;sbYZmemG2aY\lJIF{e2G7 M4rhU|czKGi{cx?= NH\LTJZCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JI1wfXOnIFLBSlMh[2WubIOgbIFz[m:{aX7nJGNFPzRvUl;TNUBi\nSncjC3NkBpenNiYomgV3JDKG:{IFPDT|gh[XO|YYmsJGlEPTBiPTCwMlAxOTJizszNMi=> MojiQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl{OEi5OFAoRjJ7Mki4PVQxRC:jPh?=
NIH-3T3 M1jkRWZ2dmO2aX;uJIF{e2G7 MYexJIhz Mly5TY5pcWKrdHnvckBw\iC5aXzkJJR6eGViaIXtZY4hTU2OND3meZNm\CCDTFug[ZhxemW|c3XkJIlvKG2xdYPlJG5KUC1|VEOgZ4VtdHNiYYPz[ZN{\WRiYYOgdIhwe3Cqb4L5cIF1\WRiQVzLJIxmfmWuIHHmeIVzKDFiaIKgZpkhe2GwZIfpZ4ghTUyLU1GsJGlEPTBiPTCwMlAxOTNizszNMi=> MoPiQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR6MUmxNVYoRjJ2OEG5NVE3RC:jPh?=
NIH/3T3 NVrZUm9ITnWwY4Tpc44h[XO|YYm= NW\Ve4NIUW6qaXLpeIlwdiCxZjD3bYxlKHS7cHWgSW1NPC:DTFugLJVvc26xd36gc5Jq\2mwKTDlfJBz\XO|ZXSgbY4hVkmKL{PUN{Bk\WyuczygTWM2OCB;IECuNFAyOyEQvF2u MVG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDR|MUO0NEc,Ojh2M{GzOFA9N2F-
NIH-3T3 MV;GeY5kfGmxbjDhd5NigQ>? MlzkNUBpeg>? MoLDTY5pcWKrdHnvckBw\iCqdX3hckBGVUx2LX\1d4VlKEGOSzDDNVE2PllibYX0ZY51KGW6cILld5Nm\CCrbjDtc5V{\SCQSVitN3Q{KGOnbHzzJIF{e2W|c3XkJIF{KHCqb4PwbI8uSUyNIHzleoVtKGGodHXyJFEhcHJiYomgd4Fv\HerY3igSWxKW0FuIFnDOVAhRSByLkCwNVYh|ryPLh?= NEfic4E9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEixPVEyPid-MkS4NVkyOTZ:L3G+
NIH/3T3 NEfQZ25HfW6ldHnvckBie3OjeR?= NGjwXWNKdmirYnn0bY9vKG:oIIfpcIQhfHmyZTDFUWw1N0GOSzDDNVE2PllibYX0ZY51KCi3bnvuc5dvKG:{aXfpckkh\XiycnXzd4VlKGmwIF7JTE8{XDNiY3XscJMtKEmFNUCgQUAxNjByMU[g{txONg>? NIHmdpQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OESzNVM1OCd-Mki0N|E{PDB:L3G+
BAF3 MVLBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? NYD2dJJVPzJiaILz NWXIOHR6SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBud3W|ZTDCRWY{KGOnbHzzJIhiemKxcnnu[{BGVUx2LVHMT{Bi\nSncjC3NkBpenNiYomgV3JDKG:{IFPDT|gh[XO|YYmsJGlEPTBiPTCwMlAxOjlizszNMi=> NX;oenI2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkmyPFg6PDBpPkK5Nlg5QTRyPD;hQi=>
KARPAS299 MnLIRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? M4r6fVczKGi{cx?= Ml\lRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCNQWLQRXMzQTliY3XscJMhcGG{Yn;ybY5oKE6STT3BUGsh[W[2ZYKgO|IhcHK|IHL5JHNTSiCxcjDDR2s5KGG|c3H5MEBKSzVyIE2gNE4xODNizszNMi=> MXm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTJ6OEm0NEc,Ojl{OEi5OFA9N2F-
