PF 06463922

Cat. No. 5640

PF 06463922 C21H19FN6O2 [1454846-35-5]

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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

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.

Licensing Information

Sold for research purposes under agreement from Pfizer Inc.

Technical Data

M.Wt:
406.41
Formula:
C21H19FN6O2
Solubility:
Soluble to 100 mM in DMSO and to 100 mM in ethanol
Purity:
>98 %
Storage:
Store at -20°C
CAS No:
1454846-35-5

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.

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Keywords: PF 06463922, supplier, anaplastic, lymphoma, kinases, (ALK), inhibitors, inhibits, inhibition, ROS1, c-ros, oncogenes, cancer, PF06463922, Tocris Bioscience, ALK Inhibitor products

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