Lorlatinib (PF-6463922)

Catalog No.S7536

For research use only.

Lorlatinib (PF-6463922) is a potent, dual ALK/ROS1 inhibitor with Ki of <0.02 nM, <0.07 nM, and 0.7 nM for ROS1, ALK (WT), and ALK (L1196M), respectively. PF-06463922 induces apoptosis. Phase 1.

Lorlatinib (PF-6463922) Chemical Structure

CAS No. 1454846-35-5

Selleck's Lorlatinib (PF-6463922) has been cited by 44 publications

Purity & Quality Control

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Biological Activity

Description Lorlatinib (PF-6463922) is a potent, dual ALK/ROS1 inhibitor with Ki of <0.02 nM, <0.07 nM, and 0.7 nM for ROS1, ALK (WT), and ALK (L1196M), respectively. PF-06463922 induces apoptosis. Phase 1.
Targets
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)
Click to View More Targets
<0.02 nM(Ki) <0.07 nM(Ki) 0.07 nM(Ki) 2.7 nM 3.3 nM
In vitro

PF-06463922 demonstrates significant cell activity against ALK and a large set of ALK clinical mutations with IC50 ranging from 0.2 nM-77 nM. [1] PF-06463922 significantly inhibits cell proliferation and induces cell apoptosis in the HCC78 human NSCLC cells harboring SLC34A2-ROS1 fusions and the BaF3-CD74-ROS1 cells expressing human CD74-ROS1.[2] PF-06463922 also shows potent growth inhibitory activity and induces apoptosis in the NSCLC cells harboring either non-mutant ALK or mutant ALK fusions. [3]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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SU-DHL1 MlXWSpVv[3Srb36gZZN{[Xl? MorlTY5pcWKrdHnvckBw\iCDTFugbY4hcHWvYX6gV3UuTEiOMTDj[YxteyCjc4Pld5Nm\CCjczDy[YR2[3Srb36gbY4hSWu2IIDoc5NxcG:{eXzheIlwdiCjdDDTOFc{KHKnc3nkeYUh[XRiMkCgeI8hQDBibl2gZYZ1\XJiMTDodkBjgSCZZYP0[ZJvKGKub4SgZY5idHm|aYO= MonjQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl{OEi5OFAoRjJ7Mki4PVQxRC:jPh?=
SU-DHL1 MnH1SpVv[3Srb36gZZN{[Xl? MUXJcohq[mm2aX;uJI9nKEGOSzDwbI9{eGixconsZZRqd25iYYSgXVEzPzhicnXzbYR2\SCrbjDoeY1idiCVVT3ETGwyKGOnbHzzJIF1KDJyIITvJFgxKG6PIHHmeIVzKDFiaIKgZpkhX2W|dHXyckBjdG:2IHHuZYx6e2m| Mle5QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl{OEi5OFAoRjJ7Mki4PVQxRC:jPh?=
SU-DHL1 Mn3xSpVv[3Srb36gZZN{[Xl? MkjKTY5pcWKrdHnvckBw\iCDTFugbY4hcHWvYX6gV3UuTEiOMTDj[YxteyCjc4Pld5Nm\CCjczDy[YR2[3Srb36gbY4hTVKNIIDoc5NxcG:{eXzheIlwdiCjdDDUNlAzNy:\MkC0JJJme2mmdXXzJIF1KDJyIITvJFgxKG6PIHHmeIVzKDFiaIKgZpkhX2W|dHXyckBjdG:2IHHuZYx6e2m| MnfoQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl{OEi5OFAoRjJ7Mki4PVQxRC:jPh?=
NCI-H3122 MnTJSpVv[3Srb36gZZN{[Xl? NUGyd2NMUW6qaXLpeIlwdiCxZjDBUGsheGixc4Doc5J6dGG2aX;uJIF1KFlzMke4JJJme2mmdXWgbY4hcHWvYX6gUmNKNUh|MUKyJINmdGy|IHH0JFIxKHSxIEiwJI5OKGGodHXyJFEhcHJiYomgW4V{fGW{bjDicI91KGGwYXz5d4l{ Mn7MQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl{OEi5OFAoRjJ7Mki4PVQxRC:jPh?=