NIH-3T3 MYrGeY5kfGmxbjDhd5NigQ>? NXfofoRVOSCqch?= NIf0VoRKdmirYnn0bY9vKG:oIHj1cYFvKEWPTESt[pV{\WRiQVzLJHMyOjB4WTDteZRidnRiZYjwdoV{e2WmIHnuJI1wfXOnIF7JTE0{XDNiY3XscJMh[XO|ZYPz[YQh[XNicHjvd5Bpdy2DTFugcIV3\WxiYX\0[ZIhOSCqcjDifUB{[W6md3njbEBGVEmVQTygTWM2OCB;IECuNFA1OiEQvF2u MWi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDhzOUGxOkc,OjR6MUmxNVY9N2F-
NIH/3T3 MX7GeY5kfGmxbjDhd5NigQ>? M4[5PWlvcGmkaYTpc44hd2Zid3ns[EB1gXCnIFXNUFQwSUyNIGOxNlA3YSCvdYThcpQhMHWwa37ve44hd3KrZ3nuLUBmgHC{ZYPz[YQhcW5iTlnIM|NVOyClZXzsd{whUUN3MDC9JFAvODB2MjFOwG0v NF\3T2Y9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OESzNVM1OCd-Mki0N|E{PDB:L3G+
SU-DHL1 Ml;YRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? MmC1O|IhcHK| NWD3cHM6SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDTWU1FUExzIHPlcIx{KGijcnLvdolv\yCQUF2tRWxMKGGodHXyJFczKGi{czDifUBUWkJib4KgR2NMQCCjc4PhfUwhUUN3MDC9JFAvODB2OTFOwG0v MYi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTJ6OEm0NEc,Ojl{OEi5OFA9N2F-
NCI-H3122 NUnq[pZwSW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= MljlO|IhcHK| M3nIO2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTlPJMWg{OTJ{IHPlcIx{KGGodHXyJFczKGi{czDifUBUWkJib4KgR2NMQCCjc4PhfUwhUUN3MDC9JFAvODB5ODFOwG0v NVXsT|RYRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkmyPFg6PDBpPkK5Nlg5QTRyPD;hQi=>
NIH-3T3 MUTGeY5kfGmxbjDhd5NigQ>? MnHkNUBpeg>? M4rnN2lvcGmkaYTpc44hd2ZiaIXtZY4hTU2OND3meZNm\CCDTFugUFEyPTKUIH31eIFvfCCneIDy[ZN{\WRiaX6gcY92e2ViTlnIMVNVOyClZXzsd{Bie3Onc4Pl[EBieyCyaH;zdIhwNUGOSzDs[ZZmdCCjZoTldkAyKGi{IHL5JJNidmS5aXPoJGVNUVODLDDJR|UxKD1iMD6wNFkh|ryPLh?= MWq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDhzOUGxOkc,OjR6MUmxNVY9N2F-
NIH/3T3 NUDJWFNoTnWwY4Tpc44h[XO|YYm= MX3Jcohq[mm2aX;uJI9nKHerbHSgeJlx\SCHTVy0M2FNUyCOMUG1NnIhdXW2YX70JEh2dmuwb4fuJI9zcWerbjmg[ZhxemW|c3XkJIlvKE6LSD:zWFMh[2WubIOsJGlEPTBiPTCwMlAxQSEQvF2u MlHlQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh2M{GzOFAoRjJ6NEOxN|QxRC:jPh?=
NIH-3T3 M1f0RWZ2dmO2aX;uJIF{e2G7 M13TdFEhcHJ? NFvEcYNKdmirYnn0bY9vKG:oIHj1cYFvKEWPTESt[pV{\WRiQVzLJGcyOjZ7QTDteZRidnRiZYjwdoV{e2WmIHnuJI1wfXOnIF7JTE0{XDNiY3XscJMh[XO|ZYPz[YQh[XNicHjvd5Bpdy2DTFugcIV3\WxiYX\0[ZIhOSCqcjDifUB{[W6md3njbEBGVEmVQTygTWM2OCB;IECuNFE2KM7:TT6= MVe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDhzOUGxOkc,OjR6MUmxNVY9N2F-
