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.
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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.
Purity & Quality Control
Choose Selective ALK Inhibitors
|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.|
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.  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. PF-06463922 also shows potent growth inhibitory activity and induces apoptosis in the NSCLC cells harboring either non-mutant ALK or mutant ALK fusions. 
|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%.  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.  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. |
|In vitro||DMSO||81 mg/mL warmed (199.3 mM)|
|Ethanol||30 mg/mL warmed (73.81 mM)|
|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.
Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)
Concentration (start) x Volume (start) = Concentration (final) x Volume (final)
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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|
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Frequently Asked Questions
Do you have any special suggestions for solution of S7536, Lorlatinib (PF-6463922) to be applied to mouse models?
For S7536, we recommend 2% DMSO+30% PEG 300+ddH2O (up to 5mg/ml) for in vivo application.