Lorlatinib (PF-6463922)
Catalog No.S7536
Molecular Weight(MW): 406.41
PF-06463922 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. Phase 1.
3 Customer Reviews
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Sub-G1 and cell cycle phase distribution of NBLW and NBLW-R cells treated for 24 hours with DMSO, 1× or 10× the respective GI 50 concentrations of PF-06463922.
Oncotarget, 2016, DOI: 10.18632/oncotarget.13541.. Lorlatinib (PF-6463922) purchased from Selleck.
NIH 3T3 cells expressing the indicated ALK variants were treated with increasing concentrations of lorlatinib (B) for 72 hours. Propidium iodide (PI) and Hoechst 33342 were added and allowed to incubate for 20 minutes before imaging on the ImageXpress. Dose-response curves were generated by determining total live cells (# of Hoechst-positive cells minus # of PI-positive cells) at each dose. A nonlinear regression of the data is represented here.
Mol Cancer Res, 2018, 10.1158/1541-7786.MCR-18-0171. Lorlatinib (PF-6463922) purchased from Selleck.
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H2228 cells were treated with the ALK-inhibitors, alectinib (500 nM), ceritinib (500 nM) and lorlatinib (100 nM) alone or with saracatinib (1 µM).
Int J Oncol, 2017, 51(5):1533-1540. Lorlatinib (PF-6463922) purchased from Selleck.
Purity & Quality Control
Choose Selective ALK Inhibitors
Biological Activity
| Description | PF-06463922 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. 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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| 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
Solubility (25°C)
| In vitro | DMSO | 81 mg/mL warmed (199.3 mM) |
|---|---|---|
| Ethanol | 30 mg/mL warmed (73.81 mM) | |
| Water | Insoluble | |
| 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 |
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Chemical Information
| Molecular Weight | 406.41 |
|---|---|
| Formula | C21H19FN6O2 |
| CAS No. | 1454846-35-5 |
| Storage | powder |
| in solvent | |
| Synonyms | N/A |
Bio Calculators
Molarity Calculator
Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:
Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)
*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).
Dilution Calculator
Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:
Concentration (start) x Volume (start) = Concentration (final) x Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )
* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).
Molecular Weight Calculator
Enter the chemical formula of a compound to calculate its molar mass and elemental composition:
Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2
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Definitions of molecular mass, molecular weight, molar mass and molar weight:
Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
Molarity Calculator
Clinical Trial Information
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT03439215 | Recruiting | Carcinoma Non-Small-Cell Lung | Fondazione Ricerca Traslazionale|Clinical Research Technology S.r.l. | June 13 2017 | Phase 2 |
| NCT02838264 | Completed | Healthy | Pfizer | August 16 2016 | Phase 1 |
| NCT02804399 | Completed | Healthy | Pfizer | July 2016 | Phase 1 |
| NCT02569554 | Completed | Healthy | Pfizer | December 2015 | Phase 1 |
| NCT02584634 | Active not recruiting | Non-Small Cell Lung Cancer | Pfizer | December 18 2015 | Phase 2 |
| NCT02564562 | Completed | Healthy | Pfizer | October 2015 | Phase 1 |
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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