NIH/3T3 M124VGZ2dmO2aX;uJIF{e2G7 MYTJcohq[mm2aX;uJI9nKHerbHSgeJlx\SCHTVy0M2FNUyCJMUK2PWEhdXW2YX70JEh2dmuwb4fuJI9zcWerbjmg[ZhxemW|c3XkJIlvKE6LSD:zWFMh[2WubIOsJGlEPTBiPTCwMlAyPSEQvF2u MYe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDR|MUO0NEc,Ojh2M{GzOFA9N2F-
NIH-3T3 NUT5b3RUTnWwY4Tpc44h[XO|YYm= NHTmZVcyKGi{ M2KyO2lvcGmkaYTpc44hd2ZiaIXtZY4hTU2OND3meZNm\CCDTFugUFEyQT[PIH31eIFvfCCneIDy[ZN{\WRiaX6gcY92e2ViTlnIMVNVOyClZXzsd{Bie3Onc4Pl[EBieyCyaH;zdIhwNUGOSzDs[ZZmdCCjZoTldkAyKGi{IHL5JJNidmS5aXPoJGVNUVODLDDJR|UxKD1iMD6wNlEh|ryPLh?= NXvtcHZTRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS4NVkyOTZpPkK0PFE6OTF4PD;hQi=>
NIH/3T3 Ml3YSpVv[3Srb36gZZN{[Xl? NVLZ[GNnUW6qaXLpeIlwdiCxZjD3bYxlKHS7cHWgSW1NPC:DTFugUFEyQT[PIH31eIFvfCBqdX7rco94diCxcnnnbY4qKGW6cILld5Nm\CCrbjDOTWgwO1R|IHPlcIx{NCCLQ{WwJF0hOC5yMkGg{txONg>? NV3zeo1tRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMki0N|E{PDBpPkK4OFMyOzRyPD;hQi=>
NIH-3T3 M{LvOGZ2dmO2aX;uJIF{e2G7 NFfnbGEyKGi{ NVL4eYhYUW6qaXLpeIlwdiCxZjDoeY1idiCHTVy0MYZ2e2WmIFHMT{AyOTVzVHnud{BufXSjboSg[ZhxemW|c3XkJIlvKG2xdYPlJG5KUC1|VEOgZ4VtdHNiYYPz[ZN{\WRiYYOgdIhwe3Cqbz3BUGshdGW4ZXygZYZ1\XJiMTDodkBjgSC|YX7ke4lkcCCHTFnTRUwhUUN3MDC9JFAvODN6IN88UU4> NXvCcoZ6RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS4NVkyOTZpPkK0PFE6OTF4PD;hQi=>
NIH/3T3 NI\qNlZHfW6ldHnvckBie3OjeR?= MknrTY5pcWKrdHnvckBw\iC5aXzkJJR6eGViRV3MOE9CVEtiMUG1NXRqdnNibYX0ZY51KCi3bnvuc5dvKG:{aXfpckkh\XiycnXzd4VlKGmwIF7JTE8{XDNiY3XscJMtKEmFNUCgQUAxNjB|ODFOwG0v NUL0S5BmRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMki0N|E{PDBpPkK4OFMyOzRyPD;hQi=>
BAF3 NXvkd5I6SW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= MlH1O|IhcHK| NIjUb3lCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JI1wfXOnIFLBSlMh[2WubIOgbIFz[m:{aX7nJGVOVDRvQVzLJGwyOTl4TTDteZRidnRiYX\0[ZIhPzJiaILzJIJ6KFOUQjDvdkBES0t6IHHzd4F6NCCLQ{WwJF0hOC5yNEK0JO69VS5? NYPiT41NRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkmyPFg6PDBpPkK5Nlg5QTRyPD;hQi=>
NIH-3T3 NXPoc2VYTnWwY4Tpc44h[XO|YYm= MljINUBpeg>? M1W4UWlvcGmkaYTpc44hd2ZiaIXtZY4hTU2OND3meZNm\CCDTFugS|EzODKUIH31eIFvfCCneIDy[ZN{\WRiaX6gcY92e2ViTlnIMVNVOyClZXzsd{Bie3Onc4Pl[EBieyCyaH;zdIhwNUGOSzDs[ZZmdCCjZoTldkAyKGi{IHL5JJNidmS5aXPoJGVNUVODLDDJR|UxKD1iMD6wO|ch|ryPLh?= NFvCO5M9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEixPVEyPid-MkS4NVkyOTZ:L3G+
