Cat. No. 5640
Alternative Name: Lorlatinib
Chemical Name: (10R)-7-Amino-12-fluoro-10,15,16,17
Biological ActivityHigh affinity and selective ALK and ROS1 inhibitor (Ki values are <0.02, <0.07 and 0.7 nM for ROS1, wild-type ALK and ALK-L1196M, respectively). Exhibits >100-fold selectivity for ROS1 over a panel of 204 other kinases. Inhibits proliferation of BaF3 cells containing crizotinib-resistant ROS1 mutation in vitro. Inhibits tumor growth in relevant mouse models. Orally available and brain penetrant.
Licensing InformationSold for research purposes under agreement from Pfizer Inc.
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Certificate of Analysis / Product Datasheet / Safety Data Sheet
Zou et al (2015) PF-06463922 is a potent and selective next-generation ROS1/ALK inhibitor capable of blocking crizotinib-resistant ROS1 mutations. Proc.Natl.Acad.Sci.U.S.A. 112 3493. PMID: 25733882.
Johnson et al (2014) Discovery of (10R)-7-amino-12-fluoro-2,10,16-trimethyl-15-oxo-10,15,16,17-tetrahydro-2H-8,4-(metheno)pyrazolo[4,3-h][2,5,11]-benzoxadiazacyclotetradecine-3-carbonitrile (PF-06463922), a macrocyclic inhibitor of anaplastic lymphoma kinase (ALK) and c-ros oncogene 1 (ROS1) with preclinical brain exposure and broad-spectrum potency against ALK-resistant mutations. J.Med.Chem. 57 4720. PMID: 24819116.
If you know of a relevant reference for this product please let us know.
Citations are publications that use Tocris products.
Do you know of a great paper that uses PF 06463922 from Tocris? If so please let us know.
View Related Products by Target
View Related Products by Product Action
Keywords: PF 06463922, supplier, anaplastic, lymphoma, kinases, (ALK), inhibitors, inhibits, inhibition, ROS1, c-ros, oncogenes, cancer, PF06463922, Tocris Bioscience, ALK Inhibitor products
Find multiple products by catalog number
New Products in this Area
Potent and selective PDGFR inhibitorGSK 1363089
Potent inhibitor of MET, VEGFR2, Ron and AXLPF 06273340
Potent and selective pan-Trk inhibitor; peripherally restricted
Follow @Tocris on Twitter
Tocris is now actively tweeting. For regular updates on news, events and special offers, follow @Tocris on Twitter.