PF 06463922
Chemical Name: (10R)-7-Amino-12-fluoro-10,15,16,17-tetrahydro-2,10,16-trimethyl-15-oxo-2H-4,8-methenopyrazolo[4,3-h][2,5,11]benzoxadiazacyclotetradecine-3-carbonitrile
Purity: ≥98%
Biological Activity
High 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.Technical Data
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Additional Information
Background References
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PF-06463922 is a potent and selective next-generation ROS1/ALK inhibitor capable of blocking crizotinib-resistant ROS1 mutations.
Zou et al.
Proc.Natl.Acad.Sci.U.S.A., 2015;112:3493 -
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 lympho
Johnson et al.
J.Med.Chem., 2014;57:4720
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Citation for PF 06463922
The citations listed below are publications that use Tocris products. Selected citations for PF 06463922 include:
1 Citation: Showing 1 - 1
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ALKALs are in vivo ligands for ALK family receptor tyrosine kinases in the neural crest and derived cells.
Authors: Fadeev Et al.
Proc Natl Acad Sci U S A 2018;115:E630
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