NIH/3T3 MWnGeY5kfGmxbjDhd5NigQ>? MmntTY5pcWKrdHnvckBw\iC5aXzkJJR6eGViRV3MOE9CVEtiR{GyNFJTKG23dHHueEApfW6tbn;3ckBwemmpaX6pJIV5eHKnc4Pl[EBqdiCQSVivN3Q{KGOnbHzzMEBKSzVyIE2gNE4xPzdizszNMi=> NVKyPXNXRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMki0N|E{PDBpPkK4OFMyOzRyPD;hQi=>
BAF3 MU\BcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? NGXVSlY4OiCqcoO= NInab4xCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JI1wfXOnIFLBSlMh[2WubIOgbIFz[m:{aX7nJGVOVDRvQVzLJGcyOjB{UjDteZRidnRiYX\0[ZIhPzJiaILzJIJ6KFOUQjDvdkBES0t6IHHzd4F6NCCLQ{WwJF0hOC5{IN88UU4> MUS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTJ6OEm0NEc,Ojl{OEi5OFA9N2F-
BAF3 NFO1SYdCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= M2C1[|czKGi{cx?= Mle4RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDtc5V{\SCEQV[zJINmdGy|IHjhdoJwemmwZzDDSFc1NVKRU{GgS|IxOzKUIH31eIFvfCCjZoTldkA4OiCqcoOgZpkhW1KEIH;yJGNEUzhiYYPzZZktKEmFNUCgQUAxNjJ4MjFOwG0v NF72VZQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUK4PFk1OCd-MkmyPFg6PDB:L3G+
HCC78 M1LU[mFvfGmycn;sbYZmemG2aY\lJIF{e2G7 MV[3NkBpenN? NY\pNo11SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDIR2M4QCClZXzsd{Bp[XKkb4LpcochW0yFM{TBNk1TV1NzIHHmeIVzKDd{IHjyd{BjgSCVUlKgc5IhS0ONODDhd5NigSxiSVO1NEA:KDBwM{W3JO69VS5? NXzoWYgyRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkmyPFg6PDBpPkK5Nlg5QTRyPD;hQi=>
SU-DHL1 M1j2SWZ2dmO2aX;uJIF{e2G7 NF;nb3FKdmirYnn0bY9vKG:oIFHMT{BqdiCqdX3hckBUXS2GSFyxJINmdGy|IHHzd4V{e2WmIHHzJJJm\HWldHnvckBqdiCVVFHUN{BxcG:|cHjvdplt[XSrb36gZZQhYTdyNTDy[ZNq\HWnIHH0JFIxKHSxIEiwJI5OKGGodHXyJFEhcHJiYomgW4V{fGW{bjDicI91KGGwYXz5d4l{ MVi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTJ6OEm0NEc,Ojl{OEi5OFA9N2F-
SU-DHL1 NYfRR2V2TnWwY4Tpc44h[XO|YYm= NEO2OVVKdmirYnn0bY9vKG:oIFHMT{BqdiCqdX3hckBUXS2GSFyxJINmdGy|IHHzd4V{e2WmIHHzJJJm\HWldHnvckBqdiCDa4SgdIhwe3Cqb4L5cIF1cW:wIHH0JHM1PzNicnXzbYR2\SCjdDCyNEB1dyB6MDDuUUBi\nSncjCxJIhzKGK7IGfld5Rmem5iYnzveEBidmGueYPpdy=> M2XWWFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7Mki4PVQxLz5{OUK4PFk1ODxxYU6=
SU-DHL1 M2rnbGZ2dmO2aX;uJIF{e2G7 NVP6VVBHUW6qaXLpeIlwdiCxZjDBUGsheGixc4Doc5J6dGG2aX;uJIF1KFlzMke4JJJme2mmdXWgbY4hcHWvYX6gV3UuTEiOMTDj[YxteyCjdDCyNEB1dyB6MDDuUUBi\nSncjCxJIhzKGK7IGfld5Rmem5iYnzveEBidmGueYPpdy=> M1Hzc|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7Mki4PVQxLz5{OUK4PFk1ODxxYU6=
