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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.
CAS No. 1454846-35-5
Selleck's Lorlatinib (PF-6463922) has been cited by 41 publications
Purity & Quality Control
Choose Selective ALK Inhibitors
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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. | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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| Targets |
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| 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] |
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| Cell Data |
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| Assay |
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| 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)
| References |
|
|---|
Solubility (25°C)
|
In vitro |
DMSO |
81 mg/mL
warmed (199.3 mM) |
| Water |
Insoluble
|
|
| Ethanol |
'30 mg/mL
warmed |
|
|
In vivo |
Add solvents to the product individually and in order |
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.
Clinical Trial Information
| 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 |
(data from https://clinicaltrials.gov, updated on 2022-01-17)
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.
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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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