NCI-H3122 MoewSpVv[3Srb36gZZN{[Xl? MYPJcohq[mm2aX;uJI9nKEGOSzDpckBpfW2jbjDOR2kuUDNzMkKgZ4VtdHNiYYPz[ZN{\WRiYYOgdoVlfWO2aX;uJIlvKFOWQWSzJJBpd3OyaH;yfYxifGmxbjDheEB[PzB3IILld4llfWViYYSgNlAhfG9iOECgcm0h[W[2ZYKgNUBpeiCkeTDX[ZN1\XKwIHLsc5Qh[W6jbInzbZM> MUe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTJ6OEm0NEc,Ojl{OEi5OFA9N2F-
NCI-H3122 NIXITnpHfW6ldHnvckBie3OjeR?= MlfrTY5pcWKrdHnvckBw\iCDTFugbY4hcHWvYX6gUmNKNUh|MUKyJINmdGy|IHHzd4V{e2WmIHHzJJJm\HWldHnvckBqdiCDa4SgdIhwe3Cqb4L5cIF1cW:wIHH0JHM1PzNicnXzbYR2\SCjdDCyNEB1dyB6MDDuUUBi\nSncjCxJIhzKGK7IGfld5Rmem5iYnzveEBidmGueYPpdy=> Mm\IQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl{OEi5OFAoRjJ7Mki4PVQxRC:jPh?=
NCI-H3122 NYHsN4w1TnWwY4Tpc44h[XO|YYm= NFvhRm9KdmirYnn0bY9vKG:oIFHMT{BqdiCqdX3hckBPS0lvSEOxNlIh[2WubIOgZZN{\XO|ZXSgZZMhemWmdXP0bY9vKGmwIFXST{BxcG:|cHjvdplt[XSrb36gZZQhXDJyMj:vXVIxPCC{ZYPp[JVmeyCjdDCyNEB1dyB6MDDuUUBi\nSncjCxJIhzKGK7IGfld5Rmem5iYnzveEBidmGueYPpdy=> NIfRfog9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUK4PFk1OCd-MkmyPFg6PDB:L3G+
Assay
Methods Test Index PMID
Western blot p-ALK / ALK 29650534
In vivo In rats, PF-06463922 displays low plasma clearance, a moderate volume of distribution, a reasonable half-life, low propensity for p-glycoprotein 1-mediated efflux and a bioavailability of 100%. [1] In vivo, PF-06463922 shows cytoreductive antitumor efficacy in the NIH3T3 xenograft models expressing human CD74-ROS1 and Fig-ROS1 via inhibition in ROS1 phosphorylation and the downstream signaling molecules, as well as inhibition of the cell cycle protein Cyclin D1 in tumors. [2] In vivo, PF-06463922 also demonstrates marked antitumor activity in mice bearing tumor xenografts expressing EML4-ALK, EML4-ALK-L1196M, EML4-ALK-G1269A, EML4-ALK-G1202R or NPM-ALK. [3]

Protocol (from reference)

Solubility (25°C)

In vitro

In vivo

Add solvents to the product individually and in order
(Data is from Selleck tests instead of citations):
2% DMSO+30% PEG 300+ddH2O
For best results, use promptly after mixing.

5mg/mL

Chemical Information

Molecular Weight 406.41
Formula

C21H19FN6O2

CAS No. 1454846-35-5
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC1C2=C(C=CC(=C2)F)C(=O)N(CC3=NN(C(=C3C4=CC(=C(N=C4)N)O1)C#N)C)C

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

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)

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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Frequently Asked Questions

Question 1:
Do you have any special suggestions for solution of S7536, Lorlatinib (PF-6463922) to be applied to mouse models?

Answer:
For S7536, we recommend 2% DMSO+30% PEG 300+ddH2O (up to 5mg/ml) for in vivo application.

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