SU-DHL1 NGjVbnlHfW6ldHnvckBie3OjeR?= MVTJcohq[mm2aX;uJI9nKEGOSzDpckBpfW2jbjDTWU1FUExzIHPlcIx{KGG|c3Xzd4VlKGG|IILl[JVkfGmxbjDpckBGWkticHjvd5Bpd3K7bHH0bY9vKGG2IGSyNFIwN1l{MESgdoV{cWS3ZYOgZZQhOjBidH:gPFAhdk1iYX\0[ZIhOSCqcjDifUBY\XO2ZYLuJIJtd3RiYX7hcJl{cXN? M13ud|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7Mki4PVQxLz5{OUK4PFk1ODxxYU6=
NCI-H3122 MV\GeY5kfGmxbjDhd5NigQ>? MoLDTY5pcWKrdHnvckBw\iCDTFugdIhwe3Cqb4L5cIF1cW:wIHH0JHkyOjd6IILld4llfWViaX6gbJVu[W5iTlPJMWg{OTJ{IHPlcIx{KGG2IEKwJJRwKDhyIH7NJIFnfGW{IEGgbJIh[nliV3XzeIVzdiCkbH;0JIFv[Wy7c3nz MnHHQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl{OEi5OFAoRjJ7Mki4PVQxRC:jPh?=
NCI-H3122 NETIfXVHfW6ldHnvckBie3OjeR?= NWXZOIZtUW6qaXLpeIlwdiCxZjDBUGshcW5iaIXtZY4hVkOLLVizNVIzKGOnbHzzJIF{e2W|c3XkJIF{KHKnZIXjeIlwdiCrbjDTWGFVOyCyaH;zdIhwenmuYYTpc44h[XRiWUewOUBz\XOrZIXlJIF1KDJyIITvJFgxKG6PIHHmeIVzKDFiaIKgZpkhX2W|dHXyckBjdG:2IHHuZYx6e2m| Mn\zQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl{OEi5OFAoRjJ7Mki4PVQxRC:jPh?=
NCI-H3122 NFTmXmlHfW6ldHnvckBie3OjeR?= MoHkTY5pcWKrdHnvckBw\iCDTFugbY4hcHWvYX6gUmNKNUh|MUKyJINmdGy|IHHzd4V{e2WmIHHzJJJm\HWldHnvckBqdiCDa4SgdIhwe3Cqb4L5cIF1cW:wIHH0JHM1PzNicnXzbYR2\SCjdDCyNEB1dyB6MDDuUUBi\nSncjCxJIhzKGK7IGfld5Rmem5iYnzveEBidmGueYPpdy=> Mn;jQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl{OEi5OFAoRjJ7Mki4PVQxRC:jPh?=
NCI-H3122 NF3TU|NHfW6ldHnvckBie3OjeR?= MmLaTY5pcWKrdHnvckBw\iCDTFugbY4hcHWvYX6gUmNKNUh|MUKyJINmdGy|IHHzd4V{e2WmIHHzJJJm\HWldHnvckBqdiCHUlugdIhwe3Cqb4L5cIF1cW:wIHH0JHQzODJxL2myNFQhemW|aXT1[ZMh[XRiMkCgeI8hQDBibl2gZYZ1\XJiMTDodkBjgSCZZYP0[ZJvKGKub4SgZY5idHm|aYO= MoT2QIEhfGG{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; 

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、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

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

  • 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
NCT04979988 Not yet recruiting Drug: Lorlatinib ALK-positive Non-small-cell Lung Cancer Pfizer August 2 2021 --
NCT03726333 Recruiting 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
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

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

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID