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 分装免费
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41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
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NIH/3T3 MmTpSpVv[3Srb36gZZN{[Xl? M{PJbGlvcGmkaYTpc44hd2Zid3ns[EB1gXCnIFXNUFQwSUyNIDj1cotvd3ewIH;ybYdqdiliZYjwdoV{e2WmIHnuJG5KUC9|VEOgZ4VtdHNuIFnDOVAhRSByLkCwNVMh|ryPLh?= NHTMVZg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OESzNVM1OCd-Mki0N|E{PDB:L3G+
NIH-3T3 NIToTm5HfW6ldHnvckBie3OjeR?= M{DQT|EhcHJ? M4fkfmlvcGmkaYTpc44hd2ZiaIXtZY4hTU2OND3meZNm\CCDTFugR|EyPT[\IH31eIFvfCCneIDy[ZN{\WRiaX6gcY92e2ViTlnIMVNVOyClZXzsd{Bie3Onc4Pl[EBieyCyaH;zdIhwNUGOSzDs[ZZmdCCjZoTldkAyKGi{IHL5JJNidmS5aXPoJGVNUVODLDDJR|UxKD1iMD6wNFE3KM7:TT6= M{nLOFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2OEG5NVE3Lz5{NEixPVEyPjxxYU6=
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SU-DHL1 Mm\URY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? Mn;3O|IhcHK| NHLpRolCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIGPVMWRJVDFiY3XscJMhcGG{Yn;ybY5oKE6STT3BUGsh[W[2ZYKgO|IhcHK|IHL5JHNTSiCxcjDDR2s5KGG|c3H5MEBKSzVyIE2gNE4xODR7IN88UU4> MkKxQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl{OEi5OFAoRjJ7Mki4PVQxRC:jPh?=
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NIH/3T3 MkS5SpVv[3Srb36gZZN{[Xl? NW\Heo5yUW6qaXLpeIlwdiCxZjD3bYxlKHS7cHWgSW1NPC:DTFugUFEyPTKUIH31eIFvfCBqdX7rco94diCxcnnnbY4qKGW6cILld5Nm\CCrbjDOTWgwO1R|IHPlcIx{NCCLQ{WwJF0hOC5yMEmg{txONg>? MkDrQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh2M{GzOFAoRjJ6NEOxN|QxRC:jPh?=
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HCC78 NHruNo1CdnSrcILvcIln\XKjdHn2[UBie3OjeR?= M4PxO|czKGi{cx?= MnLWRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCKQ1O3PEBk\WyuczDoZZJjd3KrbnegV2xEOzSDMj3SU3MyKGGodHXyJFczKGi{czDifUBUWkJib4KgR2NMQCCjc4PhfUwhUUN3MDC9JFAvOzV5IN88UU4> MUG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTJ6OEm0NEc,Ojl{OEi5OFA9N2F-
SU-DHL1 M4\QOmZ2dmO2aX;uJIF{e2G7 M1XjNGlvcGmkaYTpc44hd2ZiQVzLJIlvKGi3bXHuJHNWNUSKTEGgZ4VtdHNiYYPz[ZN{\WRiYYOgdoVlfWO2aX;uJIlvKFOWQWSzJJBpd3OyaH;yfYxifGmxbjDheEB[PzB3IILld4llfWViYYSgNlAhfG9iOECgcm0h[W[2ZYKgNUBpeiCkeTDX[ZN1\XKwIHLsc5Qh[W6jbInzbZM> M2HtbFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7Mki4PVQxLz5{OUK4PFk1ODxxYU6=
SU-DHL1 NFjoSmJHfW6ldHnvckBie3OjeR?= M3HJcWlvcGmkaYTpc44hd2ZiQVzLJIlvKGi3bXHuJHNWNUSKTEGgZ4VtdHNiYYPz[ZN{\WRiYYOgdoVlfWO2aX;uJIlvKEGtdDDwbI9{eGixconsZZRqd25iYYSgV|Q4OyC{ZYPp[JVmKGG2IEKwJJRwKDhyIH7NJIFnfGW{IEGgbJIh[nliV3XzeIVzdiCkbH;0JIFv[Wy7c3nz MYW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTJ6OEm0NEc,Ojl{OEi5OFA9N2F-
SU-DHL1 M1LQSGZ2dmO2aX;uJIF{e2G7 NWrqc4hTUW6qaXLpeIlwdiCxZjDBUGsheGixc4Doc5J6dGG2aX;uJIF1KFlzMke4JJJme2mmdXWgbY4hcHWvYX6gV3UuTEiOMTDj[YxteyCjdDCyNEB1dyB6MDDuUUBi\nSncjCxJIhzKGK7IGfld5Rmem5iYnzveEBidmGueYPpdy=> MXK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTJ6OEm0NEc,Ojl{OEi5OFA9N2F-
SU-DHL1 NHPxUoZHfW6ldHnvckBie3OjeR?= M3vkZWlvcGmkaYTpc44hd2ZiQVzLJIlvKGi3bXHuJHNWNUSKTEGgZ4VtdHNiYYPz[ZN{\WRiYYOgdoVlfWO2aX;uJIlvKEWUSzDwbI9{eGixconsZZRqd25iYYSgWFIxOi9xWUKwOEBz\XOrZIXld{BifCB{MDD0c{A5OCCwTTDh[pRmeiBzIHjyJIJ6KFenc4Tldo4h[myxdDDhcoFtgXOrcx?= NXjxXlE5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkmyPFg6PDBpPkK5Nlg5QTRyPD;hQi=>
NCI-H3122 NUC2b5NyTnWwY4Tpc44h[XO|YYm= NX3KNGRMUW6qaXLpeIlwdiCxZjDBUGsheGixc4Doc5J6dGG2aX;uJIF1KFlzMke4JJJme2mmdXWgbY4hcHWvYX6gUmNKNUh|MUKyJINmdGy|IHH0JFIxKHSxIEiwJI5OKGGodHXyJFEhcHJiYomgW4V{fGW{bjDicI91KGGwYXz5d4l{ M{mySVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7Mki4PVQxLz5{OUK4PFk1ODxxYU6=
NCI-H3122 NHnzdlFHfW6ldHnvckBie3OjeR?= M3jacmlvcGmkaYTpc44hd2ZiQVzLJIlvKGi3bXHuJG5EUS2KM{GyNkBk\WyuczDhd5Nme3OnZDDhd{Bz\WS3Y4Tpc44hcW5iU2TBWFMheGixc4Doc5J6dGG2aX;uJIF1KFl5MEWgdoV{cWS3ZTDheEAzOCC2bzC4NEBvVSCjZoTldkAyKGi{IHL5JHdme3Sncn6gZoxwfCCjbnHsfZNqew>? Ml;FQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl{OEi5OFAoRjJ7Mki4PVQxRC:jPh?=
NCI-H3122 M2\5d2Z2dmO2aX;uJIF{e2G7 MWTJcohq[mm2aX;uJI9nKEGOSzDpckBpfW2jbjDOR2kuUDNzMkKgZ4VtdHNiYYPz[ZN{\WRiYYOgdoVlfWO2aX;uJIlvKEGtdDDwbI9{eGixconsZZRqd25iYYSgV|Q4OyC{ZYPp[JVmKGG2IEKwJJRwKDhyIH7NJIFnfGW{IEGgbJIh[nliV3XzeIVzdiCkbH;0JIFv[Wy7c3nz MmnaQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl{OEi5OFAoRjJ7Mki4PVQxRC:jPh?=
NCI-H3122 M{H5b2Z2dmO2aX;uJIF{e2G7 M1;XbGlvcGmkaYTpc44hd2ZiQVzLJIlvKGi3bXHuJG5EUS2KM{GyNkBk\WyuczDhd5Nme3OnZDDhd{Bz\WS3Y4Tpc44hcW5iRWLLJJBpd3OyaH;yfYxifGmxbjDheEBVOjB{Lz;ZNlA1KHKnc3nkeYV{KGG2IEKwJJRwKDhyIH7NJIFnfGW{IEGgbJIh[nliV3XzeIVzdiCkbH;0JIFv[Wy7c3nz NX;EdnJuRGFidHHy[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、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 Recruiting Drug: Lortlatinib 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